Page last updated: 2024-12-07

artenimol

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Description

artenimol: derivative of antimalarial drug artemisinin (quinghaosu) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11358077
CHEMBL ID511326
CHEBI ID168754
SCHEMBL ID18744731
MeSH IDM0117179
PubMed CID456410
CHEMBL ID307261
SCHEMBL ID2132158
MeSH IDM0117179
PubMed CID10221470
CHEMBL ID252518
SCHEMBL ID19937859
MeSH IDM0117179

Synonyms (73)

Synonym
(1r,4s,5r,8s,9r,10r,12r,13r)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecan-10-ol
CHEBI:168754
(3r,5as,6r,8as,9r,10s,12r,12ar)-decahydro-3,6,9-trimethyl-3,12-epoxy-12h-pyrano(4,3-j)-1,2-benzodioxepin-10-ol
(3r,5as,6r,8as,9r,10s,12r,12ar)-decahydro-3,6,9-trimethyl-3,12-epoxy-12h-pyrano(4,3,-j)-1,2-benzodioxepin-10-ol
x0uiv26abx ,
nsc 758682
unii-x0uiv26abx
dtxsid5045962 ,
nsc-758682
(1r,4s,5r,8s,9r,10r,12r,13r)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.0^{4,13}.0^{8,13}]hexadecan-10-ol
artenimol [inn]
3,12-epoxy-12h-pyrano(4,3-j)-1,2-benzodioxepin-10-ol, decahydro-3,6,9-trimethyl-, (3r-(3.alpha.,5a.beta.,6.beta.,8a.beta.,9.alpha.,10.beta.,12.beta.,12ar*))-
.alpha.-dihydroartemisinin
dihydroartimisinin
3,12-epoxy-12h-pyrano(4,3-j)-1,2-benzodioxepin-10-ol, decahydro-3,6,9-trimethyl-, (3r,5as,6r,8as,9r,10r,12r,12ar)-
S2290
(3r,5as,6r,8as,9r,10s,12r,12ar)-decahydro-3,6,9-trimethyl-3,12-epoxy-12h-pyrano[4,3-j]-1,2-benzodioxepin-10-ol
AKOS022168199
Q-100792
SCHEMBL18744731
alpha-dihydroartemisinin
NCGC00346590-02
123930-80-3
CCG-267307
Q27293233
(1s,4s,5r,8s,9r,12r,13r)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecan-10-ol
dhqhs 1; -dihydroartemisinin
CHEMBL511326
(1r,4s,5r,8s,9r,10r,12r,13r)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.0?,??.0?,??]hexadecan-10-ol
EN300-7407671
AC-2067
3,12-epoxy-12h-pyrano(4,3-j)-1,2-benzodioxepin-10-ol, decahydro-3,6,9-trimethyl-, (3r-(3alpha,5abeta,6beta,8abeta,9alpha,10alpha,12beta,12ar*))-
D07362
artenimol (inn)
dihydroquinghoasu
jav-110
vm3352
[3r-(3.alpha.,5a.beta.,6.beta.,8a.beta.,9.alpha.,10.alpha.,12.beta.,12ar*)]-decahydro-10-hydroxy-3,6,9-trimethyl-3,12-epoxy-12h-pyrano[4.3-j]-1,2-benzodioxepin
D3793
SCHEMBL2132158
CHEMBL307261 ,
AKOS015962875
unii-6a9o50735x
beta-dihydroartemisinin
dhqhs 2
artemisinin, dihydro
dihydroartemisinin + proveblue
AKOS026749923
BJDCWCLMFKKGEE-KXTPALSWSA-N
bdbm50578409
(4s,5r,8s,9r,10s,12r,13r)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.0?,.0?,]hexadecan-10-ol
EN300-27122030
PD087060
artenimol
dihydroqinghaosu
cotexin
cotecxin
dihydroartemisinine
alaxin
salaxin
santecxin
artenimolum
di-hydroqinghaosu
.beta.-dihydroartemisinin
dihydroartemisinin, .beta.-
CHEMBL252518
dynamax
(1s,4s,5r,8s,9r,10s,12r,13r)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.0^{4,13}.0^{8,13}]hexadecan-10-ol
(1s,4s,5r,8s,9r,10s,12r,13r)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecan-10-ol
SCHEMBL19937859
EN300-19873907
1279039-00-7
FS-7037

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" This selective uptake may explain why the artemisinin derivatives are selectively toxic to malaria parasites."( Artemisinin neurotoxicity: neuropathology in rats and mechanistic studies in vitro.
Hossler, P; Kamchonwongpaisan, S; McKeever, P; Meshnick, SR; Ziffer, H, 1997
)
0.3
" In this assay, dihydroartemisinin is significantly more toxic than artemether or arteether."( In vitro neurotoxicity of artemisinin derivatives.
McLean, WG; Ward, SA, 1998
)
0.3
" These data indicate that once and twice daily oral administration of artemether, artesunate and dihydroartemisinin is relatively safe when compared to intramuscular administration of the oil-based compounds."( Assessment of the neurotoxicity of oral dihydroartemisinin in mice.
Looareesuwan, S; Nontprasert, A; Prakongpan, S; Pukrittayakamee, S; Supanaranond, W; White, NJ,
)
0.13
"Artekin is safe and effective combination therapy for uncomplicated malaria in children and adults."( Safety evaluation of fixed combination piperaquine plus dihydroartemisinin (Artekin) in Cambodian children and adults with malaria.
Davis, TM; Denis, MB; Hung, TY; Ilett, KF; Karunajeewa, H; Lim, C; Socheat, D, 2004
)
0.32
" Adverse events and clinical and parasitological outcomes were recorded."( Safety and efficacy of dihydroartemisinin/piperaquine (Artekin) for the treatment of uncomplicated Plasmodium falciparum malaria in Rwandan children.
D'Alessandro, U; Fanello, CI; Karema, C; Ngamije, D; van Doren, W; van Geertruyden, JP; van Overmeir, C, 2006
)
0.33
" We found dihydroartemisinin (5-25 microM) inhibited the growth and induced apoptosis of C6 cells in a concentration- and time-dependent manner; however, it was much less toxic to rat primary astrocytes."( Dihydroartemisinin exerts cytotoxic effects and inhibits hypoxia inducible factor-1alpha activation in C6 glioma cells.
Huang, XJ; Lu, YB; Ma, ZQ; Wei, EQ; Zhang, WP, 2007
)
0.34
"Dihydroartemisinin-piperaquine, a fixed-dose combination antimalarial, is an inexpensive, safe and highly effective treatment for uncomplicated falciparum or vivax malaria."( Efficacy and safety of dihydroartemisinin-piperaquine.
Ashley, EA; Day, NP; Myint, HY; Nosten, F; White, NJ, 2007
)
0.34
" Adverse events were monitored and laboratory parameters on study Days 0, 2, 5, and 7 post drug administrations were analyzed."( Comparative study of dihydroartemisinin and artesunate safety in healthy Thai volunteers.
Atipas, S; Chatsiricharoenkul, S; Kaewkungwal, J; Khuhapinant, A; Kongpatanakul, S, 2009
)
0.35
" All adverse events were mild."( Comparative study of dihydroartemisinin and artesunate safety in healthy Thai volunteers.
Atipas, S; Chatsiricharoenkul, S; Kaewkungwal, J; Khuhapinant, A; Kongpatanakul, S, 2009
)
0.35
" Participants were actively monitored for adverse events for 28 days and then passively for up to 63 days after treatment."( Safety and tolerability of artemether-lumefantrine versus dihydroartemisinin-piperaquine for malaria in young HIV-infected and uninfected children.
Arinaitwe, E; Bigira, V; Dorsey, G; Gasasira, A; Homsy, J; Kakuru, A; Kamya, MR; Katrak, S; Sandison, TG; Tappero, JW; Wanzira, H, 2009
)
0.35
" Most adverse events were rare, with only cough, diarrhoea, vomiting, and anaemia occurring in more than 1% of treatments."( Safety and tolerability of artemether-lumefantrine versus dihydroartemisinin-piperaquine for malaria in young HIV-infected and uninfected children.
Arinaitwe, E; Bigira, V; Dorsey, G; Gasasira, A; Homsy, J; Kakuru, A; Kamya, MR; Katrak, S; Sandison, TG; Tappero, JW; Wanzira, H, 2009
)
0.35
"Both AL and DP were safe and well tolerated for the treatment of uncomplicated malaria in young HIV-infected and uninfected children."( Safety and tolerability of artemether-lumefantrine versus dihydroartemisinin-piperaquine for malaria in young HIV-infected and uninfected children.
Arinaitwe, E; Bigira, V; Dorsey, G; Gasasira, A; Homsy, J; Kakuru, A; Kamya, MR; Katrak, S; Sandison, TG; Tappero, JW; Wanzira, H, 2009
)
0.35
"04), there were no differences between treatment arms in the occurrence of adverse events."( Safety and efficacy of dihydroartemisinin-piperaquine versus artemether-lumefantrine in the treatment of uncomplicated Plasmodium falciparum malaria in Zambian children.
Chaponda, M; D'Alessandro, U; Hachizovu, S; Mukwamataba, D; Mulenga, M; Nambozi, M; Ubben, D; Van Geertruyden, JP, 2011
)
0.37
"DHA/PQP was as efficacious, safe and well tolerated in treatment of uncomplicated malaria as AL, though in the latter group more new infections during the follow up were observed."( Safety and efficacy of dihydroartemisinin-piperaquine versus artemether-lumefantrine in the treatment of uncomplicated Plasmodium falciparum malaria in Zambian children.
Chaponda, M; D'Alessandro, U; Hachizovu, S; Mukwamataba, D; Mulenga, M; Nambozi, M; Ubben, D; Van Geertruyden, JP, 2011
)
0.37
" Few and mild adverse events were reported."( Efficacy and safety of artemisinin-naphthoquine versus dihydroartemisinin-piperaquine in adult patients with uncomplicated malaria: a multi-centre study in Indonesia.
Amansyah, F; Dedang, TA; Driyah, S; Ekowatiningsih, R; Hasugian, AR; Januar, L; Labora, J; Prasetyorini, B; Purnama, A; Purnamasari, T; Salwati, E; Siswantoro, H; Tjitra, E; Wijayanto, B; Yusnita, EA; Yuwarni, E, 2012
)
0.38
"AN and DHP are confirmed very effective, safe and tolerate for treatment of any malaria."( Efficacy and safety of artemisinin-naphthoquine versus dihydroartemisinin-piperaquine in adult patients with uncomplicated malaria: a multi-centre study in Indonesia.
Amansyah, F; Dedang, TA; Driyah, S; Ekowatiningsih, R; Hasugian, AR; Januar, L; Labora, J; Prasetyorini, B; Purnama, A; Purnamasari, T; Salwati, E; Siswantoro, H; Tjitra, E; Wijayanto, B; Yusnita, EA; Yuwarni, E, 2012
)
0.38
" Both DP and A + M were well tolerated, with the majority of adverse events of mild or moderate severity."( Therapeutic efficacy and safety of dihydroartemisinin-piperaquine versus artesunate-mefloquine in uncomplicated Plasmodium falciparum malaria in India.
Bacchieri, A; Bhattacharyya, PC; Corsi, M; Dev, V; Dubashi, N; Gargano, N; Ghosh, SK; Kumar, A; Rao, BH; Srivastava, B; Tommasini, S; Ubben, D; Valecha, N, 2012
)
0.38
" No neurological or cardiac toxicity was observed and seven dogs exhibited no adverse effects at all."( Safety and efficacy field study of artesunate for dogs with non-resectable tumours.
Efferth, T; Erich, SA; Fleckenstein, L; Grinwis, GC; London, CA; Mol, JA; Rutteman, GR; Spee, B, 2013
)
0.39
" No serious adverse event was noted during the study period."( Monitoring the efficacy and safety of three artemisinin based-combinations therapies in Senegal: results from two years surveillance.
Abiola, A; Faye, B; Folly, K; Gaye, O; Lo, AC; Ndiaye, JL; Ndiaye, LA; Ndiaye, M; Sow, D; Sylla, K; Tine, RC, 2013
)
0.39
"In the context of scaling up of ACTs in Senegal, ASAQ, AL and DHAPQ are highly effective and safe antimalarial drugs."( Monitoring the efficacy and safety of three artemisinin based-combinations therapies in Senegal: results from two years surveillance.
Abiola, A; Faye, B; Folly, K; Gaye, O; Lo, AC; Ndiaye, JL; Ndiaye, LA; Ndiaye, M; Sow, D; Sylla, K; Tine, RC, 2013
)
0.39
" Incidence of adverse events was related to underlying disease; malaria being reported in both treatment arms."( Efficacy and safety of artemether-lumefantrine and dihydroartemisinin-piperaquine in the treatment of uncomplicated Plasmodium falciparum malaria in Kenyan children aged less than five years: results of an open-label, randomized, single-centre study.
Akhwale, W; Eyase, F; Johnson, JD; Juma, E; Koskei, N; Obonyo, C; Ogutu, BR; Omollo, R; Omondi, EK; Ongecha, JM; Onyango, KO; Otieno, GA; Otieno, L; Perkins, DJ, 2014
)
0.4
" Both ACT regimens were safe and well tolerated."( Artemisinin-based combination therapies are efficacious and safe for treatment of uncomplicated malaria in HIV-infected Ugandan children.
Achan, J; Arinaitwe, E; Charlebois, E; Clark, TD; Dorsey, G; Havlir, D; Ikilezi, G; Kakuru, A; Kamya, MR; Muhindo, MK; Mwangwa, F; Rosenthal, PJ; Ruel, T; Tappero, JW, 2014
)
0.4
"Treatment of uncomplicated malaria with AL or DP was efficacious and safe in HIV-infected children taking ART."( Artemisinin-based combination therapies are efficacious and safe for treatment of uncomplicated malaria in HIV-infected Ugandan children.
Achan, J; Arinaitwe, E; Charlebois, E; Clark, TD; Dorsey, G; Havlir, D; Ikilezi, G; Kakuru, A; Kamya, MR; Muhindo, MK; Mwangwa, F; Rosenthal, PJ; Ruel, T; Tappero, JW, 2014
)
0.4
"9% of side reaction with 7 cases suffering from mild adverse responses among 71 of full-course medication."( [Therapeutic efficacy and safety of compound dihydroartemisinin/piperaquine for uncomplicated Plasmodium falciparum infection in Laiza City of Myanmar bordering on China].
Deng, Y; Lasi, JH; Sun, XD; Sun, XY; Wang, H; Wang, J; Yang, YC; Zhang, ZX, 2011
)
0.37
"DHAPIP is efficacious and safe for the treatment of uncomplicated falciparum malaria in Laiza city of Myanmar in the border area."( [Therapeutic efficacy and safety of compound dihydroartemisinin/piperaquine for uncomplicated Plasmodium falciparum infection in Laiza City of Myanmar bordering on China].
Deng, Y; Lasi, JH; Sun, XD; Sun, XY; Wang, H; Wang, J; Yang, YC; Zhang, ZX, 2011
)
0.37
" Even without a clear synergistic interaction, the combination of DHA and SS provides a safe and affordable form of cancer treatment."( Additive cytotoxic effects of dihydroartemisinin and sodium salicylate on cancer cells.
Singh, NP; Wickerath, M, 2014
)
0.4
" There were no differences between the study arms in the incidence of serious adverse events during the intervention and the incidence of malaria during the 1-y period after the intervention was stopped."( Protective efficacy and safety of three antimalarial regimens for the prevention of malaria in young Ugandan children: a randomized controlled trial.
Achan, J; Aweeka, FT; Bigira, V; Clark, TD; Dorsey, G; Havlir, DV; Huang, L; Kamya, MR; Kapisi, J; Kinara, S; Muhindo, MK; Mwangwa, F; Osterbauer, B; Rosenthal, PJ, 2014
)
0.4
" No statistical significant differences were observed in the occurrence of adverse events among treatment groups."( Randomized non-inferiority and safety trial of dihydroartemisin-piperaquine and artesunate-amodiaquine versus artemether-lumefantrine in the treatment of uncomplicated Plasmodium falciparum malaria in Cameroonian children.
Ali, IM; Chedjou, JP; Ekollo, AM; Evehe, MS; Froeschl, G; Heumann, C; Mansmann, U; Mbacham, WF; Moyeh, MN; Ndikum, VN; Ngongang, EO; Nji, AM; Ogundahunsi, O, 2015
)
0.42
" Patients were contacted on day 5 ± 2 to assess adherence and adverse events (AEs)."( Prospective observational study to evaluate the clinical safety of the fixed-dose artemisinin-based combination Eurartesim® (dihydroartemisinin/piperaquine), in public health facilities in Burkina Faso, Mozambique, Ghana, and Tanzania.
Abdulla, S; Adjei, A; Adjuik, M; Akparibo, R; Baiden, R; Binka, F; Compaoré, G; Gyapong, M; Halidou, T; Macete, E; Mulokozi, A; Oduro, A; Ogutu, B; Osei, I; Owusu-Agyei, S; Sevene, E; Sie, A; Smith, P; Upunda, GL; Valea, I; Yawson, A, 2015
)
0.42
" Most patients,95% (10,359/10,925), did not report any adverse event following at least one dose of Eurartesim®."( Prospective observational study to evaluate the clinical safety of the fixed-dose artemisinin-based combination Eurartesim® (dihydroartemisinin/piperaquine), in public health facilities in Burkina Faso, Mozambique, Ghana, and Tanzania.
Abdulla, S; Adjei, A; Adjuik, M; Akparibo, R; Baiden, R; Binka, F; Compaoré, G; Gyapong, M; Halidou, T; Macete, E; Mulokozi, A; Oduro, A; Ogutu, B; Osei, I; Owusu-Agyei, S; Sevene, E; Sie, A; Smith, P; Upunda, GL; Valea, I; Yawson, A, 2015
)
0.42
" The primary endpoint was the PCR-corrected adequate clinical and parasitological response (ACPR) at day 28 (D28); the secondary endpoints included ACPR at D42, clearance times for parasites, fever, and gametocytes, and the incidence of adverse events."( [Evaluation of the efficacy and safety of three 2-drug combinations for the treatment of uncomplicated Plasmodium falciparum malaria in Senegal: artesunate-amodiaquine, dihydroartemisinin-piperaquine, and artemether-lumefantrine].
Abiola, A; Ba, MS; Dieng, Y; Faye, B; Gaye, O; Lo, AC; Ndiaye, JL; Ndiaye, M; Pene, M; Seck, A; Sow, D; Sylla, K; Tine, RC,
)
0.13
" The combinations were well tolerated, with no serious adverse events reported during the follow-up period."( [Evaluation of the efficacy and safety of three 2-drug combinations for the treatment of uncomplicated Plasmodium falciparum malaria in Senegal: artesunate-amodiaquine, dihydroartemisinin-piperaquine, and artemether-lumefantrine].
Abiola, A; Ba, MS; Dieng, Y; Faye, B; Gaye, O; Lo, AC; Ndiaye, JL; Ndiaye, M; Pene, M; Seck, A; Sow, D; Sylla, K; Tine, RC,
)
0.13
" Monthly IPT-DP was associated with fewer serious adverse events than placebo, daily co-trimoxazole, or monthly SP."( Safety, tolerability, and efficacy of repeated doses of dihydroartemisinin-piperaquine for prevention and treatment of malaria: a systematic review and meta-analysis.
Dorsey, G; Gutman, J; Kovacs, S; Stergachis, A; Ter Kuile, FO, 2017
)
0.46
" Moreover, in mice, ARS4 inhibited growth and intraperitoneal dissemination and metastasis of ovarian cancer cells without observable toxic effects."( Preclinical Efficacy and Safety Assessment of Artemisinin-Chemotherapeutic Agent Conjugates for Ovarian Cancer.
Ba, Q; Chen, K; Chen, T; Li, J; Li, X; Liu, H; Liu, Y; Wang, H; Zhang, X; Zhou, Y, 2016
)
0.43
"Uncommon and rare adverse events (AEs), with delayed onset may not be detected before new drugs are licensed and deployed."( Post-licensure safety evaluation of dihydroartemisinin piperaquine in the three major ecological zones across Ghana.
Adjei, A; Adjuik, M; Baiden, R; Binka, F; Gyapong, M; Oduro, AR; Osei, I; Owusu-Agyei, S; Sobe, E; Yawson, A, 2017
)
0.46
" There were nine adverse events of special interest (AESI); itching/pruritus (7), dizziness (1), and skin lesions (1)."( Post-licensure safety evaluation of dihydroartemisinin piperaquine in the three major ecological zones across Ghana.
Adjei, A; Adjuik, M; Baiden, R; Binka, F; Gyapong, M; Oduro, AR; Osei, I; Owusu-Agyei, S; Sobe, E; Yawson, A, 2017
)
0.46
" Dizziness, nausea, vomiting, headache and asthenia as adverse events (AEs) were more common in MQAS than in AL or DHAPQ (p < 0."( Artemisinin-based combination therapy in pregnant women in Zambia: efficacy, safety and risk of recurrent malaria.
Buyze, J; D'Alessandro, U; Hachizovu, S; Kabuya, JB; Kasongo, W; Mulenga, J; Mulenga, M; Mwakazanga, D; Nambozi, M; Van Geertruyden, JP, 2017
)
0.46
" Its adverse effects are generally tolerable and temporary."( Choreoathetosis - an unusual adverse effect of dihydroartemisinin-piperaquine: a case report.
Kadia, BM; Morfaw, C; Simo, ACG, 2017
)
0.46
"Although dihydroartemisinin-piperaquine is increasingly popular as a well-tolerated/efficacious antimalarial drug, clinicians must note the rare possibility of choreoathetosis as an adverse effect of this medication and educate patients accordingly."( Choreoathetosis - an unusual adverse effect of dihydroartemisinin-piperaquine: a case report.
Kadia, BM; Morfaw, C; Simo, ACG, 2017
)
0.46
" However, whether DHA has adverse effects on oocyte maturation is unknown."( Toxicity and related mechanisms of dihydroartemisinin on porcine oocyte maturation in vitro.
Che, MJ; Fu, XW; Hou, YP; Liu, C; Liu, HG; Luo, Y, 2018
)
0.48
" After exclusion of blue urine, adverse events were similar across all groups (59 [74%] of 80 participants had 162 adverse events overall, 145 [90%] of which were mild)."( Efficacy and safety of primaquine and methylene blue for prevention of Plasmodium falciparum transmission in Mali: a phase 2, single-blind, randomised controlled trial.
Bousema, T; Bradley, J; Brown, JM; Chen, I; Diarra, K; Diawara, H; Dicko, A; Drakeley, C; Gosling, R; Hwang, J; Issiaka, D; Keita, S; Kone, DT; Lanke, K; Mahamar, A; McCulloch, C; Müller, O; Roh, ME; Sanogo, K; Soumare, HM; Srinivasan, V; Stone, WJR; Traore, SF, 2018
)
0.48
" Additional outcomes included intervention coverage, treatment adherence, occurrence of adverse events, and cumulative incidences 3, 12, and 16 months post-MDA."( A cluster randomised controlled trial of two rounds of mass drug administration in Zanzibar, a malaria pre-elimination setting-high coverage and safety, but no significant impact on transmission.
Ali, AS; Ali, SM; Aydin-Schmidt, B; Bennett, A; Björkman, A; Hodzic, L; Islam, A; Jovel, I; Khamis, M; Magnusson, E; Mårtensson, A; Mkali, H; Morris, U; Msellem, MI; Poirot, E; Sachs, MC; Shija, SJ; Tarning, J, 2018
)
0.48
" Adverse events were reported in 11."( A cluster randomised controlled trial of two rounds of mass drug administration in Zanzibar, a malaria pre-elimination setting-high coverage and safety, but no significant impact on transmission.
Ali, AS; Ali, SM; Aydin-Schmidt, B; Bennett, A; Björkman, A; Hodzic, L; Islam, A; Jovel, I; Khamis, M; Magnusson, E; Mårtensson, A; Mkali, H; Morris, U; Msellem, MI; Poirot, E; Sachs, MC; Shija, SJ; Tarning, J, 2018
)
0.48
"Plasmodium falciparum and Plasmodium vivax infections are important causes of adverse pregnancy outcomes in the Asia-Pacific region."( Efficacy and safety of intermittent preventive treatment and intermittent screening and treatment versus single screening and treatment with dihydroartemisinin-piperaquine for the control of malaria in pregnancy in Indonesia: a cluster-randomised, open-la
Adams, ER; Ahmed, R; Asih, PBS; Chen, T; Faragher, B; Khairallah, C; Lukito, T; Maratina, SS; Pace, C; Poespoprodjo, JR; Price, RN; Santana-Morales, MA; Smedley, J; Syafruddin, D; Ter Kuile, FO; Unwin, VT; Wang, D; Williams, CT, 2019
)
0.51
" Conditions related to the pregnancy, the puerperium, and the perinatal period were the most common serious adverse events for the mothers, and infections and infestations for the infants."( Efficacy and safety of intermittent preventive treatment and intermittent screening and treatment versus single screening and treatment with dihydroartemisinin-piperaquine for the control of malaria in pregnancy in Indonesia: a cluster-randomised, open-la
Adams, ER; Ahmed, R; Asih, PBS; Chen, T; Faragher, B; Khairallah, C; Lukito, T; Maratina, SS; Pace, C; Poespoprodjo, JR; Price, RN; Santana-Morales, MA; Smedley, J; Syafruddin, D; Ter Kuile, FO; Unwin, VT; Wang, D; Williams, CT, 2019
)
0.51
" They received a directly-observed 3-day standard treatment of DPQ and were followed up until day 63 for malaria infection and adverse events."( Efficacy and safety of dihydroartemisinin-piperaquine for treatment of Plasmodium falciparum uncomplicated malaria in adult patients on antiretroviral therapy in Malawi and Mozambique: an open label non-randomized interventional trial.
Banda, CG; Kalilani-Phiri, L; Khoo, SH; Lalloo, DG; Macuacua, S; Maculuve, S; Mallewa, J; Mukaka, M; Mwapasa, V; Piqueras, M; Sevene, E; Terlouw, DJ; Vala, A, 2019
)
0.51
"DPQ was highly efficacious and safe for the treatment of malaria in HIV-infected patients concurrently taking efavirenz- or nevirapine-based ART, despite known pharmacokinetic interactions between dihydroartemisinin-piperaquine and efavirenz- or nevirapine-based ART regimens."( Efficacy and safety of dihydroartemisinin-piperaquine for treatment of Plasmodium falciparum uncomplicated malaria in adult patients on antiretroviral therapy in Malawi and Mozambique: an open label non-randomized interventional trial.
Banda, CG; Kalilani-Phiri, L; Khoo, SH; Lalloo, DG; Macuacua, S; Maculuve, S; Mallewa, J; Mukaka, M; Mwapasa, V; Piqueras, M; Sevene, E; Terlouw, DJ; Vala, A, 2019
)
0.51
" Adverse events were assessed within four hours of drugs intake."( Efficacy and safety of praziquantel and dihydroartemisinin piperaquine combination for treatment and control of intestinal schistosomiasis: A randomized, non-inferiority clinical trial.
Aklillu, E; Kamuhabwa, A; Kinung'hi, S; Minzi, O; Mnkugwe, RH, 2020
)
0.56
"4%) of the study participants experienced mild and transient treatment-associated adverse events, post-treatment abdominal pain (27."( Efficacy and safety of praziquantel and dihydroartemisinin piperaquine combination for treatment and control of intestinal schistosomiasis: A randomized, non-inferiority clinical trial.
Aklillu, E; Kamuhabwa, A; Kinung'hi, S; Minzi, O; Mnkugwe, RH, 2020
)
0.56
" Both treatments were safe and well-tolerated."( Efficacy and safety of dihydroartemisinin-piperaquine versus artemether-lumefantrine for treatment of uncomplicated Plasmodium falciparum malaria in Ugandan children: a systematic review and meta-analysis of randomized control trials.
Assefa, DG; Bekele, D; Getachew, E; Joseph, M; Manyazewal, T; Tesfahunei, HA; Zeleke, ED, 2021
)
0.62
" Adverse events (AE) were collected, with a special focus on cardiovascular safety by including electrocardiogram QT intervals evaluated after correction with either Bazett's (QTcB) or Fridericia's (QTcF) methods, at baseline and after treatment."( Longitudinal study based on a safety registry for malaria patients treated with artenimol-piperaquine in six European countries.
Angheben, A; Bacchieri, A; Bardají, A; Behrens, RH; Bisoffi, Z; Bottieau, E; Bouchaud, O; Bourhis, Y; Calleri, G; Duparc, S; Hatz, C; Iannucelli, M; Jelinek, T; Martin, C; Mattera, GG; Mechain, M; Merlo Pich, E; Nothdurft, HD; Ramos, JM; Rapp, C; Rojo-Marcos, G; Salas-Coronas, J; Tommasini, S; Velasco, M; Vignier, N; Visser, LG, 2021
)
0.62
" Reactive focal mass drug administration (rfMDA) may be safe and more effective."( Effectiveness and safety of reactive focal mass drug administration (rfMDA) using dihydroartemisinin-piperaquine to reduce malaria transmission in the very low-endemic setting of Eswatini: a pragmatic cluster randomised controlled trial.
Baltzell, K; Benjamin-Chung, J; Bhangu, K; Dlamini, B; Dlamini, N; Dufour, MK; Gosling, R; Greenhouse, B; Helb, D; Hsiang, MS; Kalungero, M; Kunene, S; Malambe, C; Maphalala, G; Mngadi, N; Nhlabathi, N; Ntshalintshali, N; Pindolia, D; Prach, LM; Tesfa, G; Vilakati, S; Whittemore, B, 2021
)
0.62
" No serious adverse events occurred."( Effectiveness and safety of reactive focal mass drug administration (rfMDA) using dihydroartemisinin-piperaquine to reduce malaria transmission in the very low-endemic setting of Eswatini: a pragmatic cluster randomised controlled trial.
Baltzell, K; Benjamin-Chung, J; Bhangu, K; Dlamini, B; Dlamini, N; Dufour, MK; Gosling, R; Greenhouse, B; Helb, D; Hsiang, MS; Kalungero, M; Kunene, S; Malambe, C; Maphalala, G; Mngadi, N; Nhlabathi, N; Ntshalintshali, N; Pindolia, D; Prach, LM; Tesfa, G; Vilakati, S; Whittemore, B, 2021
)
0.62
" Imatinib + SOC-treated participants exhibited no increase in number or severity of adverse events, a significantly accelerated decline in parasite density and pyrexia, and no DPC."( Imatinib augments standard malaria combination therapy without added toxicity.
Chien, HD; Kesely, KR; Low, PS; Noomuna, P; Pantaleo, A; Putt, KS; Tuan, TA; Turrini, FM, 2021
)
0.62
"Intermittent preventive treatment in pregnancy (IPTp) with sulfadoxine-pyrimethamine (SP) is recommended by the World Health Organization for the prevention of malaria in pregnancy (MIP)-associated adverse outcomes in high burden areas."( Safety and efficacy of intermittent presumptive treatment with sulfadoxine-pyrimethamine using rapid diagnostic test screening and treatment with dihydroartemisinin-piperaquine at the first antenatal care visit (IPTp-SP+): study protocol for a randomized
Champo, D; Chongwe, G; Ippolito, MM; Kabuya, JB; Manyando, C; Mulenga, M; Mwakazanga, D; Sikalima, J; Tende, C; Young, AMP, 2021
)
0.62
" Secondary endpoints include incident MIP at other time points, placental malaria, congenital malaria, hemoglobin trends, birth outcomes, and incidence of adverse events in infants up to the first birthday."( Safety and efficacy of intermittent presumptive treatment with sulfadoxine-pyrimethamine using rapid diagnostic test screening and treatment with dihydroartemisinin-piperaquine at the first antenatal care visit (IPTp-SP+): study protocol for a randomized
Champo, D; Chongwe, G; Ippolito, MM; Kabuya, JB; Manyando, C; Mulenga, M; Mwakazanga, D; Sikalima, J; Tende, C; Young, AMP, 2021
)
0.62
" Intermittent preventive treatment in pregnancy (IPTp) with sulphadoxine-pyrimethamine is recommended for malaria prevention in HIV-uninfected women, but it is contraindicated in those HIV-infected on cotrimoxazole prophylaxis (CTXp) due to potential adverse effects."( Evaluation of the safety and efficacy of dihydroartemisinin-piperaquine for intermittent preventive treatment of malaria in HIV-infected pregnant women: protocol of a multicentre, two-arm, randomised, placebo-controlled, superiority clinical trial (MAMAH
Dimessa, LB; El Gaaloul, M; Esen, M; Garcia-Otero, L; González, R; Lagler, H; Lell, B; Menendez, C; Mischlinger, J; Mombo-Ngoma, G; Nhampossa, T; Piqueras, M; Pons-Duran, C; Ramharter, M; Sanz, S; Saute, F; Sevene, E; Tchouatieu, AM; Zoleko Manego, R, 2021
)
0.62
" Secondary outcomes include prevalence of malaria-related maternal and infant outcomes and proportion of adverse perinatal outcomes."( Evaluation of the safety and efficacy of dihydroartemisinin-piperaquine for intermittent preventive treatment of malaria in HIV-infected pregnant women: protocol of a multicentre, two-arm, randomised, placebo-controlled, superiority clinical trial (MAMAH
Dimessa, LB; El Gaaloul, M; Esen, M; Garcia-Otero, L; González, R; Lagler, H; Lell, B; Menendez, C; Mischlinger, J; Mombo-Ngoma, G; Nhampossa, T; Piqueras, M; Pons-Duran, C; Ramharter, M; Sanz, S; Saute, F; Sevene, E; Tchouatieu, AM; Zoleko Manego, R, 2021
)
0.62
" There were no reported serious adverse events associated with any of the regimens."( Efficacy and safety of artemether-lumefantrine and dihydroartemisinin-piperaquine for the treatment of uncomplicated Plasmodium falciparum malaria and prevalence of molecular markers associated with artemisinin and partner drug resistance in Uganda.
Asua, V; Belay, K; Bosco, A; Bwanika, JB; Ebong, C; Gonahasa, S; Gudoi, S; Halsey, ES; Kamya, MR; Kapisi, J; Kigozi, R; Kyabayinze, D; Lucchi, NW; Moriarty, LF; Mpimbaza, A; Namuganga, JF; Niang, M; Nsobya, SL; Opigo, J; Rubahika, D; Rutazana, D; Sebikaari, G; Souza, SSS; Sserwanga, A; Tibenderana, J; Yeka, A, 2021
)
0.62
"DP remains highly effective and safe for the treatment of uncomplicated malaria in Uganda."( Efficacy and safety of artemether-lumefantrine and dihydroartemisinin-piperaquine for the treatment of uncomplicated Plasmodium falciparum malaria and prevalence of molecular markers associated with artemisinin and partner drug resistance in Uganda.
Asua, V; Belay, K; Bosco, A; Bwanika, JB; Ebong, C; Gonahasa, S; Gudoi, S; Halsey, ES; Kamya, MR; Kapisi, J; Kigozi, R; Kyabayinze, D; Lucchi, NW; Moriarty, LF; Mpimbaza, A; Namuganga, JF; Niang, M; Nsobya, SL; Opigo, J; Rubahika, D; Rutazana, D; Sebikaari, G; Souza, SSS; Sserwanga, A; Tibenderana, J; Yeka, A, 2021
)
0.62
" No delay in parasite clearance nor severe adverse reaction was observed."( Efficacy and safety of dihydroartemisinin-piperaquine for the treatment of uncomplicated Plasmodium falciparum and Plasmodium vivax malaria in Papua and Sumatra, Indonesia.
Anggraeni, ND; Asih, PBS; Basri, HH; Bustos, MDG; Dewayanti, FK; Hutahaean, J; Kusumaningsih, M; Mulyani, PS; Robaha, M; Rozi, IE; Sariwati, E; Syafruddin, D; Wangsamuda, S; Zulfah, S, 2022
)
0.72
" Adverse events over the first 28 days were reported in 27 (54%) of 50 patients treated with dihydroartemisinin-piperaquine alone, 29 (58%) of 50 patients treated with tafenoquine plus dihydroartemisinin-piperaquine, and 22 (44%) of 50 patients treated with primaquine plus dihydroartemisinin-piperaquine."( Tafenoquine co-administered with dihydroartemisinin-piperaquine for the radical cure of Plasmodium vivax malaria (INSPECTOR): a randomised, placebo-controlled, efficacy and safety study.
Baird, JK; Berni, A; Budiman, W; Cedar, E; Chand, K; Crenna-Darusallam, C; Duparc, S; Ekawati, LL; Elyazar, I; Fernando, D; Fletcher, K; Goyal, N; Green, JA; Instiaty, I; Jones, S; Kleim, JP; Lardo, S; Martin, A; Noviyanti, R; Prasetya, CB; Rolfe, K; Santy, YW; Satyagraha, AW; Sharma, H; Soebandrio, A; Subekti, D; Sutanto, I; Tan, LK; Taylor, M, 2023
)
0.91
" Dihydroartemisinin-piperaquine and artesunate-amodiaquine were associated with a small number of mild adverse events, and there were no treatment-related serious adverse events or deaths."( Effectiveness and safety of intermittent preventive treatment with dihydroartemisinin-piperaquine or artesunate-amodiaquine for reducing malaria and related morbidities in schoolchildren in Tanzania: a randomised controlled trial.
Baraka, V; Francis, F; Geertruyden, JV; Gesase, S; Kyaruzi, E; Lusingu, JPA; Madebe, R; Makenga, G; Minja, DTR; Mtove, G; Nakato, S, 2023
)
0.91
"IPTsc with dihydroartemisinin-piperaquine or artesunate-amodiaquine is a safe and effective approach to reducing malaria parasitaemia, clinical malaria, and related morbidities, and is feasible to implement through programmes delivered by schoolteachers."( Effectiveness and safety of intermittent preventive treatment with dihydroartemisinin-piperaquine or artesunate-amodiaquine for reducing malaria and related morbidities in schoolchildren in Tanzania: a randomised controlled trial.
Baraka, V; Francis, F; Geertruyden, JV; Gesase, S; Kyaruzi, E; Lusingu, JPA; Madebe, R; Makenga, G; Minja, DTR; Mtove, G; Nakato, S, 2023
)
0.91
" Artemisinin-based combination treatments are generally well tolerated, safe and effective; the most used being artemether-lumefantrine (AL) and dihydroartemisinin-piperaquine (DP)."( Efficacy and safety of pyronaridine-artesunate (PYRAMAX) for the treatment of
D'Alessandro, U; Dabira, ED; Diakite, H; Djimde, M; Dorlo, TP; Erhart, A; González, R; Kabore, B; Kayentao, K; Keita, M; Macuacua, S; Menendez, C; Mens, P; Muhindo, HM; Piqueras, M; Sagara, I; Schallig, H; Sevene, E; Tinto, H; Traore, M; Tshiongo, JK; Vala, A, 2023
)
0.91
" RCTs comparing IPTp DP versus recommended standard treatment for IPTp with these outcome measures were analyzed; change in QTc interval, serious adverse events (SAE), grade 3 or 4 adverse events possibly related to study drug and vomiting within 30 min after study drug administration."( Safety and tolerability of repeated doses of dihydroartemisinin-piperaquine for intermittent preventive treatment of malaria in pregnancy: a systematic review and an aggregated data meta-analysis of randomized controlled trials.
Abebe, A; Ahmedin, M; Atim, MG; Embaye, SM; Kahabuka, M; Kazembe, D; Manyazewal, T; Mesfin, T; Muthoka, EN; Namuganza, S; Usmael, K, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
"The relatively short half-life of ARM may be one of the factors responsible for the poor radical cure rate of falciparum malaria with regimens employing daily dosing."( Single dose pharmacokinetics of oral artemether in healthy Malaysian volunteers.
Mansor, SM; Mordi, MN; Navaratnam, V; Wernsdorfer, WH, 1997
)
0.3
" Pharmacokinetic parameters were calculated by non-compartmental methods."( A pharmacokinetic and pharmacodynamic study of intravenous vs oral artesunate in uncomplicated falciparum malaria.
Batty, KT; Binh, TQ; Davis, TM; Hung, NC; Ilett, KF; Kim, NV; Mai, TX; Powell, SM; Thien, HV; Thu, LT; Tien, NP, 1998
)
0.3
" bolus, ARTS had a peak concentration of 29."( A pharmacokinetic and pharmacodynamic study of intravenous vs oral artesunate in uncomplicated falciparum malaria.
Batty, KT; Binh, TQ; Davis, TM; Hung, NC; Ilett, KF; Kim, NV; Mai, TX; Powell, SM; Thien, HV; Thu, LT; Tien, NP, 1998
)
0.3
" The resulting pharmacokinetic parameter estimates were substantially different not only between drugs but also between routes of administration for the same drug."( The pharmacokinetics and bioavailability of dihydroartemisinin, arteether, artemether, artesunic acid and artelinic acid in rats.
Brewer, TG; Fleckenstein, LL; Heiffer, MH; Li, QG; Masonic, K; Peggins, JO, 1998
)
0.3
" Patients with ARF had significantly higher Cmax [2."( Pharmacokinetics of intramuscular artemether in patients with severe falciparum malaria with or without acute renal failure.
Harinasuta, T; Karbwang, J; Na-Bangchang, K; Rimchala, W; Sukontason, K; Tin, T, 1998
)
0.3
"A single cross-over, comparative pharmacokinetic study of oral and rectal formulations of 200 mg artesunic acid in 12 healthy Malaysian volunteers is reported."( Comparative pharmacokinetic study of oral and rectal formulations of artesunic acid in healthy volunteers.
Abdullah, MN; Akbar, A; Mansor, SM; Mordi, MN; Navaratnam, V, 1998
)
0.3
"Comparison of pharmacokinetic parameters of artesunic acid after oral and rectal administration showed statistically significant differences in t(max) and AUC, with no changes for Cmax and t1/2."( Comparative pharmacokinetic study of oral and rectal formulations of artesunic acid in healthy volunteers.
Abdullah, MN; Akbar, A; Mansor, SM; Mordi, MN; Navaratnam, V, 1998
)
0.3
"There appear to be pharmacokinetic differences between oral and rectal modes of administration."( Comparative pharmacokinetic study of oral and rectal formulations of artesunic acid in healthy volunteers.
Abdullah, MN; Akbar, A; Mansor, SM; Mordi, MN; Navaratnam, V, 1998
)
0.3
"Pharmacokinetic and pharmacodynamic interactions between dihydroartemisinin and mefloquine were investigated in 10 healthy Thai males."( Pharmacokinetic and pharmacodynamic interactions of mefloquine and dihydroartemisinin.
Karbwang, J; Na-Bangchang, K; Thanavibul, A; Tippawangkosol, P; Ubalee, R, 1999
)
0.3
" The pharmacokinetic parameters of mefloquine were estimated using non-compartmental and compartmental analysis."( Pharmacokinetics and bioequivalence evaluation of three commercial tablet formulations of mefloquine when given in combination with dihydroartemisinin in patients with acute uncomplicated falciparum malaria.
Karbwang, J; Na-Bangchang, K; Palacios, PA; Saengtertsilapachai, S; Ubalee, R; Wernsdorfer, WH, 2000
)
0.31
" Mefloquine from the three formulations showed significantly different pharmacokinetic and bioavailability metrics."( Pharmacokinetics and bioequivalence evaluation of three commercial tablet formulations of mefloquine when given in combination with dihydroartemisinin in patients with acute uncomplicated falciparum malaria.
Karbwang, J; Na-Bangchang, K; Palacios, PA; Saengtertsilapachai, S; Ubalee, R; Wernsdorfer, WH, 2000
)
0.31
" The pharmacokinetic curves of artemether and its metabolites dihydroartemisinin and furano acetate of artemether were determined and the results showed that the half-life of artemether under the conditions simulated the pH of plasma or small intestine was more than 150 min and that of stomach acid was 74."( [Pharmacokinetic studies on artemether under conditions simulated in vivo].
Chen, YG; Yu, BY, 2002
)
0.31
"4 (range 5-108) months were recruited into the study and data from 90 of these children (30 with respiratory distress and 60 with no respiratory distress) were used in the population pharmacokinetic analysis."( Population pharmacokinetics of artemether and dihydroartemisinin following single intramuscular dosing of artemether in African children with severe falciparum malaria.
Aarons, L; Edwards, G; Kokwaro, GO; Majid, O; Marsh, K; Mithwani, S; Mohamed, S; Muchohi, S; Watkins, W, 2004
)
0.32
" Cmax values of 63."( Pharmacokinetic investigation on the therapeutic potential of artemotil (beta-arteether) in Thai patients with severe Plasmodium falciparum malaria.
Chalearmrult, K; Krudsood, S; Li, Q; Looareesuwan, S; Lugt, CB; Milhous, WK; Vannaphan, S; Wilairatana, P, 2004
)
0.32
" Significant changes in the pharmacokinetic parameters of both mefloquine and dihydroartemisinin were observed in patients with malaria compared with healthy subjects reported in a paralleled study."( Pharmacokinetics of the four combination regimens of dihydroartemisinin/mefloquine in acute uncomplicated falciparum malaria.
Karbwang, J; Na-Bangchang, K; Thanavibul, A; Tippawangkosol, P, 2005
)
0.33
" The beta-isomer of arteether was characterized by a longer elimination half-life and a relatively larger volume of distribution than the alpha-isomer, suggesting that beta-arteether may be responsible for the prolonged in vivo schizontocidal activity."( Pharmacokinetics of the diastereomers of arteether, a potent antimalarial drug, in rats.
Gupta, RC; Madhusudanan, KP; Sabarinath, S, 2005
)
0.33
"To determine the pharmacokinetic properties of dihydroartemisinin (DHA) following oral artesunate treatment in women with recrudescent multi-drug resistant falciparum malaria, in the second and third trimesters of pregnancy."( Pharmacokinetics of dihydroartemisinin following oral artesunate treatment of pregnant women with acute uncomplicated falciparum malaria.
Cho, T; Gilveray, G; Looareesuwan, S; McGready, R; Nosten, F; Stepniewska, K; Ward, SA; White, NJ, 2006
)
0.33
" Conventional non-compartmental modelling and a population one-compartment pharmacokinetic model were applied to the data."( Pharmacokinetics of dihydroartemisinin following oral artesunate treatment of pregnant women with acute uncomplicated falciparum malaria.
Cho, T; Gilveray, G; Looareesuwan, S; McGready, R; Nosten, F; Stepniewska, K; Ward, SA; White, NJ, 2006
)
0.33
"To investigate the pharmacokinetic properties of piperaquine after repeated oral administration of the antimalarial combination CV8 in healthy subjects."( Pharmacokinetics of piperaquine after repeated oral administration of the antimalarial combination CV8 in 12 healthy male subjects.
Ashton, M; Friberg Hietala, S; Hai, TN; Röshammar, D; Van Huong, N, 2006
)
0.33
" Population pharmacokinetic parameter estimates were obtained by nonlinear mixed effects modeling of the observed data using NONMEM."( Pharmacokinetics of piperaquine after repeated oral administration of the antimalarial combination CV8 in 12 healthy male subjects.
Ashton, M; Friberg Hietala, S; Hai, TN; Röshammar, D; Van Huong, N, 2006
)
0.33
" Piperaquine pharmacokinetics were characterized by a large volume of distribution and a terminal half-life of several days."( Pharmacokinetics of piperaquine after repeated oral administration of the antimalarial combination CV8 in 12 healthy male subjects.
Ashton, M; Friberg Hietala, S; Hai, TN; Röshammar, D; Van Huong, N, 2006
)
0.33
"To determine the pharmacokinetic properties of artemether and lumefantrine (AL) in pregnant women with recrudescent uncomplicated multi-drug resistant falciparum malaria."( The pharmacokinetics of artemether and lumefantrine in pregnant women with uncomplicated falciparum malaria.
Ashley, EA; La, Y; Lindegardh, N; McGready, R; Nosten, F; Singhasivanon, P; Stepniewska, K; White, NJ, 2006
)
0.33
" Serial blood samples were taken over a 7-day period, and pharmacokinetic parameters were estimated."( The pharmacokinetics of artemether and lumefantrine in pregnant women with uncomplicated falciparum malaria.
Ashley, EA; La, Y; Lindegardh, N; McGready, R; Nosten, F; Singhasivanon, P; Stepniewska, K; White, NJ, 2006
)
0.33
" The pharmacokinetic properties of DHA were determined using nonlinear mixed-effects modelling."( Population pharmacokinetics of artesunate and dihydroartemisinin following intra-rectal dosing of artesunate in malaria patients.
Agbenyega, T; Barnes, KI; Di Perri, G; Folb, P; Gomes, M; Krishna, S; Krudsood, S; Looareesuwan, S; Mansor, S; McIlleron, H; Miller, R; Molyneux, M; Mwenechanya, J; Navaratnam, V; Nosten, F; Olliaro, P; Pang, L; Ribeiro, I; Simpson, JA; Tembo, M; van Vugt, M; Ward, S; Weerasuriya, K; White, NJ; Win, K, 2006
)
0.33
"The pharmacokinetic properties of DHA were affected only by gender and body weight."( Population pharmacokinetics of artesunate and dihydroartemisinin following intra-rectal dosing of artesunate in malaria patients.
Agbenyega, T; Barnes, KI; Di Perri, G; Folb, P; Gomes, M; Krishna, S; Krudsood, S; Looareesuwan, S; Mansor, S; McIlleron, H; Miller, R; Molyneux, M; Mwenechanya, J; Navaratnam, V; Nosten, F; Olliaro, P; Pang, L; Ribeiro, I; Simpson, JA; Tembo, M; van Vugt, M; Ward, S; Weerasuriya, K; White, NJ; Win, K, 2006
)
0.33
" It was concluded that since no pharmacokinetic drug interaction was observed, MQ dose given 24 hours after an initial dose of DHA is a preferable combination treatment regimen with regard to patient compliance."( Pharmacokinetics of mefloquine with dihydroartemisinin as 2-day regimens in patients with uncomplicated falciparum malaria.
Hung, le N; Hung, NC; Na-Bangchang, K; Thuy, le TD, 2007
)
0.34
"Antimalarial treatment strategies based on in vitro studies are limited by the paucity of pharmacodynamic information for dosage regimen design."( Development of a pharmacodynamic model of murine malaria and antimalarial treatment with dihydroartemisinin.
Barrett, PH; Batty, KT; Davis, TM; Gibbons, PL; Ilett, KF, 2007
)
0.34
" However, there is a paucity of detailed preclinical and pharmacokinetic data to link PQ serum concentrations and toxicity or efficacy."( Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
Andrzejewski, C; Batty, KT; Ilett, KF; Jago, JD; Moore, BR; Page-Sharp, M, 2008
)
0.35
" The mean pharmacokinetic parameters of DHA in a single dose were: t(1/2(beta))=1."( Pharmacokinetics of dihydroartemisinin in Artekin tablets for single and repeated dosing in Chinese healthy volunteers.
Hong, X; Huang, TL; Huang, XT; Liu, CH; Mi, SQ; Ou, WP; Wang, NS; Ye, SM, 2008
)
0.35
"The aim was to study the pharmacokinetic profile of artesunate and its metabolite dihydroartemisinin (DHA) in a pig model."( Pharmacokinetics of artesunate in the domestic pig.
Aglioni, C; Bressolle, FM; Mosnier, J; Parzy, D; Sinou, V; Taudon, N, 2008
)
0.35
"The pharmacokinetic properties of artesunate and DHA in pigs were similar to those reported in humans, suggesting that the swine model is suitable for determining the preclinical pharmacokinetics of artemisinin derivatives."( Pharmacokinetics of artesunate in the domestic pig.
Aglioni, C; Bressolle, FM; Mosnier, J; Parzy, D; Sinou, V; Taudon, N, 2008
)
0.35
" Reduced half-life (T(1/2z)) and lower area under concentration curve (AUC(infinity)) values were observed on the final day of treatment in comparison to those obtained on the first day."( Pharmacokinetics of a five-day oral dihydroartemisinin monotherapy regimen in patients with uncomplicated falciparum malaria.
Le Thi, DT; Le, NH; Na-Bangchang, K; Nguyen, CH; Phan Thi, D, 2008
)
0.35
" The aim of this study was to determine the influence of a standard Vietnamese meal on the single-dose pharmacokinetics of piperaquine when administered in combination with dihydroartemisinin, and to gain extended data on the terminal half-life of piperaquine in healthy Vietnamese volunteers."( The influence of food on the pharmacokinetics of piperaquine in healthy Vietnamese volunteers.
Ashton, M; Hai, TN; Hietala, SF; Van Huong, N, 2008
)
0.35
"The pharmacokinetic (PK) parameters of artesunate, recently discovered to possess promising trematocidal activity, and its main metabolite dihydroartemisinin (DHA) were determined in rats infected with hepatic and biliary stages of Fasciola hepatica and compared with uninfected rats after single intragastric and intravenous (iv) doses."( Pharmacokinetic parameters of artesunate and dihydroartemisinin in rats infected with Fasciola hepatica.
Decosterd, L; Gruyer, MS; Keiser, J; Mercier, T; Perrottet, N; Zanolari, B, 2009
)
0.35
" Blood samples for pharmacokinetic analysis were collected up to 24 h post-first dose."( Pharmacokinetics of chlorproguanil, dapsone, artesunate and their major metabolites in patients during treatment of acute uncomplicated Plasmodium falciparum malaria.
Bandyopadhyay, N; Duparc, S; Kirby, PL; Miller, AK; Ward, SA; Winstanley, PA; Wootton, DG, 2009
)
0.35
"The pharmacokinetic analysis included 115 patients."( Pharmacokinetics of chlorproguanil, dapsone, artesunate and their major metabolites in patients during treatment of acute uncomplicated Plasmodium falciparum malaria.
Bandyopadhyay, N; Duparc, S; Kirby, PL; Miller, AK; Ward, SA; Winstanley, PA; Wootton, DG, 2009
)
0.35
" Nonlinear mixed-effect modelling was used to obtain the pharmacokinetic and variability (inter-individual and residual variability) parameter estimates."( Population pharmacokinetics of artesunate and dihydroartemisinin following single- and multiple-dosing of oral artesunate in healthy subjects.
Craft, JC; Fleckenstein, L; Jang, IJ; Kirsch, LE; Naik, H; Shin, CS; Tan, B; Yu, KS, 2009
)
0.35
"A novel parent-metabolite pharmacokinetic model consisting of a dosing compartment, a central compartment for AS, a central compartment and a peripheral compartment for DHA was developed."( Population pharmacokinetics of artesunate and dihydroartemisinin following single- and multiple-dosing of oral artesunate in healthy subjects.
Craft, JC; Fleckenstein, L; Jang, IJ; Kirsch, LE; Naik, H; Shin, CS; Tan, B; Yu, KS, 2009
)
0.35
"A novel simultaneous parent-metabolite pharmacokinetic model with good predictive power was developed to study the population pharmacokinetics of AS and DHA in healthy subjects following single- and multiple-dosing of AS with or without the presence of food."( Population pharmacokinetics of artesunate and dihydroartemisinin following single- and multiple-dosing of oral artesunate in healthy subjects.
Craft, JC; Fleckenstein, L; Jang, IJ; Kirsch, LE; Naik, H; Shin, CS; Tan, B; Yu, KS, 2009
)
0.35
" The main disposition parameters to AS+AQ were: for DHA, AUC = 632 +/- 475 ng h/ml and Cmax = 432 +/- 325 ng/ml, and for MdAQ = 14268 +/- 4114 ng h/ml and Cmax = 336 +/- 225 ng/ml (mean +/- standard deviation)."( Pharmacokinetics and pharmacodynamics of a new ACT formulation: Artesunate/Amodiaquine (TRIMALACT) following oral administration in African malaria patients.
Alegre, SS; Benakis, A; Bertaux, L; Lwango, R; Malaika, LT; Parzy, D; Sinou, V; Sugnaux, F; Taudon, N,
)
0.13
"The overall pharmacokinetic properties of artemether and dihydroartemisinin in healthy Pakistani subjects are comparable to healthy subjects and patients from other populations."( Pharmacokinetics of artemether and dihydroartemisinin in healthy Pakistani male volunteers treated with artemether-lumefantrine.
Ali, S; Lindegardh, N; Najmi, MH; Tarning, J, 2010
)
0.36
" Pharmacokinetic and safety data supporting the use of artemisinin derivatives in pregnancy are urgently needed."( Pharmacokinetics and pharmacodynamics of artesunate and dihydroartemisinin following oral treatment in pregnant women with asymptomatic Plasmodium falciparum infections in Kinshasa DRC.
Atibu, J; Bose, C; Capparelli, EV; Douoguih, M; Fleckenstein, L; Hemingway-Foday, J; Koch, MA; Lokomba, V; Meshnick, SR; Onyamboko, MA; Ryder, RW; Tshefu, AK; Wesche, D; Wright, LL, 2011
)
0.37
" Non-compartmental pharmacokinetic analysis was performed using standard methods."( Pharmacokinetics and pharmacodynamics of artesunate and dihydroartemisinin following oral treatment in pregnant women with asymptomatic Plasmodium falciparum infections in Kinshasa DRC.
Atibu, J; Bose, C; Capparelli, EV; Douoguih, M; Fleckenstein, L; Hemingway-Foday, J; Koch, MA; Lokomba, V; Meshnick, SR; Onyamboko, MA; Ryder, RW; Tshefu, AK; Wesche, D; Wright, LL, 2011
)
0.37
" Estimates for pharmacokinetic and variability parameters were obtained through nonlinear mixed effects modelling."( Population pharmacokinetics of artesunate and dihydroartemisinin in pregnant and non-pregnant women with malaria.
Atibu, J; Bose, C; Capparelli, E; Douoguih, M; Fleckenstein, L; Hemingway-Foday, J; Koch, MA; Lokomba, V; Meshnick, S; Morris, CA; Onyamboko, MA; Ryder, RW; Tshefu, AK; Wesche, D; Wright, L, 2011
)
0.37
"In this analysis, pharmacokinetic modelling suggests that pregnant women have accelerated DHA clearance compared to non-pregnant women receiving orally administered AS."( Population pharmacokinetics of artesunate and dihydroartemisinin in pregnant and non-pregnant women with malaria.
Atibu, J; Bose, C; Capparelli, E; Douoguih, M; Fleckenstein, L; Hemingway-Foday, J; Koch, MA; Lokomba, V; Meshnick, S; Morris, CA; Onyamboko, MA; Ryder, RW; Tshefu, AK; Wesche, D; Wright, L, 2011
)
0.37
" Pharmacokinetic data for CQ in animal models are limited; thus, we conducted a three-part investigation, comprising (i) pharmacodynamic studies of CQ and CQ plus dihydroartemisinin (DHA) in Plasmodium berghei-infected mice, (ii) pharmacokinetic studies of CQ in healthy and malaria-infected mice, and (iii) interspecies allometric scaling for CQ from 6 animal and 12 human studies."( Pharmacokinetics, pharmacodynamics, and allometric scaling of chloroquine in a murine malaria model.
Batty, KT; Ilett, KF; Jago, JD; Moore, BR; Page-Sharp, M; Stoney, JR, 2011
)
0.37
" Intravenous AS is associated with high initial AS concentrations which subsequently decline rapidly, with typical AS half-life estimates of less than 15 minutes."( Review of the clinical pharmacokinetics of artesunate and its active metabolite dihydroartemisinin following intravenous, intramuscular, oral or rectal administration.
Borghini-Fuhrer, I; Duparc, S; Fleckenstein, L; Jung, D; Morris, CA; Shin, CS, 2011
)
0.37
"0057), and the terminal elimination half-life was significantly shorter (17."( Pharmacokinetics of dihydroartemisinin and piperaquine in pregnant and nonpregnant women with uncomplicated falciparum malaria.
Laochan, N; Lindegardh, N; McGready, R; Mu, O; Nosten, F; Phyo, AP; Rijken, MJ; Singhasivanon, P; Tarning, J; Than, HH; White, N; Win, AK, 2011
)
0.37
" The pharmacokinetic properties of antimalarial drugs are often affected by pregnancy, resulting in lower drug concentrations and a consequently higher risk of treatment failure."( Population pharmacokinetics of dihydroartemisinin and piperaquine in pregnant and nonpregnant women with uncomplicated malaria.
Day, NP; Hanpithakpong, W; Lindegardh, N; McGready, R; Nosten, F; Phyo, AP; Rijken, MJ; Tarning, J; White, NJ, 2012
)
0.38
" The aim of this study was to describe the pharmacokinetic and pharmacodynamic properties of piperaquine in 236 children with uncomplicated falciparum malaria in Burkina Faso."( Population pharmacokinetics and pharmacodynamics of piperaquine in children with uncomplicated falciparum malaria.
Day, NP; Hanpithakpong, W; Jongrak, N; Lindegardh, N; Nosten, F; Ouedraogo, JB; Parikh, S; Rosenthal, PJ; Rouamba, N; Somé, FA; Tarning, J; White, NJ; Zongo, I, 2012
)
0.38
" No significant dose-effect or concentration-effect relationships between pharmacokinetic (PK) and parasite clearance parameters were observed, though baseline parasitemia was modestly correlated with increased parasite clearance times."( Pharmacokinetics and pharmacodynamics of oral artesunate monotherapy in patients with uncomplicated Plasmodium falciparum malaria in western Cambodia.
Bethell, D; Chanthap, L; Fukuda, M; Khemawoot, P; Lin, J; Noedl, H; Ringwald, P; Rutvisuttinunt, W; Saunders, D; Se, Y; Siripokasupkul, R; Smith, B; Socheat, D; Sriwichai, S; Teja-Isavadharm, P; Timmermans, A; Tyner, S; Vanachayangkul, P, 2012
)
0.38
" Pregnancy has been reported to alter the pharmacokinetic properties of many anti-malarial drugs."( Population pharmacokinetics of Artemether and dihydroartemisinin in pregnant women with uncomplicated Plasmodium falciparum malaria in Uganda.
Day, NP; Dhorda, M; Guerin, PJ; Kloprogge, F; Lindegardh, N; Muwanga, S; Nosten, F; Nuengchamnong, N; Piola, P; Tarning, J; Turyakira, E; White, NJ, 2012
)
0.38
" A simultaneous drug-metabolite population pharmacokinetic model for artemether and dihydroartemisinin was developed taking into account different disposition, absorption, error and covariate models."( Population pharmacokinetics of Artemether and dihydroartemisinin in pregnant women with uncomplicated Plasmodium falciparum malaria in Uganda.
Day, NP; Dhorda, M; Guerin, PJ; Kloprogge, F; Lindegardh, N; Muwanga, S; Nosten, F; Nuengchamnong, N; Piola, P; Tarning, J; Turyakira, E; White, NJ, 2012
)
0.38
"002) with EFV, but the LR half-life was unchanged."( Concomitant efavirenz reduces pharmacokinetic exposure to the antimalarial drug artemether-lumefantrine in healthy volunteers.
Aweeka, FT; Dorsey, G; Havlir, D; Huang, L; Lizak, P; Marzan, F; Parikh, S; Rosenthal, PJ, 2012
)
0.38
" The sex-specific effect on the pharmacokinetic profiles of DHA and its metabolites was studied."( An investigation of the auto-induction of and gender-related variability in the pharmacokinetics of dihydroartemisinin in the rat.
Du, F; Li, X; Xing, J; Zhu, F, 2012
)
0.38
" The pharmacokinetic properties of many anti-malarials are also altered during pregnancy, often resulting in a decreased drug exposure."( A population pharmacokinetic model of piperaquine in pregnant and non-pregnant women with uncomplicated Plasmodium falciparum malaria in Sudan.
Adam, I; Ashton, M; Day, NP; Hanpithakpong, W; Hoglund, RM; Lindegardh, N; Nosten, F; Tarning, J; White, NJ, 2012
)
0.38
" A statistically significant decrease in estimated terminal piperaquine half-life in pregnant compared with non-pregnant women was found, but there were no differences in post-hoc estimates of total piperaquine exposure."( A population pharmacokinetic model of piperaquine in pregnant and non-pregnant women with uncomplicated Plasmodium falciparum malaria in Sudan.
Adam, I; Ashton, M; Day, NP; Hanpithakpong, W; Hoglund, RM; Lindegardh, N; Nosten, F; Tarning, J; White, NJ, 2012
)
0.38
"The population pharmacokinetic properties of piperaquine were well described by a three-compartment disposition model in pregnant and non-pregnant women with uncomplicated malaria."( A population pharmacokinetic model of piperaquine in pregnant and non-pregnant women with uncomplicated Plasmodium falciparum malaria in Sudan.
Adam, I; Ashton, M; Day, NP; Hanpithakpong, W; Hoglund, RM; Lindegardh, N; Nosten, F; Tarning, J; White, NJ, 2012
)
0.38
" A population pharmacokinetic study of ARS and dihydroartemisinin (DHA) was conducted from sparse sampling in 70 Tanzanian children of ages 6 months to 11 years."( Population pharmacokinetics of intramuscular artesunate in African children with severe malaria: implications for a practical dosing regimen.
Day, NP; Dondorp, AM; Gesase, S; Hendriksen, IC; Kent, A; Lemnge, MM; Lindegardh, N; Mtove, G; Reyburn, H; Tarning, J; von Seidlein, L; White, NJ, 2013
)
0.39
"Pregnancy alters the pharmacokinetic properties of many drugs used in the treatment of malaria, usually resulting in lower drug exposures."( Pharmacokinetic properties of artemether, dihydroartemisinin, lumefantrine, and quinine in pregnant women with uncomplicated plasmodium falciparum malaria in Uganda.
Dhorda, M; Guerin, PJ; Jullien, V; Kloprogge, F; Nosten, F; Piola, P; Tarning, J; White, NJ, 2013
)
0.39
"Simultaneous modelling of dense and sparse pharmacokinetic data is possible with a population approach."( Statistical power calculations for mixed pharmacokinetic study designs using a population approach.
Day, NP; Kloprogge, F; Simpson, JA; Tarning, J; White, NJ, 2014
)
0.4
" The objective of this study is to show the pharmacokinetic (PK) profile of intravenous artesunate (AS), which was manufactured under good manufacturing practice (GMP) conditions, in adults with uncomplicated falciparum malaria in Kenya."( Pharmacokinetic evaluation of intravenous artesunate in adults with uncomplicated falciparum malaria in Kenya: a phase II study.
Hickman, MR; Li, Q; Melendez, V; Miller, SR; Ogutu, B; Otieno, W; Polhemus, M; Remich, S; Smith, B; Teja-Isavadharm, P; Weina, PJ, 2014
)
0.4
" Pharmacokinetic data were analysed with a compartmental analysis for AS and DHA."( Pharmacokinetic evaluation of intravenous artesunate in adults with uncomplicated falciparum malaria in Kenya: a phase II study.
Hickman, MR; Li, Q; Melendez, V; Miller, SR; Ogutu, B; Otieno, W; Polhemus, M; Remich, S; Smith, B; Teja-Isavadharm, P; Weina, PJ, 2014
)
0.4
" The high mean peak concentration (Cmax) of AS was shown to be 28,558 ng/mL while the Cmax of DHA was determined to be 2,932 ng/mL."( Pharmacokinetic evaluation of intravenous artesunate in adults with uncomplicated falciparum malaria in Kenya: a phase II study.
Hickman, MR; Li, Q; Melendez, V; Miller, SR; Ogutu, B; Otieno, W; Polhemus, M; Remich, S; Smith, B; Teja-Isavadharm, P; Weina, PJ, 2014
)
0.4
" Given the much longer half-life of DHA compared to the short half-life of AS, DHA also plays a significant role in treatment of severe malaria."( Pharmacokinetic evaluation of intravenous artesunate in adults with uncomplicated falciparum malaria in Kenya: a phase II study.
Hickman, MR; Li, Q; Melendez, V; Miller, SR; Ogutu, B; Otieno, W; Polhemus, M; Remich, S; Smith, B; Teja-Isavadharm, P; Weina, PJ, 2014
)
0.4
" Compartmental pharmacokinetic models for PQ and DHA were developed using a population-based approach."( Effect of coadministered fat on the tolerability, safety, and pharmacokinetic properties of dihydroartemisinin-piperaquine in Papua New Guinean children with uncomplicated malaria.
Batty, KT; Benjamin, JM; Davis, TM; Ginny, E; Griffin, S; Moore, BR; Mueller, I; Page-Sharp, M; Robinson, LJ; Salman, S; Siba, P, 2014
)
0.4
" A combined drug-metabolite population pharmacokinetic model was developed to describe the plasma pharmacokinetics of ARS and DHA in plasma."( Population pharmacokinetics of artesunate and dihydroartemisinin during long-term oral administration of artesunate to patients with metastatic breast cancer.
Äbelö, A; Ashton, M; Blank, A; Ericsson, T; von Hagens, C, 2014
)
0.4
" Pharmacokinetic assessment was done with a noncompartmental approach."( Open-label crossover study of primaquine and dihydroartemisinin-piperaquine pharmacokinetics in healthy adult thai subjects.
Ashley, EA; Chotsiri, P; Day, NP; Hanboonkunupakarn, B; Hanpithakpong, W; Jittamala, P; Lee, SJ; Panapipat, S; Pukrittayakamee, S; Tarning, J; Wattanakul, T; White, NJ, 2014
)
0.4
" A single-dose, randomized, three-sequence crossover study was conducted in healthy Thai volunteers to characterize potential pharmacokinetic interactions between these drugs."( Pharmacokinetic interactions between primaquine and pyronaridine-artesunate in healthy adult Thai subjects.
Ashley, EA; Blessborn, D; Chairat, K; Day, NP; Hanboonkunupakarn, B; Jittamala, P; Lee, SJ; Nosten, F; Panapipat, S; Pukrittayakamee, S; Tarning, J; Thana, P; White, NJ, 2015
)
0.42
" The polymorphic effects of UGT1A9 (I399C>T) and UGT2B7*2 (802C>T), the major enzymes involved in the metabolism of DHA, on the pharmacokinetic profiles of DHA and its metabolite was also studied."( The effect of UGTs polymorphism on the auto-induction phase II metabolism-mediated pharmacokinetics of dihydroartemisinin in healthy Chinese subjects after oral administration of a fixed combination of dihydroartemisinin-piperaquine.
Li, X; Liu, H; Xing, J; Yang, A; Zang, M; Zhao, L; Zhu, F, 2014
)
0.4
" No polymorphic effect was found for UGT1A9 (I399C>T) and UGT2B7*2 (802C>T) on the pharmacokinetic profiles of DHA and its metabolite DHA-Glu."( The effect of UGTs polymorphism on the auto-induction phase II metabolism-mediated pharmacokinetics of dihydroartemisinin in healthy Chinese subjects after oral administration of a fixed combination of dihydroartemisinin-piperaquine.
Li, X; Liu, H; Xing, J; Yang, A; Zang, M; Zhao, L; Zhu, F, 2014
)
0.4
" Malaria and pregnancy had no effect on the pharmacokinetic properties of artesunate or dihydroartemisinin after intravenous artesunate administration."( Opposite malaria and pregnancy effect on oral bioavailability of artesunate - a population pharmacokinetic evaluation.
Day, NP; Hanpithakpon, W; Hlaing, N; Kloprogge, F; McGready, R; Nosten, F; Phyo, AP; Rijken, MJ; Tarning, J; Than, HH; White, NJ; Zin, NT, 2015
)
0.42
"The population pharmacokinetic analysis demonstrated opposite effects of malaria and pregnancy on the bioavailability of orally administered artesunate."( Opposite malaria and pregnancy effect on oral bioavailability of artesunate - a population pharmacokinetic evaluation.
Day, NP; Hanpithakpon, W; Hlaing, N; Kloprogge, F; McGready, R; Nosten, F; Phyo, AP; Rijken, MJ; Tarning, J; Than, HH; White, NJ; Zin, NT, 2015
)
0.42
" Compartmental pharmacokinetic models were developed using a population-based approach."( Population pharmacokinetics, tolerability, and safety of dihydroartemisinin-piperaquine and sulfadoxine-pyrimethamine-piperaquine in pregnant and nonpregnant Papua New Guinean women.
Batty, KT; Benjamin, JM; Davis, TM; Lorry, L; Moore, BR; Mueller, I; Page-Sharp, M; Robinson, LJ; Salman, S; Siba, PM; Tawat, S; Yadi, G, 2015
)
0.42
"Piperaquine-dihydroartemisinin combination therapy has established efficacy for the treatment of malaria; however, a more comprehensive understanding of the pharmacokinetic properties and factors contributing to inter- and intra-individual variability is critical to optimize clinical use."( Effect of food on the pharmacokinetics of piperaquine and dihydroartemisinin.
Bacchieri, A; Evans, AM; Francis, B; Lungershausen, Y; Pace, S; Reuter, SE; Shakib, S; Ubben, D; Valentini, G, 2015
)
0.42
" Blood samples were collected for analysis of plasma piperaquine and dihydroartemisinin concentrations, which were utilized for calculation of pharmacokinetic parameters, using a standard model-independent approach."( Effect of food on the pharmacokinetics of piperaquine and dihydroartemisinin.
Bacchieri, A; Evans, AM; Francis, B; Lungershausen, Y; Pace, S; Reuter, SE; Shakib, S; Ubben, D; Valentini, G, 2015
)
0.42
" The observation of a shorter terminal half-life for lumefantrine may have contributed to a higher frequency of reinfection or a shorter posttreatment prophylactic period in pregnant women than in nonpregnant adults."( Artemether-Lumefantrine Pharmacokinetics and Clinical Response Are Minimally Altered in Pregnant Ugandan Women Treated for Uncomplicated Falciparum Malaria.
Achan, J; Aweeka, F; Huang, L; Kajubi, R; Kiconco, S; Mwebaza, N; Mwima, MW; Nguyen, VK; Nyunt, MM; Parikh, S; Ssebuliba, J, 2015
)
0.42
"Median parasite clearance half-life was prolonged, and clearance half-life was greater than 5 h in 21% of patients."( Parasite clearance rates in Upper Myanmar indicate a distinctive artemisinin resistance phenotype: a therapeutic efficacy study.
Ashley, EA; Aung, SS; Day, NP; Dhorda, M; Dondorp, AM; Hlaing, TM; Imwong, M; Jeeyapant, A; Promnarate, C; Smithuis, FM; Thein, M; Tun, KM; White, NJ; Woodrow, CJ; Yuentrakul, P, 2016
)
0.43
" The pharmacokinetic parameters of tafenoquine, piperaquine, lumefantrine, artemether, and dihydroartemisinin were determined by using noncompartmental methods."( Pharmacokinetic Interactions between Tafenoquine and Dihydroartemisinin-Piperaquine or Artemether-Lumefantrine in Healthy Adult Subjects.
Bouhired, S; Duparc, S; Goyal, N; Green, JA; Hussaini, A; Jones, SW; Koh, GC; Kostov, I; Mohamed, K; Taylor, M; Wolstenholm, A, 2016
)
0.43
" A population pharmacokinetic model was developed to compare exposure-response relationships between the 2DP and 3DP regimens while accounting for differences in regimen and sample collection times between studies."( Piperaquine Population Pharmacokinetics and Cardiac Safety in Cambodia.
Buathong, N; Cantilena, L; Chann, S; Haigney, M; Ittiverakul, M; Kodchakorn, C; Kuntawunginn, W; Lanteri, C; Lon, C; Manning, J; Milner, E; Pann, ST; Prom, S; Saunders, D; So, M; Sok, S; Spring, M; Sriwichai, S; Ta-Aksorn, W; Vanachayangkul, P; Wojnarski, M; Youdaline, T, 2017
)
0.46
"The aims of the present study were to evaluate the pharmacokinetic properties of dihydroartemisinin (DHA) and piperaquine, potential drug-drug interactions with concomitant primaquine treatment, and piperaquine effects on the electrocardiogram in healthy volunteers."( Population pharmacokinetics and electrocardiographic effects of dihydroartemisinin-piperaquine in healthy volunteers.
Blessborn, D; Chotsiri, P; Day, NPJ; Hanboonkunupakarn, B; Hoglund, RM; Jittamala, P; Pukrittayakamee, S; Tarning, J; Wattanakul, T; White, NJ, 2017
)
0.46
"The population pharmacokinetic properties of DHA and piperaquine were assessed in 16 healthy Thai adults using an open-label, randomized, crossover study."( Population pharmacokinetics and electrocardiographic effects of dihydroartemisinin-piperaquine in healthy volunteers.
Blessborn, D; Chotsiri, P; Day, NPJ; Hanboonkunupakarn, B; Hoglund, RM; Jittamala, P; Pukrittayakamee, S; Tarning, J; Wattanakul, T; White, NJ, 2017
)
0.46
" Concomitant treatment with primaquine did not affect the pharmacokinetic properties of DHA or piperaquine."( Population pharmacokinetics and electrocardiographic effects of dihydroartemisinin-piperaquine in healthy volunteers.
Blessborn, D; Chotsiri, P; Day, NPJ; Hanboonkunupakarn, B; Hoglund, RM; Jittamala, P; Pukrittayakamee, S; Tarning, J; Wattanakul, T; White, NJ, 2017
)
0.46
"Characterization of the pharmacokinetic properties of the enantiomers of primaquine and carboxyprimaquine following administration of racemic primaquine given alone and in combination with commonly used antimalarial drugs."( Enantiospecific pharmacokinetics and drug-drug interactions of primaquine and blood-stage antimalarial drugs.
Blessborn, D; Chairat, K; Day, NPJ; Hanboonkunupakarn, B; Hanpithakpong, W; Jittamala, P; Pukrittayakamee, S; Tarning, J; White, NJ, 2018
)
0.48
"Population pharmacokinetic models characterizing the enantiospecific properties of primaquine were developed successfully."( Enantiospecific pharmacokinetics and drug-drug interactions of primaquine and blood-stage antimalarial drugs.
Blessborn, D; Chairat, K; Day, NPJ; Hanboonkunupakarn, B; Hanpithakpong, W; Jittamala, P; Pukrittayakamee, S; Tarning, J; White, NJ, 2018
)
0.48
" The pharmacokinetic differences among blood cells and plasma still remain unclear."( Comparison of in vitro/in vivo blood distribution and pharmacokinetics of artemisinin, artemether and dihydroartemisinin in rats.
Dai, R; Dai, T; Guo, Z; Jiang, W; Xie, Y, 2019
)
0.51
" All studies on ART and DHA pharmacokinetic post-administration of artesunate in human patients or volunteers were included."( Systematic review of artesunate pharmacokinetics: Implication for treatment of resistant malaria.
Bienvenu, AL; Bonnot, G; Kouakou, YI; Lavoignat, A; Leboucher, G; Picot, S; Tod, M, 2019
)
0.51
" However, the RSA has several drawbacks: it is relatively low throughput, has high variance due to microscopy readout, and correlates poorly with the current benchmark for in vivo resistance, patient clearance half-life post-artemisinin treatment."( The extended recovery ring-stage survival assay provides a superior association with patient clearance half-life and increases throughput.
Anderson, TJC; Button-Simons, KA; Cassady, Z; Checkley, LA; Davis, SZ; Ferdig, MT; Foster, GJ; McDew-White, M; Nosten, FH; Shoue, DA; Sievert, MAC; Singh, PP; Vendrely, KM, 2020
)
0.56
" Due to the large number of pyknotic and dying parasites at 66 h post-exposure (72 h sample), parasites were grown for an additional cell cycle (114 h post-exposure, 120 h sample), which drastically improved correlation with patient clearance half-life compared to the 66 h post-exposure sample."( The extended recovery ring-stage survival assay provides a superior association with patient clearance half-life and increases throughput.
Anderson, TJC; Button-Simons, KA; Cassady, Z; Checkley, LA; Davis, SZ; Ferdig, MT; Foster, GJ; McDew-White, M; Nosten, FH; Shoue, DA; Sievert, MAC; Singh, PP; Vendrely, KM, 2020
)
0.56
" To optimally apply these drugs, information about their tissue-specific disposition is required, and one approach to predict these pharmacokinetic characteristics is physiologically based pharmacokinetic (PBPK) modeling."( Predicting the Disposition of the Antimalarial Drug Artesunate and Its Active Metabolite Dihydroartemisinin Using Physiologically Based Pharmacokinetic Modeling.
Arey, R; Reisfeld, B, 2021
)
0.62
" On this basis, the chemical components of XECQ were targeted and enriched by network pharmacology, to screen the main pharmacodynamic substances of XECQ in the treatment of acute upper respiratory tract infection in children and discuss the mechanism of action."( [Pharmacodynamic substances and mechanism of action of Xiaoer Chiqiao Qingre Granules in treatment of acute upper respiratory tract infection in children].
Feng, L; Jia, XB; Liu, J; Lu, GZ; Yang, YJ; Zhao, J; Zhu, MM; Zhu, XJ, 2022
)
0.72

Compound-Compound Interactions

ExcerptReferenceRelevance
"To observe the therapeutic efficacy of dihydroartemisinin combined with naphthoquine phosphate in patients with falciparum malaria."( [Therapeutic effect of dihydroartemisinin combined with naphthoquine phosphate in patients with falciparum malaria].
Lin, SG; Meng, F; Pang, XJ; Shen, H; Wang, SQ; Wen, Y; Zeng, LH; Zhu, QX; Zhuo, KR, 2002
)
0.31
"Patients with Plasmodium falciparum were selected as the subjects, treated with a single dose of dihydroarteminisinin 160 mg combined with naphthoquine phosphate 400 mg (for adults) and followed up in preselective time by blood and temperature examination for 28 days after drug administration."( [Therapeutic effect of dihydroartemisinin combined with naphthoquine phosphate in patients with falciparum malaria].
Lin, SG; Meng, F; Pang, XJ; Shen, H; Wang, SQ; Wen, Y; Zeng, LH; Zhu, QX; Zhuo, KR, 2002
)
0.31
" This study was conducted to evaluate the antimalarial potential of clindamycin in combination with dihydroartemisinin in continuously cultured and in freshly isolated Plasmodium falciparum parasites, measuring the inhibition of Plasmodium falciparum histidine-rich protein II synthesis."( In vitro activity and interaction of clindamycin combined with dihydroartemisinin against Plasmodium falciparum.
Graninger, W; Kremsner, PG; Noedl, H; Ramharter, M; Wernsdorfer, WH; Winkler, H; Winkler, S, 2003
)
0.32
" Competitive uptake of radiolabeled chloroquine and dihydroartemisinin in combination with other antimalarials was observed."( Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
Adagu, IS; Fivelman, QL; Warhurst, DC, 2007
)
0.34
" This study also demonstrated the effectiveness of high-resolution mass spectrometry in combination with an online H/D exchange LC/HR-MS(n) technique in rapid identification of drug metabolites."( Metabolite identification of artemether by data-dependent accurate mass spectrometric analysis using an LTQ-Orbitrap hybrid mass spectrometer in combination with the online hydrogen/deuterium exchange technique.
Du, F; Liu, T; Xing, J; Zhu, F, 2011
)
0.37
"A multiple dose, parallel group study was conducted to assess for a drug-drug interaction between the pyronaridine/artesunate (PA) combination antimalarial and ritonavir."( Drug-drug interaction analysis of pyronaridine/artesunate and ritonavir in healthy volunteers.
Borghini-Fuhrer, I; Duparc, S; Fleckenstein, L; Jung, D; Lopez-Lazaro, L; Methaneethorn, J; Morris, CA; Pokorny, R; Shin, CS, 2012
)
0.38
"A high prevalence of chloroquine-resistant Plasmodium vivax in Indonesia has shifted first-line treatment to artemisinin-based combination therapies, combined with primaquine (PQ) for radical cure."( A randomized comparison of dihydroartemisinin-piperaquine and artesunate-amodiaquine combined with primaquine for radical treatment of vivax malaria in Sumatera, Indonesia.
Chavez, I; Chokejindachai, W; Dondorp, AM; Imwong, M; Pasaribu, AP; Pasaribu, S; Sirivichayakul, C; Tanomsing, N; Tjitra, E; White, NJ, 2013
)
0.39
"Artesunate (AS) in combination with sulfadoxine/pyrimethamine (SP) is the first-line therapy for management of uncomplicated Plasmodium falciparum malaria in Sudan."( Pharmacokinetics of artesunate alone and in combination with sulfadoxine/pyrimethamine in healthy Sudanese volunteers.
Awad, AI; Elamin, SB; Matar, KM, 2014
)
0.4
" Therefore, a more thorough assessment of their potential clinical use through a rodent model and an in vitro evaluation of their combination with artemisinin was undertaken."( Enantiomerically pure amino-alcohol quinolines: in vitro anti-malarial activity in combination with dihydroartemisinin, cytotoxicity and in vivo efficacy in a Plasmodium berghei mouse model.
Agnamey, P; Degrouas, C; Jonet, A; Mullié, C; Pascual, A; Sonnet, P; Taudon, N, 2014
)
0.4
" falciparum clones with varying resistance profiles and regional origins was performed for the (S)-pentyl and (S)-heptyl substituted quinoline derivatives, followed by an in vitro assessment of their combination with dihydroartemisinin (DHA) on the 3D7 clone and an in vivo assay in a mouse model infected with Plasmodium berghei."( Enantiomerically pure amino-alcohol quinolines: in vitro anti-malarial activity in combination with dihydroartemisinin, cytotoxicity and in vivo efficacy in a Plasmodium berghei mouse model.
Agnamey, P; Degrouas, C; Jonet, A; Mullié, C; Pascual, A; Sonnet, P; Taudon, N, 2014
)
0.4
" The in vitro combination with DHA yielded an additive or synergic effect for both that was as good as that of the DHA/MQ combination."( Enantiomerically pure amino-alcohol quinolines: in vitro anti-malarial activity in combination with dihydroartemisinin, cytotoxicity and in vivo efficacy in a Plasmodium berghei mouse model.
Agnamey, P; Degrouas, C; Jonet, A; Mullié, C; Pascual, A; Sonnet, P; Taudon, N, 2014
)
0.4
"Characterization of the pharmacokinetic properties of the enantiomers of primaquine and carboxyprimaquine following administration of racemic primaquine given alone and in combination with commonly used antimalarial drugs."( Enantiospecific pharmacokinetics and drug-drug interactions of primaquine and blood-stage antimalarial drugs.
Blessborn, D; Chairat, K; Day, NPJ; Hanboonkunupakarn, B; Hanpithakpong, W; Jittamala, P; Pukrittayakamee, S; Tarning, J; White, NJ, 2018
)
0.48
"Enantiomeric pharmacokinetics were evaluated in 49 healthy adult volunteers enrolled in three randomized cross-over studies in which a single dose of primaquine was given alone and then, after a suitable washout period, in combination with chloroquine, dihydroartemisinin/piperaquine or pyronaridine/artesunate."( Enantiospecific pharmacokinetics and drug-drug interactions of primaquine and blood-stage antimalarial drugs.
Blessborn, D; Chairat, K; Day, NPJ; Hanboonkunupakarn, B; Hanpithakpong, W; Jittamala, P; Pukrittayakamee, S; Tarning, J; White, NJ, 2018
)
0.48
" No drug-drug interaction effects were seen on the pharmacokinetics of either carboxyprimaquine enantiomer."( Enantiospecific pharmacokinetics and drug-drug interactions of primaquine and blood-stage antimalarial drugs.
Blessborn, D; Chairat, K; Day, NPJ; Hanboonkunupakarn, B; Hanpithakpong, W; Jittamala, P; Pukrittayakamee, S; Tarning, J; White, NJ, 2018
)
0.48
" Furthermore, doxycycline has anti-malarial properties and is already recommended as prophylaxis for travellers and for treatment of falciparum malaria in combination with other anti-malarial drugs."( Has doxycycline, in combination with anti-malarial drugs, a role to play in intermittent preventive treatment of Plasmodium falciparum malaria infection in pregnant women in Africa?
Boxberger, M; Gaillard, T; Madamet, M; Pradines, B, 2018
)
0.48
" Thus, we are in dire need of alternate chemotherapeutic agents which in combination with artemisinin (or its analogues) are efficacious against chloroquine-resistant strains."( In vitro synergistic interaction of potent 4-aminoquinolines in combination with dihydroartemisinin against chloroquine-resistant Plasmodium falciparum.
Agarwal, D; Awasthi, SK; Gupta, RD; Singh, S, 2019
)
0.51
" Although the clinical importance remains unclear to date, clinicians should be aware of potential drug-drug interactions and monitor patients on ACT closely."( Drug-Drug Interactions of Artemisinin-Based Combination Therapies in Malaria Treatment: A Narrative Review of the Literature.
Grundmann, O; Hernandez Maldonado, J, 2022
)
0.72
" We aimed to establish the efficacy and safety of three single low doses of tafenoquine in combination with dihydroartemisinin-piperaquine for reducing gametocyte density and transmission to mosquitoes."( Single low-dose tafenoquine combined with dihydroartemisinin-piperaquine to reduce Plasmodium falciparum transmission in Ouelessebougou, Mali: a phase 2, single-blind, randomised clinical trial.
Attaher, O; Bousema, T; Bradley, J; Diallo, M; Dicko, A; Dicko, OM; Drakeley, C; Issiaka, D; Keita, S; Lanke, K; Maguiraga, SO; Mahamar, A; McCall, MBB; Niambele, SM; Sacko, A; Samake, S; Sanogo, K; Sinaba, Y; Smit, MJ; Stone, W; Ter Heine, R; Traore, SF, 2022
)
0.72
" This study evaluated the efficacy of different dosages of aqueous extract of Strychnos ligustrina combined with dihydroartemisinin and piperaquine phosphate (DHP) against murine Plasmodium berghei infection."( Antimalarial Efficacy of Aqueous Extract of Strychnos ligustrina and Its Combination with Dihydroartemisinin and Piperaquine Phosphate (DHP) against Plasmodium berghei Infection.
Cahyaningsih, U; Maring, AJ; Nugraha, AB; Sa'diah, S; Sari, RK; Syafii, W, 2022
)
0.72

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
"Tetrazole, a bioisostere of the carboxylic acid group, can replace the carboxyl group in drugs to increase the lipophilicity, bioavailability and reduce side effects."( Recent advances of tetrazole derivatives as potential anti-tubercular and anti-malarial agents.
Chang, L; Ding, C; Feng, LS; Gao, C; Wu, X; Xu, Z; Yan, XF; Zhao, F, 2019
)
0.51
" It would appear that the bioavailability of DHQHS tablets is much higher than that of QHS when given orally to the dog."( [The pharmacokinetics of dihydroqinghasu given orally to rabbits and dogs].
Song, ZY; Zhao, KC, 1990
)
0.28
" We conclude that the bioavailability of intramuscular AM in children with severe malaria may be highly variable, particularly in the presence of respiratory distress, and may be associated with an inadequate therapeutic response."( The disposition of intramuscular artemether in children with cerebral malaria; a preliminary study.
Crawley, J; English, M; Lowe, B; Marsh, K; Mberu, E; Muhia, D; Murphy, SA; Newton, CR; Waruiru, C; Watkins, WM; Winstanley, P,
)
0.13
"The pharmacokinetics and bioavailability of dihydroartemisinin (DQHS), artemether (AM), arteether (AE), artesunic acid (AS) and artelinic acid (AL) have been investigated in rats after single intravenous, intramuscular and intragastric doses of 10 mg kg(-1)."( The pharmacokinetics and bioavailability of dihydroartemisinin, arteether, artemether, artesunic acid and artelinic acid in rats.
Brewer, TG; Fleckenstein, LL; Heiffer, MH; Li, QG; Masonic, K; Peggins, JO, 1998
)
0.3
" Pharmacokinetics of dihydroartemisinin and mefloquine when given concurrently were similar, except for the absorption rate of mefloquine which was faster in the presence of dihydroartemisinin."( Pharmacokinetic and pharmacodynamic interactions of mefloquine and dihydroartemisinin.
Karbwang, J; Na-Bangchang, K; Thanavibul, A; Tippawangkosol, P; Ubalee, R, 1999
)
0.3
" The aim of this study was to evaluate the effect of grapefruit juice on the decreasing bioavailability over time of artemether."( The effect of grapefruit juice on the time-dependent decline of artemether plasma levels in healthy subjects.
Gupta, V; van Agtmael, MA; van Boxtel, CJ; van der Graaf, CA, 1999
)
0.3
"Grapefruit juice significantly increased the oral bioavailability of artemether but did not prevent the time-dependent reduction in bioavailability."( The effect of grapefruit juice on the time-dependent decline of artemether plasma levels in healthy subjects.
Gupta, V; van Agtmael, MA; van Boxtel, CJ; van der Graaf, CA, 1999
)
0.3
" Mefloquine from the three formulations showed significantly different pharmacokinetic and bioavailability metrics."( Pharmacokinetics and bioequivalence evaluation of three commercial tablet formulations of mefloquine when given in combination with dihydroartemisinin in patients with acute uncomplicated falciparum malaria.
Karbwang, J; Na-Bangchang, K; Palacios, PA; Saengtertsilapachai, S; Ubalee, R; Wernsdorfer, WH, 2000
)
0.31
"To obtain comprehensive bioavailability data for artesunate (ARTS) and its active metabolite dihydroartemisinin (DHA) following their separate oral administration to Vietnamese volunteers and to patients with acute, uncomplicated falciparum malaria."( Oral bioavailability of dihydroartemisinin in Vietnamese volunteers and in patients with falciparum malaria.
Batty, KT; Binh, TQ; Davis, TM; Hung, NC; Ilett, KF; Phuöng, HL; Phuong, VD; Powell, SM; Thien, HV; Thu, LT, 2001
)
0.31
" Pharmacokinetic descriptors were obtained from noncompartmental analysis and bioavailability was calculated from AUC data."( Oral bioavailability of dihydroartemisinin in Vietnamese volunteers and in patients with falciparum malaria.
Batty, KT; Binh, TQ; Davis, TM; Hung, NC; Ilett, KF; Phuöng, HL; Phuong, VD; Powell, SM; Thien, HV; Thu, LT, 2001
)
0.31
"In Group 1 (volunteers), the mean (95% CI) absolute bioavailability of oral ARTS was 80% (62,98%), while in Group 2 (volunteers), the bioavailability of oral DHA was 45% (34,56%)."( Oral bioavailability of dihydroartemisinin in Vietnamese volunteers and in patients with falciparum malaria.
Batty, KT; Binh, TQ; Davis, TM; Hung, NC; Ilett, KF; Phuöng, HL; Phuong, VD; Powell, SM; Thien, HV; Thu, LT, 2001
)
0.31
"The study shows that the absolute bioavailability of DHA was significantly lower than that for ARTS in healthy volunteers."( Oral bioavailability of dihydroartemisinin in Vietnamese volunteers and in patients with falciparum malaria.
Batty, KT; Binh, TQ; Davis, TM; Hung, NC; Ilett, KF; Phuöng, HL; Phuong, VD; Powell, SM; Thien, HV; Thu, LT, 2001
)
0.31
"34 hr, and the bioavailability over 12 hr (area under the curve [AUC](0-12)) was 253+/-185 nmol hr/L."( Comparative pharmacokinetics and effect kinetics of orally administered artesunate in healthy volunteers and patients with uncomplicated falciparum malaria.
Brewer, TG; Eamsila, C; Jongsakul, K; Keeratithakul, G; Kyle, DE; Li, Q; Luesutthiviboon, L; Sirisopana, N; Teja-Isavadharm, P; Watt, G, 2001
)
0.31
" The mean antimalarial activity in terms of the bioavailability of DHA relative to that of artesunate did not differ significantly from 1, suggesting that DHA can be formulated to be an acceptable oral alternative to artesunate."( Comparison of oral artesunate and dihydroartemisinin antimalarial bioavailabilities in acute falciparum malaria.
Looareesuwan, S; Newton, PN; Nosten, F; Rasameesoroj, M; Ruangveerayuth, R; Siriyanonda, D; Slight, T; Suputtamongkol, Y; Teerapong, P; Teja-Isavadharm, P; van Vugt, M; White, NJ, 2002
)
0.31
"The aim of this study was to evaluate the bioavailability of artesunate (ARTS) and dihydroartemisinin (DHA)."( Relative bioavailability of artesunate and dihydroartemisinin: investigations in the isolated perfused rat liver and in healthy Caucasian volunteers.
Batty, KT; Davis, TM; Iletr, KE; Martin, J; Powell, SM, 2002
)
0.31
" The mean common volumes of distribution for ARTS and DHA relative to bioavailability were 42."( Disposition of artesunate and dihydroartemisinin after administration of artesunate suppositories in children from Papua New Guinea with uncomplicated malaria.
Alpers, MP; Barrett, PH; Bockarie, M; Davis, TM; Dufall, K; Ilett, KF; Karunajeewa, HA; Kemiki, A; Vicini, P, 2004
)
0.32
" Patients with the lowest area under the DHA concentration curve did not have slower parasite clearance, suggesting that rectal artesunate is well absorbed in most patients with moderately severe malaria."( Population pharmacokinetics of artesunate and dihydroartemisinin following intra-rectal dosing of artesunate in malaria patients.
Agbenyega, T; Barnes, KI; Di Perri, G; Folb, P; Gomes, M; Krishna, S; Krudsood, S; Looareesuwan, S; Mansor, S; McIlleron, H; Miller, R; Molyneux, M; Mwenechanya, J; Navaratnam, V; Nosten, F; Olliaro, P; Pang, L; Ribeiro, I; Simpson, JA; Tembo, M; van Vugt, M; Ward, S; Weerasuriya, K; White, NJ; Win, K, 2006
)
0.33
" This thermolability coupled with the poor physicochemical properties and relative oral bioavailability of DHA suggests that it is inferior to artesunate in application as an antimalarial drug."( Artesunate and dihydroartemisinin (DHA): unusual decomposition products formed under mild conditions and comments on the fitness of DHA as an antimalarial drug.
Cartwright, A; Chan, HW; Gomes, MF; Haynes, RK; Lung, CM; Ng, NC; Shek, LY; Williams, ID; Wong, HN, 2007
)
0.34
" We summarized the data under the following themes: content and dissolution; relative bioavailability of antimalarial products; antimalarial stability and shelf life; general tests on pharmaceutical dosage forms; and the presence of degradation or unidentifiable impurities in formulations."( Antimalarial drug quality in Africa.
Amin, AA; Kokwaro, GO, 2007
)
0.34
" The literature was varied in the quality and breadth of data presented, with most bioavailability studies poorly designed and executed."( Antimalarial drug quality in Africa.
Amin, AA; Kokwaro, GO, 2007
)
0.34
"79 L/kg); the bioavailability was 100%."( Pharmacokinetics of artesunate in the domestic pig.
Aglioni, C; Bressolle, FM; Mosnier, J; Parzy, D; Sinou, V; Taudon, N, 2008
)
0.35
" The method is sensitive, selective, accurate, reproducible and suited particularly for pharmacokinetic study of AS-AQ drug combination and can also be used to compare the bioavailability of different formulations, including a fixed-dose AS-AQ co-formulation."( Validation of high performance liquid chromatography-electrochemical detection methods with simultaneous extraction procedure for the determination of artesunate, dihydroartemisinin, amodiaquine and desethylamodiaquine in human plasma for application in c
Lai, CS; Mansor, SM; Muniandy, A; Nair, NK; Navaratnam, V; Olliaro, PL, 2009
)
0.35
" In addition, the oral bioavailability of piperaquine improves when given with a high-fat meal, though this does not necessarily translate into a higher efficacy."( Progress in the development of piperaquine combinations for the treatment of malaria.
D'alessandro, U, 2009
)
0.35
" During early development of this new formulation, two studies were performed in healthy subjects, one to evaluate the palatability of three flavours of A-L, and a second one to compare the bioavailability of active principles between the dispersible tablet and the tablet (administered crushed and intact)."( Early clinical development of artemether-lumefantrine dispersible tablet: palatability of three flavours and bioavailability in healthy subjects.
Abdulla, S; Amuri, B; Fitoussi, S; Kabanywanyi, AM; Kaiser, G; Lefèvre, G; Nuortti, M; Pascoe, S; Reynolds, C; Séchaud, R; Ubben, D; Yeh, CM, 2010
)
0.36
" The objectives were to compare the bioavailability of artemether, dihydroartemisinin (DHA) and lumefantrine between the dispersible tablet and the tablet administered crushed (primary objective) and intact (secondary objective)."( Early clinical development of artemether-lumefantrine dispersible tablet: palatability of three flavours and bioavailability in healthy subjects.
Abdulla, S; Amuri, B; Fitoussi, S; Kabanywanyi, AM; Kaiser, G; Lefèvre, G; Nuortti, M; Pascoe, S; Reynolds, C; Séchaud, R; Ubben, D; Yeh, CM, 2010
)
0.36
"The aim of the present study was to compare the pharmacokinetic properties, bioavailability and tolerability of artesunate (AS) and amodiaquine (AQ) administered as a fixed-dose combination (Amonate FDC tablets; Dafra Pharma, Turnhout, Belgium) or as a non-fixed dose combination of separate AS tablets (Arsuamoon; Guilin Pharmaceutical Co, Shanghai, China) and AQ tablets (Flavoquine; Sanofi-Aventis, Paris, France)."( Comparative oral bioavailability of non-fixed and fixed combinations of artesunate and amodiaquine in healthy Indian male volunteers.
Fortin, A; Jansen, FH; Verbeeck, RK, 2011
)
0.37
"Dihydroartemisinin (DHA) is a poorly water-soluble drug that displays low bioavailability after oral administration."( Improving the solubility and bioavailability of dihydroartemisinin by solid dispersions and inclusion complexes.
Ansari, MT; Batty, KT; Iqbal, I; Sunderland, VB, 2011
)
0.37
" The lipophilic characteristic of piperaquine suggests that administration together with fat will increase the oral bioavailability of the drug, and this has been reported for healthy volunteers."( A small amount of fat does not affect piperaquine exposure in patients with malaria.
Annerberg, A; Ashley, E; Day, NP; Khrutsawadchai, S; Lindegardh, N; Lwin, KM; Nosten, F; Singhasivanon, P; Tarning, J; White, NJ, 2011
)
0.37
" Similarly high bioavailability of DHA (> 80%) is associated with oral administration."( Review of the clinical pharmacokinetics of artesunate and its active metabolite dihydroartemisinin following intravenous, intramuscular, oral or rectal administration.
Borghini-Fuhrer, I; Duparc, S; Fleckenstein, L; Jung, D; Morris, CA; Shin, CS, 2011
)
0.37
" The corresponding median absolute oral bioavailability (F%) was 21."( Artesunate/dihydroartemisinin pharmacokinetics in acute falciparum malaria in pregnancy: absorption, bioavailability, disposition and disease effects.
Hanpithakpon, W; Hlaing, N; Lindegardh, N; McGready, R; Nosten, F; Phyo, AP; Rijken, MJ; Singhasivanon, P; Tarning, J; Than, HH; White, NJ; Zin, NT, 2012
)
0.38
" Piperaquine was best described by a three-compartment disposition model with a 45% higher elimination clearance and a 47% increase in relative bioavailability in pregnant women compared with nonpregnant women."( Population pharmacokinetics of dihydroartemisinin and piperaquine in pregnant and nonpregnant women with uncomplicated malaria.
Day, NP; Hanpithakpong, W; Lindegardh, N; McGready, R; Nosten, F; Phyo, AP; Rijken, MJ; Tarning, J; White, NJ, 2012
)
0.38
" This study examined increasing DHA bioavailability by encapsulating DHA within gelatin (GEL) or hyaluronan (HA) nanoparticles via an electrostatic field system."( Enhanced apoptotic effects of dihydroartemisinin-aggregated gelatin and hyaluronan nanoparticles on human lung cancer cells.
Chang, SJ; Chen, IF; Gao, J; Kuo, SM; Sun, Q; Teong, B, 2014
)
0.4
" Besides its effectiveness, it is a poorly water soluble drug with low bioavailability and low half-life (34-90 min), therefore, the development of new formulations of dihydroartemisinin to increase bioavailability is in great need."( Strategy to provide a useful solution to effective delivery of dihydroartemisinin: development, characterization and in vitro studies of liposomal formulations.
Bergonzi, MC; Bilia, AR; Coronnello, M; Isacchi, B; Mastrantoni, A; Mini, E; Righeschi, C, 2014
)
0.4
"Coadministration of dihydroartemisinin-piperaquine (DHA-PQ) with fat may improve bioavailability and antimalarial efficacy, but it might also increase toxicity."( Effect of coadministered fat on the tolerability, safety, and pharmacokinetic properties of dihydroartemisinin-piperaquine in Papua New Guinean children with uncomplicated malaria.
Batty, KT; Benjamin, JM; Davis, TM; Ginny, E; Griffin, S; Moore, BR; Mueller, I; Page-Sharp, M; Robinson, LJ; Salman, S; Siba, P, 2014
)
0.4
" The metabolic capability could recover after a 12-h dosing interval, which suggested that the alternative common three-day regimen (once daily) for DHA-PQ could probably lead to higher bioavailability of DHA."( The effect of UGTs polymorphism on the auto-induction phase II metabolism-mediated pharmacokinetics of dihydroartemisinin in healthy Chinese subjects after oral administration of a fixed combination of dihydroartemisinin-piperaquine.
Li, X; Liu, H; Xing, J; Yang, A; Zang, M; Zhao, L; Zhu, F, 2014
)
0.4
" Malaria increased the absolute oral bioavailability of artesunate by 87%, presumably by inhibiting first pass effect, whereas pregnancy decreased oral bioavailability by 23%."( Opposite malaria and pregnancy effect on oral bioavailability of artesunate - a population pharmacokinetic evaluation.
Day, NP; Hanpithakpon, W; Hlaing, N; Kloprogge, F; McGready, R; Nosten, F; Phyo, AP; Rijken, MJ; Tarning, J; Than, HH; White, NJ; Zin, NT, 2015
)
0.42
"The population pharmacokinetic analysis demonstrated opposite effects of malaria and pregnancy on the bioavailability of orally administered artesunate."( Opposite malaria and pregnancy effect on oral bioavailability of artesunate - a population pharmacokinetic evaluation.
Day, NP; Hanpithakpon, W; Hlaing, N; Kloprogge, F; McGready, R; Nosten, F; Phyo, AP; Rijken, MJ; Tarning, J; Than, HH; White, NJ; Zin, NT, 2015
)
0.42
"001) in association with a greater clearance relative to bioavailability (73."( Population pharmacokinetics, tolerability, and safety of dihydroartemisinin-piperaquine and sulfadoxine-pyrimethamine-piperaquine in pregnant and nonpregnant Papua New Guinean women.
Batty, KT; Benjamin, JM; Davis, TM; Lorry, L; Moore, BR; Mueller, I; Page-Sharp, M; Robinson, LJ; Salman, S; Siba, PM; Tawat, S; Yadi, G, 2015
)
0.42
" This likely reflects an increase in the oral bioavailability of the drug, directly related to the fat content of the meal."( Effect of food on the pharmacokinetics of piperaquine and dihydroartemisinin.
Bacchieri, A; Evans, AM; Francis, B; Lungershausen, Y; Pace, S; Reuter, SE; Shakib, S; Ubben, D; Valentini, G, 2015
)
0.42
"The use of dihydroartemisinin (DHA) for effective malaria treatment is challenged by its poor aqueous solubility and inadequate bioavailability leading to treatment failures and emergence of resistant strains."( Development Insights of Surface Modified Lipid Nanoemulsions of Dihydroartemisinin for Malaria Chemotherapy: Characterization, and in vivo Antimalarial Evaluation.
Attama, A; Chukwuka, R; Obachie, O; Umeyor, CE, 2019
)
0.51
"Magnetic DHA nano-liposomes (DHA-MLPs) were developed to improve the targeting antitumor efficiency and bioavailability of DHA, and their physical properties were characterized."( Effects of magnetic dihydroartemisinin nano-liposome in inhibiting the proliferation of head and neck squamous cell carcinomas.
Li, H; Li, X; Li, Z; Shi, X; Sun, Y, 2019
)
0.51
" However, it is associated with some limitations, such as low bioavailability which is hampered by its poor aqueous solubility and its rapid metabolism in systemic circulation."( Hyaluronic acid - dihydroartemisinin conjugate: Synthesis, characterization and in vitro evaluation in lung cancer cells.
Kumar, R; Meena, J; Panda, AK; Saneja, A; Singh, M; Singhvi, P; Thiyagarajan, D, 2019
)
0.51
" They also showed exceptionally better treatment of malaria owing to their sustained release properties and improved bioavailability and are recommended to Pharmaceutical companies for further studies."( Assessment of the Anti-Malarial Properties of Dihydroartemisinin- Piperaquine Phosphate Solid Lipid-Based Tablets.
Amarachi, CS; Attama, AA; Onunkwo, GC, 2022
)
0.72
" Nevertheless, the poor water solubility and low bioavailability of DHA seriously impede its clinical applications."( Self-assembly and self-delivery of the pure nanodrug dihydroartemisinin for tumor therapy and mechanism analysis.
Bi, J; Feng, X; Li, W; Li, Y; Shi, N; Xie, Z; Zhang, W; Zhu, W, 2023
)
0.91

Dosage Studied

ExcerptRelevanceReference
"5 micrograms/ml of DHA was reached at about 3 minutes after dosing and the AUC was 82 mg/L."( [Pharmacokinetics and metabolism of artesunate in cows].
Huo, JZ; Xia, WJ; Xue, M; Zhou, ZT, 1991
)
0.28
" This novel drug delivery system may be an easy and safe way to administer artemisinin-type antimalarials and also a good alternative dosage form for active compounds with solubility problems."( Antimalarial activity of dihydroartemisinin derivatives by transdermal application.
Ager, AL; Klayman, DL; Lin, AJ, 1994
)
0.29
" A suppository of QHS, a dual-pack dosage form of ATS (artesunic acid to be dissolved in sodium bicarbonate solution just before iv injection) and an oil solution of ATM for im injection had been approved by our Ministry of Health for clinical use."( [Pharmacokinetics of dihydroqinghaosu in human volunteers and comparison with qinghaosu].
Song, ZY; Zhao, KC, 1993
)
0.29
" A significant therapeutic problem is a high, late recrudescence rate, probably due to short half-lives of both artesunate and its active metabolite dihydroartemisinin relative to conventional dosing intervals."( Chemical stability of artesunate injection and proposal for its administration by intravenous infusion.
Batty, KT; Davis, ME; Davis, T; Ilett, KF, 1996
)
0.29
" berghei (with 3/8 cured) superior to that of artelinic acid (1/8 cured), whereas p-fluorophenyl and p-methoxyphenyl analogs demonstrated activity only comparable (1/8 cured) to that of artelinic acid at the same dosage level (64 mg/kg twice a day)."( Antimalarial activity of new dihydroartemisinin derivatives. 7. 4-(p-substituted phenyl)-4(R or S)-[10(alpha or beta)-dihydroartemisininoxy]butyric acids.
Kyle, DE; Lin, AJ; Zikry, AB, 1997
)
0.3
" Plasma was separated from blood samples collected at different times after dosing and analysed for parent drug."( The pharmacokinetics and bioavailability of dihydroartemisinin, arteether, artemether, artesunic acid and artelinic acid in rats.
Brewer, TG; Fleckenstein, LL; Heiffer, MH; Li, QG; Masonic, K; Peggins, JO, 1998
)
0.3
"5) hours after dosing [median (range)]."( Pharmacokinetics and ex vivo anti-malarial activity of sera following a single oral dose of dihydroartemisinin in healthy Thai males.
Congpoung, K; Karbwang, J; Na-Bangchang, K; Tan-anya, P; Thanavibul, A; Ubalee, R, 1997
)
0.3
" The dosage was 60 mg daily or 2 mg/kg for paediatric patients for 7 successive days with the first dose doubled."( [Efficacy of dihydroartemisinin in treatment of 37 malaria cases].
Ding, Y; Qi, Z; Xu, C, 1997
)
0.3
" For monotherapeutic regimen(s) of DHA, dosing frequency of at least twice a day is suggested."( Phamacokinetics of a single oral dose of dihydroartemisinin in Vietnamese healthy volunteers.
Karbwang, J; Le, NH; Le, TD; Na-Bangchang, K; Thrinh, KA, 1999
)
0.3
" Thus, the use of conventional oral dosage regimens of ARTS appears preferable to oral administration of DHA."( Relative bioavailability of artesunate and dihydroartemisinin: investigations in the isolated perfused rat liver and in healthy Caucasian volunteers.
Batty, KT; Davis, TM; Iletr, KE; Martin, J; Powell, SM, 2002
)
0.31
" Dose-response curves for a Plasmodium falciparum clone (clone W2) and DHA were used as a standard for each assay."( Plasmodium falciparum-based bioassay for measurement of artemisinin derivatives in plasma or serum.
Brewer, TG; Kyle, DE; Peggins, JO; Teja-Isavadharm, P; Webster, HK; White, NJ, 2004
)
0.32
"The current dosage of DP (6."( Randomized, controlled dose-optimization studies of dihydroartemisinin-piperaquine for the treatment of uncomplicated multidrug-resistant falciparum malaria in Thailand.
Ashley, EA; Brockman, A; Hutagalung, R; Krudsood, S; Leowattana, W; Looareesuwan, S; McGready, R; Nosten, F; Phaiphun, L; Srivilairit, S; White, NJ; Wilairatana, P, 2004
)
0.32
"7 hours on day 4 for both dosage regimens."( Pharmacokinetic investigation on the therapeutic potential of artemotil (beta-arteether) in Thai patients with severe Plasmodium falciparum malaria.
Chalearmrult, K; Krudsood, S; Li, Q; Looareesuwan, S; Lugt, CB; Milhous, WK; Vannaphan, S; Wilairatana, P, 2004
)
0.32
" Two dosage regimens were tested: prophylaxis and treatment."( Treatment of malaria in a mouse model by intranasal drug administration.
Godin, B; Golenser, J; Touitou, E; Waknine, JH, 2006
)
0.33
" To inform dosage recommendations we assessed the pharmacokinetics of intravenous artesunate after the first dose."( The pharmacokinetics of intravenous artesunate in adults with severe falciparum malaria.
Barnes, KI; Chierakul, W; Evans, AC; Newton, PN; Ruangveerayuth, R; Smith, PJ; White, NJ, 2006
)
0.33
"Antimalarial treatment strategies based on in vitro studies are limited by the paucity of pharmacodynamic information for dosage regimen design."( Development of a pharmacodynamic model of murine malaria and antimalarial treatment with dihydroartemisinin.
Barrett, PH; Batty, KT; Davis, TM; Gibbons, PL; Ilett, KF, 2007
)
0.34
" The dosing regimen has been simplified from four doses to once daily over 3 days."( Efficacy and safety of dihydroartemisinin-piperaquine.
Ashley, EA; Day, NP; Myint, HY; Nosten, F; White, NJ, 2007
)
0.34
" We summarized the data under the following themes: content and dissolution; relative bioavailability of antimalarial products; antimalarial stability and shelf life; general tests on pharmaceutical dosage forms; and the presence of degradation or unidentifiable impurities in formulations."( Antimalarial drug quality in Africa.
Amin, AA; Kokwaro, GO, 2007
)
0.34
" The review highlights the common finding in drug quality studies that (i) most antimalarial products pass the basic tests for pharmaceutical dosage forms, such as the uniformity of weight for tablets, (ii) most antimalarial drugs pass the content test and (iii) in vitro product dissolution is the main problem area where most drugs fail to meet required pharmacopoeial specifications, especially with regard to sulfadoxine-pyrimethamine products."( Antimalarial drug quality in Africa.
Amin, AA; Kokwaro, GO, 2007
)
0.34
" After dose range study, rats were dosed at either 160 mg/kg daily for 9 consecutive days or at 288 mg/kg once every other day for five doses, so that the total dose (1440 mg/kg) and duration (9 days) were identical."( Neurotoxicity and toxicokinetics of artelinic acid following repeated oral administration in rats.
Bennett, K; Johnson, TO; Li, Q; Mog, S; Si, Y; Weina, PJ; Xie, L,
)
0.13
"The population pharmacokinetics of piperaquine in adults and children with uncomplicated Plasmodium falciparum malaria treated with two different dosage regimens of dihydroartemisinin-piperaquine were characterized."( Population pharmacokinetics of piperaquine after two different treatment regimens with dihydroartemisinin-piperaquine in patients with Plasmodium falciparum malaria in Thailand.
Ashley, EA; Ashton, M; Day, NP; Lindegardh, N; McGready, R; Nosten, F; Phaiphun, L; Stepniewska, K; Tarning, J; White, NJ, 2008
)
0.35
" However, AL has several limitations, including a twice-daily dosing regimen, recommendation for administration with fatty food, and a high risk of reinfection soon after therapy in high transmission areas."( Artemether-lumefantrine versus dihydroartemisinin-piperaquine for treating uncomplicated malaria: a randomized trial to guide policy in Uganda.
Bukirwa, H; Dorsey, G; Kamya, MR; Lugemwa, M; Rosenthal, PJ; Rwakimari, JB; Staedke, SG; Talisuna, A; Wabwire-Mangen, F; Yeka, A, 2008
)
0.35
"DP is highly efficacious, and operationally preferable to AL because of a less intensive dosing schedule and requirements."( Artemether-lumefantrine versus dihydroartemisinin-piperaquine for treating uncomplicated malaria: a randomized trial to guide policy in Uganda.
Bukirwa, H; Dorsey, G; Kamya, MR; Lugemwa, M; Rosenthal, PJ; Rwakimari, JB; Staedke, SG; Talisuna, A; Wabwire-Mangen, F; Yeka, A, 2008
)
0.35
"Groups of up to 15 pregnant females were dosed on Gestation Days (GD) 20-50 or for 3-7-day intervals."( Artesunate: developmental toxicity and toxicokinetics in monkeys.
Arima, A; Bernard, F; Clark, RL; Gristwood, W; Harrell, A; Makori, N; Nakata, Y; White, TE; Wier, PJ, 2008
)
0.35
"Artesunate was embryolethal at > or =12 mg/kg/day when dosed for at least 12 days at the beginning of organogenesis, but not when dosed for 3 or 7 days, indicating that developmental toxicity of artesunate is dependent upon duration of dosing in cynomologus monkeys."( Artesunate: developmental toxicity and toxicokinetics in monkeys.
Arima, A; Bernard, F; Clark, RL; Gristwood, W; Harrell, A; Makori, N; Nakata, Y; White, TE; Wier, PJ, 2008
)
0.35
" C(max) and AUC of artesunate and DHA following iv dosing were 5784 +/- 3718 and 140 938 +/- 128 783 ng."( Pharmacokinetic parameters of artesunate and dihydroartemisinin in rats infected with Fasciola hepatica.
Decosterd, L; Gruyer, MS; Keiser, J; Mercier, T; Perrottet, N; Zanolari, B, 2009
)
0.35
" For CCG and MADDS, small to moderate increases in exposure with artesunate dosing were observed."( Pharmacokinetics of chlorproguanil, dapsone, artesunate and their major metabolites in patients during treatment of acute uncomplicated Plasmodium falciparum malaria.
Bandyopadhyay, N; Duparc, S; Kirby, PL; Miller, AK; Ward, SA; Winstanley, PA; Wootton, DG, 2009
)
0.35
"A single-center, randomized, single-blind, cross-over clinical study was conducted in 18 healthy volunteers with a dosage of 300 mg daily for 2 days."( Comparative study of dihydroartemisinin and artesunate safety in healthy Thai volunteers.
Atipas, S; Chatsiricharoenkul, S; Kaewkungwal, J; Khuhapinant, A; Kongpatanakul, S, 2009
)
0.35
" However, children, compared to the population mean profile, tend to have a smaller central volume of distribution, a shorter distribution half-life and a more rapid fall in early piperaquine plasma concentrations, suggesting that an increase of the weight-adjusted dosage in children may be required."( Progress in the development of piperaquine combinations for the treatment of malaria.
D'alessandro, U, 2009
)
0.35
"The dosage recommended for children may need to be reviewed and the usefulness of the coadministration with food should be determined."( Progress in the development of piperaquine combinations for the treatment of malaria.
D'alessandro, U, 2009
)
0.35
"A novel parent-metabolite pharmacokinetic model consisting of a dosing compartment, a central compartment for AS, a central compartment and a peripheral compartment for DHA was developed."( Population pharmacokinetics of artesunate and dihydroartemisinin following single- and multiple-dosing of oral artesunate in healthy subjects.
Craft, JC; Fleckenstein, L; Jang, IJ; Kirsch, LE; Naik, H; Shin, CS; Tan, B; Yu, KS, 2009
)
0.35
" falciparum malaria in central Sudan, although treatment with DHA-P (which requires a simpler dosing regimen) might be preferred to treatment with AL."( Dihydroartemisinin-piperaquine versus artemether-lumefantrine, in the treatment of uncomplicated Plasmodium falciparum malaria in central Sudan.
Adam, I; Elhassan, AH; Elmardi, KA; Eltahir, HG; Malik, EM; Salah, MT, 2010
)
0.36
" These findings outline the relevance of DHA dosage and timing to prevent embryotoxicity and support current WHO recommendations of avoiding malaria treatment with artemisinins during the first trimester of pregnancy."( Selective toxicity of dihydroartemisinin on human CD34+ erythroid cell differentiation.
Cappellini, MD; Cattaneo, A; Colancecco, A; Finaurini, S; Ronzoni, L; Taramelli, D; Ward, SA, 2010
)
0.36
"Rats were dosed orally with chlorproguanil/dapsone/artesunate (including 11."( Localization of artesunate and its derivatives in the pregnant rat and fetus following oral administration and relationship to developmental toxicity.
Clark, RL; Gristwood, WE; Harrell, AW; Lewsley, R; Wilson, R, 2010
)
0.36
" It may also allow a reduction in dosage and a decrease in systemic toxicity."( Dihydroartemisinin loaded nanostructured lipid carriers (DHA-NLC): evaluation of pharmacokinetics and tissue distribution after intravenous administration to rats.
Dong, H; Liu, J; Ni, J; Qiao, H; Shen, C; Shi, Y; Xu, Y; Zhang, X, 2010
)
0.36
" CQ showed a delayed dose-response relationship in the murine malaria model and additive efficacy when combined with DHA."( Pharmacokinetics, pharmacodynamics, and allometric scaling of chloroquine in a murine malaria model.
Batty, KT; Ilett, KF; Jago, JD; Moore, BR; Page-Sharp, M; Stoney, JR, 2011
)
0.37
" The data are reassuring regarding current dosing recommendations."( Artesunate/dihydroartemisinin pharmacokinetics in acute falciparum malaria in pregnancy: absorption, bioavailability, disposition and disease effects.
Hanpithakpon, W; Hlaing, N; Lindegardh, N; McGready, R; Nosten, F; Phyo, AP; Rijken, MJ; Singhasivanon, P; Tarning, J; Than, HH; White, NJ; Zin, NT, 2012
)
0.38
" A three-day course of total 8 tablets compound dihydroartemisinin-piperaquine was administered to an adult (each tablet containing 40 mg of dihydroartemisinin and 320 mg of piperaquine phosphate), dosage for children was based on ages (details in the treatment regimen) ."( [Efficacy of compound dihydroartemisinin/piperaquine in treatment of uncomplicated falciparum malaria in Myanmar].
Li, CF; Liu, H; Nie, RH; Wang, HY; Yang, HL; Zhang, J, 2011
)
0.37
" In the three AL body weight dosing groups (5 to < 15 kg, 15 to < 25 kg and 25 to < 35 kg), 80% of patients were aged 10-50 months, 46-100 months and 90-147 months, respectively."( Similar efficacy and safety of artemether-lumefantrine (Coartem®) in African infants and children with uncomplicated falciparum malaria across different body weight ranges.
Bashraheil, M; Bassat, Q; González, R; Kipkeu, C; Lefèvre, G; Lyimo, J; Machevo, S; Maiga, H; Mårtensson, A; Menéndez, C; Nahum, A; Nwaiwu, O; Ogutu, B; Ouma, P; Ubben, D; Walter, V, 2011
)
0.37
"Efficacy of AL in uncomplicated falciparum malaria is similar across body weight dosing groups as currently recommended in the label with no clinically relevant differences in safety or tolerability."( Similar efficacy and safety of artemether-lumefantrine (Coartem®) in African infants and children with uncomplicated falciparum malaria across different body weight ranges.
Bashraheil, M; Bassat, Q; González, R; Kipkeu, C; Lefèvre, G; Lyimo, J; Machevo, S; Maiga, H; Mårtensson, A; Menéndez, C; Nahum, A; Nwaiwu, O; Ogutu, B; Ouma, P; Ubben, D; Walter, V, 2011
)
0.37
" However, the observed modest changes probably do not warrant dosage adjustment during co-administration of AL with EFV."( Concomitant efavirenz reduces pharmacokinetic exposure to the antimalarial drug artemether-lumefantrine in healthy volunteers.
Aweeka, FT; Dorsey, G; Havlir, D; Huang, L; Lizak, P; Marzan, F; Parikh, S; Rosenthal, PJ, 2012
)
0.38
"Mechanistic within-host models relating blood anti-malarial drug concentrations with the parasite-time profile help in assessing dosing schedules and partner drugs for new anti-malarial treatments."( Assessing the utility of an anti-malarial pharmacokinetic-pharmacodynamic model for aiding drug clinical development.
Charman, SA; Gamo-Benito, J; Humberstone, A; Jamsen, KM; McCaw, J; Moehrle, J; Price, RN; Simpson, JA; Smith, K; Zaloumis, S, 2012
)
0.38
" Declining plasma concentrations during the repeated dosing have been reported for QHS, artemether and less convincingly for artesunate (ARS)."( An investigation of the auto-induction of and gender-related variability in the pharmacokinetics of dihydroartemisinin in the rat.
Du, F; Li, X; Xing, J; Zhu, F, 2012
)
0.38
" The better safety profile of DP and once-daily dosage improves adherence and its fixed co-formulation ensures that both drugs are taken together."( Efficacy and safety of dihydroartemisinin-piperaquine for treatment of uncomplicated Plasmodium falciparum malaria in endemic countries: meta-analysis of randomised controlled studies.
Aung, K; Mak, JW; Naing, C; Wong, JY, 2013
)
0.39
" An adapted dosing regimen including a practical dosing table per weight band is proposed for young children based on the pharmacokinetic model."( Population pharmacokinetics of intramuscular artesunate in African children with severe malaria: implications for a practical dosing regimen.
Day, NP; Dondorp, AM; Gesase, S; Hendriksen, IC; Kent, A; Lemnge, MM; Lindegardh, N; Mtove, G; Reyburn, H; Tarning, J; von Seidlein, L; White, NJ, 2013
)
0.39
" Pre-clinical studies in dogs indicated morbidity at high dosage levels."( Safety and efficacy field study of artesunate for dogs with non-resectable tumours.
Efferth, T; Erich, SA; Fleckenstein, L; Grinwis, GC; London, CA; Mol, JA; Rutteman, GR; Spee, B, 2013
)
0.39
" More studies with appropriate control groups in larger series are needed to characterize the degree to which pregnant women are underdosed with current antimalarial dosing regimens."( Pharmacokinetic properties of artemether, dihydroartemisinin, lumefantrine, and quinine in pregnant women with uncomplicated plasmodium falciparum malaria in Uganda.
Dhorda, M; Guerin, PJ; Jullien, V; Kloprogge, F; Nosten, F; Piola, P; Tarning, J; White, NJ, 2013
)
0.39
"Dihydroartemisinin-piperaquine (DP) is increasingly recommended for antimalarial treatment in many endemic countries; however, concerns have been raised over its potential under dosing in young children."( The effect of dosing regimens on the antimalarial efficacy of dihydroartemisinin-piperaquine: a pooled analysis of individual patient data.
, 2013
)
0.39
" The better safety profile of DHP and the once-daily dosage improves adherence, and its fixed co-formulation ensures that both drugs (dihydroartemisinin and piperaquine) are taken together."( Efficacy and safety of dihydroartemisinin-piperaquine for treatment of Plasmodium vivax malaria in endemic countries: meta-analysis of randomized controlled studies.
Aung, K; Mak, JW; Naing, C; Racloz, V; Reid, SA; Tanner, M; Whittaker, MA, 2013
)
0.39
" The dosing schedule is simpler with the artenimol + piperaquine combination than with artemether + lumefantrine."( Artenimol + piperaquine. Very slow piperaquine elimination: cardiovascular risks and interactions.
, 2014
)
0.4
" However, the optimal drug and dosing regimens for IPT remain to be determined."( Impact of intermittent preventive treatment with dihydroartemisinin-piperaquine on malaria in Ugandan schoolchildren: a randomized, placebo-controlled trial.
Amuge, P; Brooker, SJ; Dorsey, G; Kamya, MR; Kiwanuka, N; Nankabirwa, JI; Rosenthal, PJ; Staedke, SG; Wandera, B, 2014
)
0.4
" The development of appropriate pragmatic dosing regimens for low-resource settings or community-based use is not formally regulated, even though these may alter factors which can substantially affect individual patient and population level outcome, such as drug exposure, patient adherence and the spread of drug resistance and can affect a drug's reputation and its eventual therapeutic lifespan."( Optimizing the programmatic deployment of the anti-malarials artemether-lumefantrine and dihydroartemisinin-piperaquine using pharmacological modelling.
Hastings, IM; Hayes, DJ; Hodel, EM; Kay, K; Terlouw, DJ, 2014
)
0.4
"An in silico pharmacological model of anti-malarial drug treatment with the pharmacokinetic/pharmacodynamic profiles of artemether-lumefantrine (AM-LF, Coartem®) and dihydroartemisinin-piperaquine (DHA-PPQ, Eurartesim®) was constructed to assess the potential impact of programmatic factors, including regionally optimized, age-based dosing regimens, poor patient adherence, food effects and drug resistance on treatment outcome at population level, and compared both drugs' susceptibility to these factors."( Optimizing the programmatic deployment of the anti-malarials artemether-lumefantrine and dihydroartemisinin-piperaquine using pharmacological modelling.
Hastings, IM; Hayes, DJ; Hodel, EM; Kay, K; Terlouw, DJ, 2014
)
0.4
"Compared with DHA-PPQ, therapeutic effectiveness of AM-LF seems more robust to factors affecting drug exposure, such as age- instead of weight-based dosing or poor adherence."( Optimizing the programmatic deployment of the anti-malarials artemether-lumefantrine and dihydroartemisinin-piperaquine using pharmacological modelling.
Hastings, IM; Hayes, DJ; Hodel, EM; Kay, K; Terlouw, DJ, 2014
)
0.4
"This study has developed mechanistic models that describe the parasite-time curve after single, multiple or combination dosing of antimalarials to mice."( Predicting the parasite killing effect of artemisinin combination therapy in a murine malaria model.
Batty, KT; Gibbons, PL; Kirkpatrick, CM; Moore, BR; Patel, K, 2014
)
0.4
" The cases were given a 2-day course with DHAPIP tablets each containing 40 mg of dihydroartemisinin and 320 mg of piperaquine phosphate, and the total dosage varied with the body weight."( [Therapeutic efficacy and safety of compound dihydroartemisinin/piperaquine for uncomplicated Plasmodium falciparum infection in Laiza City of Myanmar bordering on China].
Deng, Y; Lasi, JH; Sun, XD; Sun, XY; Wang, H; Wang, J; Yang, YC; Zhang, ZX, 2011
)
0.37
" The safety and efficacy of a monthly 2-day dosing regimen of dihydroartemisinin-piperaquine were evaluated in a two-arm, randomized, double-blind, placebo-controlled cohort study with 2:1 treatment allocation."( Randomized, double-blind, placebo-controlled clinical trial of a two-day regimen of dihydroartemisinin-piperaquine for malaria prevention halted for concern over prolonged corrected QT interval.
Auayporn, M; Buathong, N; Cantilena, L; Chann, S; Chour, CM; Haigney, M; Kaewkungwal, J; Kuntawunginn, W; Lanteri, C; Lon, C; Manning, J; Mitprasat, M; Phann, ST; Prom, S; Saunders, D; Se, Y; Sea, D; Siripokasupkul, R; So, M; Soh, E; Somethy, S; Spring, M; Sriwichai, S; Tang, D; Teja-Isavadharm, P; Timmermans, A; Vanachayangkul, P, 2014
)
0.4
" However, the optimal chemoprevention drug and dosing strategy is unclear in areas of year-round transmission and resistance to many antimalarial drugs."( Protective efficacy and safety of three antimalarial regimens for the prevention of malaria in young Ugandan children: a randomized controlled trial.
Achan, J; Aweeka, FT; Bigira, V; Clark, TD; Dorsey, G; Havlir, DV; Huang, L; Kamya, MR; Kapisi, J; Kinara, S; Muhindo, MK; Mwangwa, F; Osterbauer, B; Rosenthal, PJ, 2014
)
0.4
" This result relies on the assumption that compliance to treatment with DhP is higher than that with AL due to its relatively simple once-a-day dosage regimen."( Cost-effectiveness of dihydroartemisinin-piperaquine compared with artemether-lumefantrine for treating uncomplicated malaria in children at a district hospital in Tanzania.
Mori, AT; Ngalesoni, F; Norheim, OF; Robberstad, B, 2014
)
0.4
" Due to auto-induction metabolism, declining plasma concentrations after the repeated dosing have been reported for artemisinin (Qing-hao-su) and artemether."( The effect of UGTs polymorphism on the auto-induction phase II metabolism-mediated pharmacokinetics of dihydroartemisinin in healthy Chinese subjects after oral administration of a fixed combination of dihydroartemisinin-piperaquine.
Li, X; Liu, H; Xing, J; Yang, A; Zang, M; Zhao, L; Zhu, F, 2014
)
0.4
" The metabolic capability could recover after a 12-h dosing interval, which suggested that the alternative common three-day regimen (once daily) for DHA-PQ could probably lead to higher bioavailability of DHA."( The effect of UGTs polymorphism on the auto-induction phase II metabolism-mediated pharmacokinetics of dihydroartemisinin in healthy Chinese subjects after oral administration of a fixed combination of dihydroartemisinin-piperaquine.
Li, X; Liu, H; Xing, J; Yang, A; Zang, M; Zhao, L; Zhu, F, 2014
)
0.4
"Adherence to anti-malarial dosing schedules is essential to ensure effective treatment."( Perceptions and utilization of the anti-malarials artemether-lumefantrine and dihydroartemisinin-piperaquine in young children in the Chikhwawa District of Malawi: a mixed methods study.
Ewing, VL; Kapinda, A; Lalloo, DG; Pace, C; Richards, E; Terlouw, DJ; Tolhurst, R, 2015
)
0.42
" While the sweet taste of dispersible AL may have reduced conflict between the child and caregiver, sub-optimal dosing due to medication loss remained a problem and overall adherence was greater among those receiving DHA-PPQ, which requires fewer doses."( Perceptions and utilization of the anti-malarials artemether-lumefantrine and dihydroartemisinin-piperaquine in young children in the Chikhwawa District of Malawi: a mixed methods study.
Ewing, VL; Kapinda, A; Lalloo, DG; Pace, C; Richards, E; Terlouw, DJ; Tolhurst, R, 2015
)
0.42
" Current weight-based dosing does not adequately address physiological changes in early childhood."( Population Pharmacokinetics of Piperaquine in Young Ugandan Children Treated With Dihydroartemisinin-Piperaquine for Uncomplicated Malaria.
Arinaitwe, E; Aweeka, FT; Bigira, V; Creek, DJ; Kakuru, A; Lindegardh, N; McCormack, SA; Nosten, F; Parikh, S; Sambol, NC; Tappero, JW; Tarning, J; Wanzira, H; Yan, L, 2015
)
0.42
" Hence, dosing recommendations cannot be made in infants <5 kg as implications for toxicity are unknown."( Increased systemic exposures of artemether and dihydroartemisinin in infants under 5 kg with uncomplicated Plasmodium falciparum malaria treated with artemether-lumefantrine (Coartem®).
Alao, MJ; Cousin, M; Duparc, S; Hamed, K; Jain, JP; Lefèvre, G; Lingani, M; Meremikwu, M; Ogutu, B; Ouedraogo, A; Tinto, H; Tiono, AB; Tshefu, A, 2015
)
0.42
" In particular, the malaria community may be missing the opportunity to dramatically increase ACT effectiveness through regimen changes, particularly through a switch to twice-daily regimens and/or increases in artemisinin dosing levels."( How Robust Are Malaria Parasite Clearance Rates as Indicators of Drug Effectiveness and Resistance?
Hastings, IM; Hodel, EM; Kay, K, 2015
)
0.42
" Children were randomized at 6 months of age to no chemoprevention (n = 89) or monthly DHA/PQ (n = 87) and followed through 24 months of age, with pharmacokinetic sampling performed at variable times following monthly dosing of DHA/PQ."( Variable piperaquine exposure significantly impacts protective efficacy of monthly dihydroartemisinin-piperaquine for the prevention of malaria in Ugandan children.
Aweeka, F; Bigira, V; Dorsey, G; Huang, L; Jagannathan, P; Kakuru, MM; Kamya, MR; Kapisi, J; Savic, R; Sundell, K, 2015
)
0.42
" Strategies to ensure good adherence to monthly dosing and optimize drug exposure are critical to maximize the efficacy of this promising malaria control strategy."( Variable piperaquine exposure significantly impacts protective efficacy of monthly dihydroartemisinin-piperaquine for the prevention of malaria in Ugandan children.
Aweeka, F; Bigira, V; Dorsey, G; Huang, L; Jagannathan, P; Kakuru, MM; Kamya, MR; Kapisi, J; Savic, R; Sundell, K, 2015
)
0.42
" There were fewer concerns about treatment, mostly because of the simpler dosing regimen of the study drug (dihydroartemisinin-piperaquine) compared to the current first-line treatment (artemether-lumefantrine)."( Community perceptions of mass screening and treatment for malaria in Siaya County, western Kenya.
Allen, DR; Awino, N; Desai, M; Kariuki, S; Ouma, P; Samuels, A; Shuford, K; Were, F, 2016
)
0.43
" This therapeutic failure with DP by under-dosing highlighted the importance of appropriate dosing guidelines and the need of research data (efficacy, pharmacokinetics and pharmacodynamics) in over-weight patient group."( Failure of dihydroartemisinin plus piperaquine treatment of falciparum malaria by under-dosing in an overweight patient.
Javelle, E; Madamet, M; Paleiron, N; Pradines, B; Roseau, JB; Simon, F; Vedy, S, 2016
)
0.43
" This study explored alternative DHA-PQ adult dosing regimens compared to the monthly adult dosing regimen currently being studied in clinical trials."( Prediction of Improved Antimalarial Chemoprevention with Weekly Dosing of Dihydroartemisinin-Piperaquine.
Bergstrand, M; Karlsson, MO; Nosten, F; Permala, J; Tarning, J; White, NJ, 2017
)
0.46
"For HIV-infected pregnant women receiving efavirenz, low daily DHA-PQ dosing was predicted to improve protection against parasitemia and reduce risk of toxicity compared to monthly dosing."( Predicting Optimal Dihydroartemisinin-Piperaquine Regimens to Prevent Malaria During Pregnancy for Human Immunodeficiency Virus-Infected Women Receiving Efavirenz.
Aweeka, F; Dorsey, G; Havlir, D; Huang, L; Jagannathan, P; Kakuru, A; Kamya, M; Muhindo, M; Nakalembe, M; Natureeba, P; Rosenthal, PJ; Savic, RM; Vucicevic, K; Wallender, E, 2018
)
0.48
" Determining associations between piperaquine (PQ) exposure, malaria risk, and adverse birth outcomes informs optimal dosing strategies."( Intermittent Preventive Treatment for Malaria in Pregnancy: Optimization of Target Concentrations of Dihydroartemisinin-Piperaquine.
Aweeka, FT; Clark, TD; Dorsey, G; Havlir, DV; Huang, L; Jagannathan, P; Kajubi, R; Kakuru, A; Kamya, M; Muhindo, MK; Mwebaza, N; Opira, B; Rosenthal, PJ; Savic, RM; Wallender, E; Were, M; Zhang, N, 2018
)
0.48
" Simulations of new dosing scenarios were performed."( Intermittent Preventive Treatment for Malaria in Pregnancy: Optimization of Target Concentrations of Dihydroartemisinin-Piperaquine.
Aweeka, FT; Clark, TD; Dorsey, G; Havlir, DV; Huang, L; Jagannathan, P; Kajubi, R; Kakuru, A; Kamya, M; Muhindo, MK; Mwebaza, N; Opira, B; Rosenthal, PJ; Savic, RM; Wallender, E; Were, M; Zhang, N, 2018
)
0.48
" Studies of the efficacy and safety of alternative DHA-PQ IPTp dosing strategies are warranted."( Intermittent Preventive Treatment for Malaria in Pregnancy: Optimization of Target Concentrations of Dihydroartemisinin-Piperaquine.
Aweeka, FT; Clark, TD; Dorsey, G; Havlir, DV; Huang, L; Jagannathan, P; Kajubi, R; Kakuru, A; Kamya, M; Muhindo, MK; Mwebaza, N; Opira, B; Rosenthal, PJ; Savic, RM; Wallender, E; Were, M; Zhang, N, 2018
)
0.48
" All treatments were once-daily or twice-daily tablets or granules given orally and dosed by bodyweight over 3 days at the study centre."( Pyronaridine-artesunate or dihydroartemisinin-piperaquine versus current first-line therapies for repeated treatment of uncomplicated malaria: a randomised, multicentre, open-label, longitudinal, controlled, phase 3b/4 trial.
, 2018
)
0.48
" We provide published data supporting the use of a higher dosage regimen of ivermectin in malaria and difficult-to-treat head lice, and announce an ongoing randomized clinical trial in severe scabies."( High-dose ivermectin in malaria and other parasitic diseases: a new step in the development of a neglected drug.
Bernigaud, C; Chosidow, O; Do-Pham, G, 2018
)
0.48
"Nous soulignons l’absence de données probantes de haut niveau sur les études de dosage concernant l’utilisation de l’ivermectine par voie orale dans les maladies parasitaires sensibles."( High-dose ivermectin in malaria and other parasitic diseases: a new step in the development of a neglected drug.
Bernigaud, C; Chosidow, O; Do-Pham, G, 2018
)
0.48
" Future studies are needed to better understand the biological mechanisms of in utero drug exposure on drug metabolism and how this may affect the dosing of antimalarial drugs for treatment and prevention during infancy."( Dihydroartemisinin-piperaquine for intermittent preventive treatment of malaria during pregnancy and risk of malaria in early childhood: A randomized controlled trial.
Aweeka, F; Beeson, J; Charlebois, ED; Clark, TD; Dorsey, G; Drakeley, C; Feeney, ME; Greenhouse, B; Havlir, DV; Jagannathan, P; Kakuru, A; Kamya, MR; Muhindo, MK; Nakalembe, M; Nankya, F; Natureeba, P; Okiring, J; Olwoch, P; Opira, B; Prahl, M; Reiling, L; Rodriguez-Barraquer, I; Ssewanyana, I; Tetteh, K; Wallender, E, 2018
)
0.48
" falciparum intraerythrocytic stage were observed, and then the 3D7 life cycle and effects of different developmental stages after dosing was explored."( [Effect of dihydroartemisinin at low concentration on intervention of Plasmodium falciparum 3D7 strain].
Chen, LN; Guo, Y; Jiang, XH; Li, K; Li, YJ; Yang, T; Zheng, XJ; Zheng, ZY, 2018
)
0.48
" The favourable biodistribution and tumour uptake of NCPs and the absence of peripheral neuropathy allow for repeated dosing to afford 100% tumour eradication."( Immunostimulatory nanomedicines synergize with checkpoint blockade immunotherapy to eradicate colorectal tumors.
Chan, C; Duan, X; Guo, N; Han, W; Lin, W; Weichselbaum, RR, 2019
)
0.51
"Dihydroartemisinin (DHA)-piperaquine is being evaluated as intermittent preventive therapy for malaria, but dosing has not been optimized for children."( Reduced Exposure to Piperaquine, Compared to Adults, in Young Children Receiving Dihydroartemisinin-Piperaquine as Malaria Chemoprevention.
Aweeka, FT; Chamankhah, N; Dorsey, G; Huang, L; Jagannathan, P; Kajubi, R; Kamya, MR; Mwebaza, N; Orukan, F; Rosenthal, PJ; Wallender, E; Whalen, ME, 2019
)
0.51
" However, the optimal dosing strategy is unclear and conflicting evidence exists regarding the risk of malaria after cessation of chemoprevention."( Intermittent preventive treatment with dihydroartemisinin-piperaquine and risk of malaria following cessation in young Ugandan children: a double-blind, randomised, controlled trial.
Charlebois, E; Clark, TD; Dorsey, G; Feeney, ME; Havlir, DV; Jagannathan, P; Kakuru, A; Kamya, MR; Muhindo, MK; Nalugo, N; Okiring, J; Olwoch, P; Opira, B; Ruel, T, 2019
)
0.51
"Considering the low day 7 concentrations of piperaquine reported in the patients studied here, we suggest to adopt the recently recommended higher dose of DP in young children or a prolonged 5-day dosing in children living in malaria endemic areas who have suffered an initial episode of severe malaria in order to achieve adequate drug exposures for effective post-treatment prophylactic effects."( Piperaquine concentration and malaria treatment outcomes in Ugandan children treated for severe malaria with intravenous Artesunate or quinine plus Dihydroartemisinin-Piperaquine.
Blessborn, D; Byakika-Kibwika, P; Lamorde, M; Ssenyonga, R; Tarning, J, 2019
)
0.51
" These data suggest that malaria and HIV coinfected pregnant women may require adjustments in AL dosage or treatment duration to achieve exposure comparable with HIV-uninfected pregnant women."( Efavirenz-Based Antiretroviral Therapy Reduces Artemether-Lumefantrine Exposure for Malaria Treatment in HIV-Infected Pregnant Women.
Aweeka, F; Huang, L; Hughes, E; Kajubi, R; Mwebaza, N; Mwima, MW; Nguyen, V; Nyunt, MM; Orukan, F; Parikh, S, 2020
)
0.56
"Findings will provide timely information on the safety, efficacy, and optimal dosing of t-PA to treat moderate/severe COVID-19-induced ARDS, which can be rapidly adapted to a phase III trial (NCT04357730; FDA IND 149634)."(
Abbasi, S; Abd El-Wahab, A; Abdallah, M; Abebe, G; Aca-Aca, G; Adama, S; Adefegha, SA; Adidigue-Ndiome, R; Adiseshaiah, P; Adrario, E; Aghajanian, C; Agnese, W; Ahmad, A; Ahmad, I; Ahmed, MFE; Akcay, OF; Akinmoladun, AC; Akutagawa, T; Alakavuklar, MA; Álava-Rabasa, S; Albaladejo-Florín, MJ; Alexandra, AJE; Alfawares, R; Alferiev, IS; Alghamdi, HS; Ali, I; Allard, B; Allen, JD; Almada, E; Alobaid, A; Alonso, GL; Alqahtani, YS; Alqarawi, W; Alsaleh, H; Alyami, BA; Amaral, BPD; Amaro, JT; Amin, SAW; Amodio, E; Amoo, ZA; Andia Biraro, I; Angiolella, L; Anheyer, D; Anlay, DZ; Annex, BH; Antonio-Aguirre, B; Apple, S; Arbuznikov, AV; Arinsoy, T; Armstrong, DK; Ash, S; Aslam, M; Asrie, F; Astur, DC; Atzrodt, J; Au, DW; Aucoin, M; Auerbach, EJ; Azarian, S; Ba, D; Bai, Z; Baisch, PRM; Balkissou, AD; Baltzopoulos, V; Banaszewski, M; Banerjee, S; Bao, Y; Baradwan, A; Barandika, JF; Barger, PM; Barion, MRL; Barrett, CD; Basudan, AM; Baur, LE; Baz-Rodríguez, SA; Beamer, P; Beaulant, A; Becker, DF; Beckers, C; 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Yamamoto, S; Yan, D; Yan, H; Yan, S; Yan, X; Yang, AD; Yang, E; Yang, H; Yang, J; Yang, JL; Yang, K; Yang, M; Yang, P; Yang, Q; Yang, S; Yang, W; Yang, X; Yang, Y; Yao, JC; Yao, WL; Yao, Y; Yaqub, TB; Ye, J; Ye, W; Yen, CW; Yeter, HH; Yin, C; Yip, V; Yong-Yi, J; Yu, HJ; Yu, MF; Yu, S; Yu, W; Yu, WW; Yu, X; Yuan, P; Yuan, Q; Yue, XY; Zaia, AA; Zakhary, SY; Zalwango, F; Zamalloa, A; Zamparo, P; Zampini, IC; Zani, JL; Zeitoun, R; Zeng, N; Zenteno, JC; Zepeda-Palacio, C; Zhai, C; Zhang, B; Zhang, G; Zhang, J; Zhang, K; Zhang, Q; Zhang, R; Zhang, T; Zhang, X; Zhang, Y; Zhang, YY; Zhao, B; Zhao, D; Zhao, G; Zhao, H; Zhao, Q; Zhao, R; Zhao, S; Zhao, T; Zhao, X; Zhao, XA; Zhao, Y; Zhao, Z; Zheng, Z; Zhi-Min, G; Zhou, CL; Zhou, HD; Zhou, J; Zhou, W; Zhou, XQ; Zhou, Z; Zhu, C; Zhu, H; Zhu, L; Zhu, Y; Zitzmann, N; Zou, L; Zou, Y, 2022
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0.72
" It is expected that such a tool will be useful in characterizing the disposition of these chemicals and ultimately improve dosing regimens by enabling a quantitative assessment of the tissue-specific drug levels critical in the evaluation of efficacy and toxicity."( Predicting the Disposition of the Antimalarial Drug Artesunate and Its Active Metabolite Dihydroartemisinin Using Physiologically Based Pharmacokinetic Modeling.
Arey, R; Reisfeld, B, 2021
)
0.62
" Participants in the intermittent preventive malaria treatment arm will receive dihydroartemisinin/piperaquine (DP) dosed by weight, 1 month apart, prior to the first immunisation, followed by monthly treatment thereafter."( Effect of intermittent preventive treatment for malaria with dihydroartemisinin-piperaquine on immune responses to vaccines among rural Ugandan adolescents: randomised controlled trial protocol B for the '
Akello, F; Amongi, S; Amongin, R; Cose, S; Elliott, AM; Kabuubi, PN; Kiwanuka, S; Kiwudhu, F; Kizindo, R; Mutebe, A; Nakazibwe, E; Nassuuna, J; Natukunda, A; Nkurunungi, G; Nsubuga, D; Oduru, G; Onen, C; Sewankambo, M; Staedke, SG; Webb, E; Zirimenya, L, 2021
)
0.62
" Additionally, these models are able to identify patient characteristics that cause alterations in the expected PK/PD profiles and through simulations can recommend changes to dosing which compensate for the differences."( Malaria PK/PD and the Role Pharmacometrics Can Play in the Global Health Arena: Malaria Treatment Regimens for Vulnerable Populations.
Hughes, E; Jagannathan, P; Mohamed Ali, A; Savic, RM; Wallender, E, 2021
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" Optimal DP dosing regimens will maximize efficacy and reduce toxicity and resistance selection."( Identifying an optimal dihydroartemisinin-piperaquine dosing regimen for malaria prevention in young Ugandan children.
Ali, AM; Aweeka, F; Dorsey, G; Duvalsaint, M; Huang, L; Hughes, E; Jagannathan, P; Kakuru, A; Kamya, MR; Legac, J; Muhindo, MK; Opira, B; Rosenthal, PJ; Savic, RM; Wallender, E; Whalen, M, 2021
)
0.62
" Piperaquine prolongs the corrected QT interval (QTc), and it is possible that repeated monthly dosing could lead to progressive QTc prolongation."( Piperaquine-Induced QTc Prolongation Decreases With Repeated Monthly Dihydroartemisinin-Piperaquine Dosing in Pregnant Ugandan Women.
Aweeka, F; Clark, TD; Dorsey, G; Hughes, E; Jagannathan, P; Kajubi, R; Kakuru, A; Kamya, MR; Ochieng, T; Rosenthal, PJ; Savic, RM; Wallender, E, 2022
)
0.72
"Repeated DHA-PQ dosing did not result in increased risk of QTc prolongation and the postdose QTc intervals progressively decreased."( Piperaquine-Induced QTc Prolongation Decreases With Repeated Monthly Dihydroartemisinin-Piperaquine Dosing in Pregnant Ugandan Women.
Aweeka, F; Clark, TD; Dorsey, G; Hughes, E; Jagannathan, P; Kajubi, R; Kakuru, A; Kamya, MR; Ochieng, T; Rosenthal, PJ; Savic, RM; Wallender, E, 2022
)
0.72
" Participants were randomly assigned (1:1:1:1) to standard treatment with dihydroartemisinin-piperaquine, or dihydroartemisinin-piperaquine plus a single dose of tafenoquine (in solution) at a final dosage of 0·42 mg/kg, 0·83 mg/kg, or 1·66 mg/kg."( Single low-dose tafenoquine combined with dihydroartemisinin-piperaquine to reduce Plasmodium falciparum transmission in Ouelessebougou, Mali: a phase 2, single-blind, randomised clinical trial.
Attaher, O; Bousema, T; Bradley, J; Diallo, M; Dicko, A; Dicko, OM; Drakeley, C; Issiaka, D; Keita, S; Lanke, K; Maguiraga, SO; Mahamar, A; McCall, MBB; Niambele, SM; Sacko, A; Samake, S; Sanogo, K; Sinaba, Y; Smit, MJ; Stone, W; Ter Heine, R; Traore, SF, 2022
)
0.72
" Participants were randomly assigned (1:1) to receive single low-dose primaquine combined with either artemether-lumefantrine or dihydroartemisinin-piperaquine, dosed by bodyweight."( Safety of age-dosed, single low-dose primaquine in children with glucose-6-phosphate dehydrogenase deficiency who are infected with Plasmodium falciparum in Uganda and the Democratic Republic of the Congo: a randomised, double-blind, placebo-controlled, n
Abongo, G; Basara, BB; Baseke, J; Bongo, GS; Day, NJP; Dhorda, M; Dondorp, AM; Fanello, C; Kayembe, DK; Maitland, K; Muhindo, R; Mukaka, M; Namayanja, C; Ndjowo, PO; Okalebo, CB; Olupot-Olupot, P; Onyamboko, MA; Onyas, P; Peerawaranun, P; Tarning, J; Taya, C; Taylor, WR; Titin, H; Uyoga, S; Waithira, N; Weere, W; Williams, TN, 2023
)
0.91
" Better dosing regimens are needed to optimize malaria prevention in malnourished populations, but, importantly, malaria chemoprevention may reduce the burden of malnutrition in early childhood."( Interplay among malnutrition, chemoprevention, and the risk of malaria in young Ugandan children: Longitudinal pharmacodynamic and growth analysis.
Ali, AM; Dorsey, G; Hughes, E; Savic, RM; Wallender, E, 2023
)
0.91
" We will also assess toxicity from cumulative DP dosing and the development of resistance."( Dihydroartemisinin-piperaquine or sulphadoxine-pyrimethamine for the chemoprevention of malaria in children with sickle cell anaemia in eastern and southern Africa (CHEMCHA): a protocol for a multi-centre, two-arm, double-blind, randomised, placebo-contro
Akun, P; Galileya, LT; Idro, R; Kalibbala, D; Nambatya, W; Nkosi-Gondwe, T; Opoka, R; Phiri, K; Robberstad, B; Rujumba, J; Ssenkusu, J; TerKuile, F, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
artemisinin derivativeAny organic peroxide formally obtained from artemisinin.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)125.00000.00011.753610.0000AID1212138
Cytochrome P450 2B6Homo sapiens (human)IC50 (µMol)125.00000.00113.418610.0000AID1212134
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (21)

Processvia Protein(s)Taxonomy
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2B6Homo sapiens (human)
steroid metabolic processCytochrome P450 2B6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2B6Homo sapiens (human)
cellular ketone metabolic processCytochrome P450 2B6Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2B6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (27)

Processvia Protein(s)Taxonomy
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2B6Homo sapiens (human)
iron ion bindingCytochrome P450 2B6Homo sapiens (human)
testosterone 16-alpha-hydroxylase activityCytochrome P450 2B6Homo sapiens (human)
heme bindingCytochrome P450 2B6Homo sapiens (human)
testosterone 16-beta-hydroxylase activityCytochrome P450 2B6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2B6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2B6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2B6Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 2B6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2B6Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2B6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (3)

Processvia Protein(s)Taxonomy
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2B6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2B6Homo sapiens (human)
cytoplasmCytochrome P450 2B6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (807)

Assay IDTitleYearJournalArticle
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1609530Antiproliferative activity against human HCT116 cells assessed as inhibition of cell viability after 48 hrs by MTS assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Design and synthesis of novel artemisinin derivatives with potent activities against colorectal cancer in vitro and in vivo.
AID1733061Cytotoxicity against human SMMC-7721 cells assessed as cell viability after 24 hrs by MTT assay2021European journal of medicinal chemistry, Apr-05, Volume: 215Synthesis of artemisinin-piperazine-furan ether hybrids and evaluation of in vitro cytotoxic activity.
AID1609531Antiproliferative activity against human WM266.4 cells assessed as inhibition of cell viability after 48 hrs by MTS assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Design and synthesis of novel artemisinin derivatives with potent activities against colorectal cancer in vitro and in vivo.
AID1609535Antitumour activity against human HCT116 cells xenografted in BALB/c nude mouse assessed as reduction in tumour growth at 10 mg/kg, ip administered daily for 18 days started from 2 days after tumor cell inoculation by digital caliper method2019European journal of medicinal chemistry, Nov-15, Volume: 182Design and synthesis of novel artemisinin derivatives with potent activities against colorectal cancer in vitro and in vivo.
AID1733062Cytotoxicity against human L02 cells assessed as cell viability after 24 hrs by MTT assay2021European journal of medicinal chemistry, Apr-05, Volume: 215Synthesis of artemisinin-piperazine-furan ether hybrids and evaluation of in vitro cytotoxic activity.
AID1655967Inhibition of human TOP1B expressed in Saccharomyces cerevisiae EKY3 lacking top1 assessed as reduction in yeast cell growth at 30 uM2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Artemisinin Derivatives with Antimelanoma Activity Show Inhibitory Effect against Human DNA Topoisomerase 1.
AID1401025Antiproliferative activity against human NB4 cells after 96 hrs by MTT assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis, anticancer evaluation and pharmacokinetic study of novel 10-O-phenyl ethers of dihydroartemisinin.
AID1648007Cytotoxicity against HEK293 cells assessed as growth inhibition at 20 uM relative to control2020Journal of natural products, 02-28, Volume: 83, Issue:2
A Meroisoprenoid, Heptenolides, and
AID1326706Cytotoxicity against human HL60 cells assessed as cell growth inhibition at 10 uM after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1441235Antimalarial activity against quinine-resistant asexual blood stage Plasmodium falciparum 3D7 after 72 hrs by SYBR green-based fluorometric analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Target Elucidation by Cocrystal Structures of NADH-Ubiquinone Oxidoreductase of Plasmodium falciparum (PfNDH2) with Small Molecule To Eliminate Drug-Resistant Malaria.
AID1326702Cytotoxicity against human LS180 cells assessed as cell growth inhibition at 30 uM after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1272409Activity at MDR1 (unknown origin) expressed in MDCK cells assessed as permeability across apical to basolateral after 90 mins by LC-MS/MS analysis2016European journal of medicinal chemistry, Jan-27, Volume: 108Combating P-glycoprotein-mediated multidrug resistance with 10-O-phenyl dihydroartemisinin ethers in MCF-7 cells.
AID1888544Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as food intake at 150 mg/kg, ig for 4 weeks2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1357959Cytotoxicity against human HT-29 cells after 96 hrs under normoxic condition by MTT assay
AID1777162Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 incubated for 72 hrs by spectrophotometry based parasite lactate dehydrogenase assay2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Enantioselective Synthesis and Profiling of Potent, Nonlinear Analogues of Antimalarial Tetraoxanes E209 and N205.
AID1327394Selectivity index, ratio of IC50 for human WI38 cells to IC50 for chloroquine-sensitive asexual erythrocyte stage form Plasmodium falciparum NF542016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin.
AID1888546Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as decrease in TC concentration in serum at 150 mg/kg, ig for 4 weeks2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1782711Antimalarial activity against Plasmodium falciparum 3D7 assessed as parasite growth inhibition incubated for 48 hrs by SYBR green DNA fluorescent dye-binding assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Combating multi-drug resistant malaria parasite by inhibiting falcipain-2 and heme-polymerization: Artemisinin-peptidyl vinyl phosphonate hybrid molecules as new antimalarials.
AID1708863Antiplasmodial activity against Plasmodium falciparum GB4 infected in human erythrocytes assessed as reduction in parasite growth incubated for 72 hrs by Giemsa staining based light microscopic method2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Discovery of Novel
AID1545819Antiproliferative activity against human HL60 cells by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1326716Cytotoxicity against human PC3 cells assessed as cell growth inhibition after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1326747Induction of apoptosis in human HL60 cells assessed as loss of mitochondrial membrane potential at 5 uM after 24 hrs by Rh123 dye-based FACS analysis (Rvb = 5%)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1272411Permeability across apical to basolateral side in MDCK cells after 90 mins by LC-MS/MS analysis2016European journal of medicinal chemistry, Jan-27, Volume: 108Combating P-glycoprotein-mediated multidrug resistance with 10-O-phenyl dihydroartemisinin ethers in MCF-7 cells.
AID1437506Selectivity index, ratio of growth inhibitory effect against HEK293 cells at 20 uM to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 infected in human RBC
AID1326722Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for human HepG2 cells2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1888558Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as increase in Cyp7b1 mRNA expression in liver in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1825877Antimalarial activity against asexual blood stage quinine-resistant Plasmodium falcipuram C2A assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green I staining based fluorescence analysis
AID1274586Cytotoxicity against HEK293 cells assessed as cell viability at 40 uM after 72 hrs by resazurin-based plate reader analysis2015Journal of natural products, Dec-24, Volume: 78, Issue:12
Rotenoids, Flavonoids, and Chalcones from the Root Bark of Millettia usaramensis.
AID1888552Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as AST level in serum at 150 mg/kg, ig for 4 weeks2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1674381Antimalarial activity against Plasmodium falcipuram K1 by microculture radioistope technique2020Journal of natural products, 07-24, Volume: 83, Issue:7
Highly Modified Lanostane Triterpenes from the Wood-Rot Basidiomycete
AID1812439Inhibition of human HDAC using human HeLa cell nuclear extract measured after 60 mins by fluorescence assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1272408Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay2016European journal of medicinal chemistry, Jan-27, Volume: 108Combating P-glycoprotein-mediated multidrug resistance with 10-O-phenyl dihydroartemisinin ethers in MCF-7 cells.
AID1779235Selectivity index, ratio of IC50 for antimalarial activity against Plasmodium falciparum Dd2 to IC50 of antimalarial activity against Plasmodium falciparum 3D72021European journal of medicinal chemistry, Oct-05, Volume: 221Discovery and development of 2-aminobenzimidazoles as potent antimalarials.
AID1546485Induction of apoptosis in human PC14 cells assessed as increase in apoptotic cells at 30 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometric analysis relative to control2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Artemisia: a promising plant for the treatment of cancer.
AID1395097Antiproliferative activity against human A375 cells after 72 hrs by CCK-8 assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Synthesis of novel ring-contracted artemisinin dimers with potent anticancer activities.
AID1545824Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 24 hrs by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1441258Antimalarial activity against Plasmodium yoelii YM infected in BALB/c mouse assessed as parasite growth inhibition at 90 mg/kg, sc administered BID for 4 days starting at 96 hrs post infection, 8 hrs apart by Giemsa-staining based microscopic analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Target Elucidation by Cocrystal Structures of NADH-Ubiquinone Oxidoreductase of Plasmodium falciparum (PfNDH2) with Small Molecule To Eliminate Drug-Resistant Malaria.
AID1326731Cell cycle arrest in human HL60 cells assessed as accumulation at G2 phase at 0.2 uM after 24 hrs by propidium iodide-DNA fluorescence based FACS analysis (Rvb = 1 %)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1888543Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as body weight at 150 mg/kg, ig for 4 weeks2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1272414Efflux ratio of permeability across basolateral to apical side over apical to basolateral side in MDCK cells2016European journal of medicinal chemistry, Jan-27, Volume: 108Combating P-glycoprotein-mediated multidrug resistance with 10-O-phenyl dihydroartemisinin ethers in MCF-7 cells.
AID1326721Cytotoxicity against human HepG2 cells assessed as cell growth inhibition after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1888573Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as increase in Scd1 mRNA expression in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1326735Cell cycle arrest in human HL60 cells assessed as accumulation at G2 phase at 0.5 uM after 24 hrs by propidium iodide-DNA fluorescence based FACS analysis (Rvb = 1 %)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1708858Antiplasmodial activity against synchronized ring stage Plasmodium falciparum Dd2 infected in human erythrocytes assessed as reduction in parasite growth incubated for 72 hrs by Giemsa staining based light microscopic method2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Discovery of Novel
AID1810292Antimalarial activity against chloroquine, pyrimethamine, mefloquine and atovaquone- resistant Plasmodium falciparum TM90-C2B infected in human erythrocytes assessed as reduction in parasite growth incubated for 48 hrs followed by addition of [3H]-hypoxan2021Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
Aminoalkoxycarbonyloxymethyl Ether Prodrugs with a pH-Triggered Release Mechanism: A Case Study Improving the Solubility, Bioavailability, and Efficacy of Antimalarial 4(1
AID1853165Selectivity index, ratio of IC50 for Antimalarial activity against chloroquine sensitive Plasmodium falciparum 3D7 infected in human RBC to IC50 for Cytotoxicity against human HepG2 cells2022RSC medicinal chemistry, Dec-14, Volume: 13, Issue:12
Preparation, biological evaluation and QSAR analysis of urea substituted 2,4-diamino-pyrimidine anti-malarials.
AID1326696Cytotoxicity against human MIAPaCa2 cells assessed as cell growth inhibition at 30 uM after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1395044Inhibition of PDE1 (unknown origin) using [3H]cAMP or [3H]cGMP as substrate liquid scintillation counting method2018European journal of medicinal chemistry, Apr-25, Volume: 150Inhibitors of phosphodiesterase as cancer therapeutics.
AID1401029Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis, anticancer evaluation and pharmacokinetic study of novel 10-O-phenyl ethers of dihydroartemisinin.
AID1825879Antimalarial activity against asexual blood stage wild-type Plasmodium falciparum 3D7 assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green I staining based fluorescence analysis
AID1326713Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for human MIAPaCa2 cells2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1545821Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 24 hrs by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1441256Antimalarial activity against Plasmodium yoelii YM infected in BALB/c mouse assessed as time duration for parasite cure at 30 mg/kg, sc administered BID for 4 days starting at 96 hrs post infection, 8 hrs apart by Giemsa-staining based microscopic analysi2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Target Elucidation by Cocrystal Structures of NADH-Ubiquinone Oxidoreductase of Plasmodium falciparum (PfNDH2) with Small Molecule To Eliminate Drug-Resistant Malaria.
AID1326708Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for human HL60 cells2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1727378Parasiticidal activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in erythrocytes assessed as reduction in parasitemia at 50 nM incubated for 24 to 48 hrs followed by compound washout and then incubated for 96 hrs by Giemsa staining 2021European journal of medicinal chemistry, Jan-01, Volume: 209Discovery of fast-acting dual-stage antimalarial agents by profiling pyridylvinylquinoline chemical space via copper catalyzed azide-alkyne cycloadditions.
AID1770979Anticancer activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 reagent assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Study on the structure-activity relationship of dihydroartemisinin derivatives: Discovery, synthesis, and biological evaluation of dihydroartemisinin-bile acid conjugates as potential anticancer agents.
AID1676920Antiplasmodial activity against synchronous gametocyte early stage of Plasmodium falciparum 3D7 harboring luc7 incubated for 72 hrs by ONE-Glo luciferase assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Synthesis, Structure-Activity Relationship, and Antimalarial Efficacy of 6-Chloro-2-arylvinylquinolines.
AID1326704Cytotoxicity against human HL60 cells assessed as cell growth inhibition at 0.5 uM after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1676941Antiplasmodial activity against synchronized chloroquine-resistant Plasmodium falciparum Dd2 reduction in microbial growth at 50 nM treated with compound at 42 hrs post infection measured after 12 hrs by Giemsa staining-based microscopic analysis2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Synthesis, Structure-Activity Relationship, and Antimalarial Efficacy of 6-Chloro-2-arylvinylquinolines.
AID1274588Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis2015Journal of natural products, Dec-24, Volume: 78, Issue:12
Rotenoids, Flavonoids, and Chalcones from the Root Bark of Millettia usaramensis.
AID1326703Cytotoxicity against human LS180 cells assessed as cell growth inhibition at 50 uM after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1573775Antiviral activity against recombinant HCMV AD169 expressing GFP infected in human foreskin fibroblasts measured after 7 days by GFP-based multi-round replication assay2019Bioorganic & medicinal chemistry, 01-01, Volume: 27, Issue:1
Synthesis of new betulinic acid/betulin-derived dimers and hybrids with potent antimalarial and antiviral activities.
AID1354680Antiplasmodial activity against Plasmodium falciparum NF542018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Plasmodial Kinase Inhibitors: License to Cure?
AID1497085Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13
Design, synthesis and biological evaluation of artemisinin derivatives containing fluorine atoms as anticancer agents.
AID1708866Antiplasmodial activity against artemisinin-resistant Plasmodium falciparum 6218 infected in human erythrocytes assessed as reduction in parasite growth incubated for 72 hrs by Giemsa staining based light microscopic method2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Discovery of Novel
AID1708860Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Discovery of Novel
AID1326694Cytotoxicity against human HL60 cells assessed as cell growth inhibition at 50 uM after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1772149Antimalarial activity against Plasmodium falciparum K1 assessed as inhibition of parasite growth by microculture radioisotope technique2021Journal of natural products, 11-26, Volume: 84, Issue:11
Antimicrobial and Cytotoxic Angucyclic Quinones from
AID1271049Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Synthesis and in vitro antitumor evaluation of dihydroartemisinin-cinnamic acid ester derivatives.
AID1888571Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as increase in Fasn mRNA expression in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1489613Antimalarial activity against mefloquine/chloroquine/atovaquone/pyrimethamine-resistant Plasmodium falciparum TM90-C2B infected in human type A-positive erythrocytes after 48 hrs by [3H]-hypoxanthine incorporation assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design and Synthesis of Orally Bioavailable Piperazine Substituted 4(1H)-Quinolones with Potent Antimalarial Activity: Structure-Activity and Structure-Property Relationship Studies.
AID1699653Selectivity index, ratio of IC50 for cytotoxicity against human HEK293 cells to IC50 for antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 ring stage2020Journal of natural products, 11-25, Volume: 83, Issue:11
Antiplasmodial Alkaloids from the Australian Bryozoan
AID1457810Antiplasmodial activity against Plasmodium falciparum Cam3.2 infected in human RBC assessed as time required to reduce early ring stage parasite viability by 50% by SYTO 61-staining-based flow cytometry2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID1890799Inhibition of Th17 cells differentiation in C57BL/6 mouse spleen CD4+ve Th cells assessed as decrease in IL-17A production at 10 uM measured after 4 days by flow cytometry analysis
AID1437499Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in human RBC after 72 hrs by DAPI staining based confocal microscopic method
AID1888578Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as decrease in Srebf1 mRNA expression in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1327390Antiplasmodial activity against chloroquine-resistant asexual erythrocyte stage form Plasmodium falciparum Dd2 measured after 48 hrs by pLDH assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin.
AID1888568Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as decrease in Slc10a2 mRNA expression in Ileum at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1708864Antiplasmodial activity against Plasmodium falciparum C2A infected in human erythrocytes assessed as reduction in parasite growth incubated for 72 hrs by Giemsa staining based light microscopic method2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Discovery of Novel
AID1612608Antimalarial activity against ring-stage multidrug-resistant Plasmodium falciparum Dd2 preincubated for 6 hrs followed by compound wash and measured after 66 hrs by Giemsa-staining based light microscopic analysis2019European journal of medicinal chemistry, Feb-01, Volume: 163Recent advances of tetrazole derivatives as potential anti-tubercular and anti-malarial agents.
AID1699650Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 ring stage incubated for 72 hrs by DAPI-staining based imaging analysis2020Journal of natural products, 11-25, Volume: 83, Issue:11
Antiplasmodial Alkaloids from the Australian Bryozoan
AID1888566Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as increase in Abcb4 mRNA expression in liver in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1498473Antiviral activity against GFP-fused Human cytomegalovirus AD169 infected in primary HFF2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Access to new highly potent antileukemia, antiviral and antimalarial agents via hybridization of natural products (homo)egonol, thymoquinone and artemisinin.
AID1271051Selectivity index, ratio of IC50 for human L02 cells to IC50 for human A549 cells2016European journal of medicinal chemistry, Jan-01, Volume: 107Synthesis and in vitro antitumor evaluation of dihydroartemisinin-cinnamic acid ester derivatives.
AID1810291Antimalarial activity against chloroquine and pyrimethamine resistant Plasmodium falciparum W2 infected in human erythrocytes assessed as reduction in parasite growth incubated for 48 hrs followed by addition of [3H]-hypoxanthine and measured after 24 hrs2021Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
Aminoalkoxycarbonyloxymethyl Ether Prodrugs with a pH-Triggered Release Mechanism: A Case Study Improving the Solubility, Bioavailability, and Efficacy of Antimalarial 4(1
AID1639284Antiplasmodial activity against drug-resistant Plasmodium falciparum Dd2 ring stage forms assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis2019Journal of natural products, 04-26, Volume: 82, Issue:4
Acrotrione: An Oxidized Xanthene from the Roots of Acronychia pubescens.
AID1890798Inhibition of Th1 cells differentiation in C57BL/6 mouse spleen CD4+ve Th cells assessed as decrease in IFNgamma production at 10 uM measured after 4 days by flow cytometry analysis relative to control
AID1673893Selectivity ratio of IC50 for human IOSE144 cells to IC50 for human A2780 cells2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Monomeric Targeted Protein Degraders.
AID1873114Antimalarial activity against Plasmodium falciparum Cam3.I^R539T assessed as inhibition of parasite growth measured after 6 hrs2022European journal of medicinal chemistry, Jul-05, Volume: 237Spiral molecules with antimalarial activities: A review.
AID1888574Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as increase in Fasn protein expression in liver at 150 mg/kg, ig for 4 weeks by western blot analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1545511Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes after 72 hrs by SYBR Green1 dye based fluorescence assay relative to control2019European journal of medicinal chemistry, May-15, Volume: 170Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.
AID1326741Cell cycle arrest in human HL60 cells assessed as accumulation at G1 phase at 5 uM after 24 hrs by propidium iodide-DNA fluorescence based FACS analysis (Rvb = 46 %)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1497080Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13
Design, synthesis and biological evaluation of artemisinin derivatives containing fluorine atoms as anticancer agents.
AID1812445Inhibition of human recombinant HDAC6 using Tosyl-Gly-ProLys(Ac)-AMC as substrate measured after 60 mins by fluorescence assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1326740Cell cycle arrest in human HL60 cells assessed as accumulation at subG0 phase at 5 uM after 24 hrs by propidium iodide-DNA fluorescence based FACS analysis (Rvb = 5 %)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1274390Antimalarial activity against 4th to 5th gametocyte stage of Plasmodium falciparum 3D7elo1-pfs16-CBG99 assessed as inhibition of gametocyte viability by luciferase reporter gene assay2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials?
AID1612609Antimalarial activity against ring-stage chloroquine-susceptible Plasmodium falciparum 3D7 preincubated for 6 hrs followed by compound wash and measured after 66 hrs by Giemsa-staining based light microscopic analysis2019European journal of medicinal chemistry, Feb-01, Volume: 163Recent advances of tetrazole derivatives as potential anti-tubercular and anti-malarial agents.
AID1546483Cytotoxicity against human U251/CP2 cells assessed as reduction in cell viability after 24 hrs by MTT assay2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Artemisia: a promising plant for the treatment of cancer.
AID1890800Inhibition of Th17 cells differentiation in C57BL/6 mouse spleen CD4+ve Th cells assessed as decrease in IL-17A production at low concentration measured after 4 days by flow cytometry analysis
AID1770983Anticancer activity against human PC-3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 reagent assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Study on the structure-activity relationship of dihydroartemisinin derivatives: Discovery, synthesis, and biological evaluation of dihydroartemisinin-bile acid conjugates as potential anticancer agents.
AID1271047Antiproliferative activity against human SGC7901 cells after 72 hrs by MTT assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Synthesis and in vitro antitumor evaluation of dihydroartemisinin-cinnamic acid ester derivatives.
AID1326697Cytotoxicity against human MIAPaCa2 cells assessed as cell growth inhibition at 50 uM after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1888553Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as ldlr-mRNA expression in liver in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1327392Cytotoxicity against human WI38 cells assessed as reduction in cell viability measured after 48 hrs by SRB assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin.
AID1395100Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Synthesis of novel ring-contracted artemisinin dimers with potent anticancer activities.
AID1545930Antiproliferative activity against human KB cells by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1489616Cytotoxicity against mouse J774 cells after 72 hrs by CellTiter-96 aqueous one solution cell proliferation assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design and Synthesis of Orally Bioavailable Piperazine Substituted 4(1H)-Quinolones with Potent Antimalarial Activity: Structure-Activity and Structure-Property Relationship Studies.
AID1812436Cytotoxicity against human HL-60 cells assessed as inhibition of cell proliferation measured after 72 hrs by ATPlite assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1888550Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as decrease in size of lipid droplet concentration in serum at 150 mg/kg, ig for 4 weeks by H and E staining based assay2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1395101Antiproliferative activity against rat PC12 cells after 72 hrs by CCK-8 assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Synthesis of novel ring-contracted artemisinin dimers with potent anticancer activities.
AID1395099Antiproliferative activity against human SH-SY5Y cells after 72 hrs by CCK-8 assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Synthesis of novel ring-contracted artemisinin dimers with potent anticancer activities.
AID1441260Antimalarial activity against Plasmodium yoelii YM infected in BALB/c mouse assessed as mouse survival at 90 mg/kg, sc administered BID for 4 days starting at 96 hrs post infection, 8 hrs apart by Giemsa-staining based microscopic analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Target Elucidation by Cocrystal Structures of NADH-Ubiquinone Oxidoreductase of Plasmodium falciparum (PfNDH2) with Small Molecule To Eliminate Drug-Resistant Malaria.
AID1440393Antibiofilm activity against Candida albicans SC5314 after 24 hrs in presence of miconazole by Cell-Titer Blue assay2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Tackling Fungal Resistance by Biofilm Inhibitors.
AID1699649Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 ring stage incubated for 72 hrs by DAPI-staining based imaging analysis2020Journal of natural products, 11-25, Volume: 83, Issue:11
Antiplasmodial Alkaloids from the Australian Bryozoan
AID1583706Antischistosomal activity against Schistosoma mansoni infected in NMRI mouse assessed as reduction in total adult worm burden at 400 mg/kg, po administered as single dose starting on day 49 post-infection and measured at 28 days post treatment relative to2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Structure-Activity Relationship of Antischistosomal Ozonide Carboxylic Acids.
AID1326695Cytotoxicity against human HL60 cells assessed as cell growth inhibition at 30 uM after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1401024Antiproliferative activity against human K562 cells after 96 hrs by MTT assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis, anticancer evaluation and pharmacokinetic study of novel 10-O-phenyl ethers of dihydroartemisinin.
AID1779234Antimalarial activity against synchronous ring stage of Plasmodium falciparum Dd2 assessed as parasite growth inhibition incubated for 72 hrs by Griffith assay based fluorescence analysis2021European journal of medicinal chemistry, Oct-05, Volume: 221Discovery and development of 2-aminobenzimidazoles as potent antimalarials.
AID1401023Antiproliferative activity against human U937 cells after 96 hrs by MTT assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis, anticancer evaluation and pharmacokinetic study of novel 10-O-phenyl ethers of dihydroartemisinin.
AID1489612Antimalarial activity against pyrimethamine/chloroquine-resistant Plasmodium falciparum W2 infected in human type A-positive erythrocytes after 48 hrs by [3H]-hypoxanthine incorporation assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design and Synthesis of Orally Bioavailable Piperazine Substituted 4(1H)-Quinolones with Potent Antimalarial Activity: Structure-Activity and Structure-Property Relationship Studies.
AID1888560Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as increase in Abcg5 mRNA expression in liver in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1272410Activity at MDR1 (unknown origin) expressed in MDCK cells assessed as permeability across basolateral to apical after 90 mins by LC-MS/MS analysis2016European journal of medicinal chemistry, Jan-27, Volume: 108Combating P-glycoprotein-mediated multidrug resistance with 10-O-phenyl dihydroartemisinin ethers in MCF-7 cells.
AID1326701Cytotoxicity against human HepG2 cells assessed as cell growth inhibition at 50 uM after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1699652Selectivity index, ratio of IC50 for cytotoxicity against human HEK293 cells to IC50 for antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 ring stage2020Journal of natural products, 11-25, Volume: 83, Issue:11
Antiplasmodial Alkaloids from the Australian Bryozoan
AID1357960Cytotoxicity against human MDA-MB-231 cells after 96 hrs under hypoxic condition by MTT assay
AID1888551Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as ALT level in serum at 150 mg/kg, ig for 4 weeks2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1457833Antiplasmodial activity against Plasmodium falciparum Cam3.2_rev infected in human RBC assessed as time required to reduce early ring stage parasite viability by 50% by SYTO 61-staining-based flow cytometry2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID1562839Solubility of compound in water2019European journal of medicinal chemistry, Sep-15, Volume: 178Synthesis of novel S-linked dihydroartemisinin derivatives and evaluation of their anticancer activity.
AID1401028Antiproliferative activity against human MDA-MB-231 cells after 96 hrs by MTT assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis, anticancer evaluation and pharmacokinetic study of novel 10-O-phenyl ethers of dihydroartemisinin.
AID1545825Antiproliferative activity against human COLO205 cells assessed as reduction in cell viability after 24 hrs by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1326732Cell cycle arrest in human HL60 cells assessed as accumulation at subG0 phase at 0.5 uM after 24 hrs by propidium iodide-DNA fluorescence based FACS analysis (Rvb = 5 %)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1504889Selectivity index, ratio of IC50 for HEK293 cells to IC50 for chloroquine-sensitive Plasmodium falciparum 3D72017Journal of natural products, 12-22, Volume: 80, Issue:12
Pimentelamines A-C, Indole Alkaloids Isolated from the Leaves of the Australian Tree Flindersia pimenteliana.
AID1888554Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as hmgcr-mRNA expression in liver in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1271050Cytotoxicity against human L02 cells after 72 hrs by MTT assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Synthesis and in vitro antitumor evaluation of dihydroartemisinin-cinnamic acid ester derivatives.
AID1401022Antiproliferative activity against human HL60 cells after 96 hrs by MTT assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis, anticancer evaluation and pharmacokinetic study of novel 10-O-phenyl ethers of dihydroartemisinin.
AID1888555Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as Cyp39a1 mRNA expression in liver in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1357958Cytotoxicity against human HT-29 cells after 96 hrs under hypoxic condition by MTT assay
AID1648008Selectivity ratio of IC50 for HEK293 cells to IC50 for antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd22020Journal of natural products, 02-28, Volume: 83, Issue:2
A Meroisoprenoid, Heptenolides, and
AID1888564Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as increase in Slcob2 mRNA expression in liver in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1699658Cytotoxicity against human HEK293 cells assessed as reduction in cell viability at 0.1 uM after 72 hrs by resazurin dye based assay2020Journal of natural products, 11-25, Volume: 83, Issue:11
Antiplasmodial Alkaloids from the Australian Bryozoan
AID1770986Anticancer activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 reagent assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Study on the structure-activity relationship of dihydroartemisinin derivatives: Discovery, synthesis, and biological evaluation of dihydroartemisinin-bile acid conjugates as potential anticancer agents.
AID1327395Selectivity index, ratio of IC50 for CHO cells to IC50 for chloroquine-sensitive asexual erythrocyte stage form Plasmodium falciparum NF542016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin.
AID1326698Cytotoxicity against human PC3 cells assessed as cell growth inhibition at 30 uM after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1626152Cytotoxicity against mouse J774 cells2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
ICI 56,780 Optimization: Structure-Activity Relationship Studies of 7-(2-Phenoxyethoxy)-4(1H)-quinolones with Antimalarial Activity.
AID1327391Resistance index, ratio of IC50 for chloroquine-resistant asexual erythrocyte stage form Plasmodium falciparum Dd2 to IC50 for chloroquine-sensitive asexual erythrocyte stage form Plasmodium falciparum NF542016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin.
AID1272413Activity at MDR1 (unknown origin) expressed in MDCK cells assessed as efflux ratio of permeability across basolateral to apical side over apical to basolateral side2016European journal of medicinal chemistry, Jan-27, Volume: 108Combating P-glycoprotein-mediated multidrug resistance with 10-O-phenyl dihydroartemisinin ethers in MCF-7 cells.
AID1888572Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as increase in SCD1 protein expression in liver at 150 mg/kg, ig for 4 weeks by western blot analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1782709Inhibition of recombinant Plasmodium falciparum falcipain-2 expressed in Escherichia coli M15 assessed as reduction in free AMC release using Z-FR-AMC as a substrate measured over 30 mins by fluorometric assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Combating multi-drug resistant malaria parasite by inhibiting falcipain-2 and heme-polymerization: Artemisinin-peptidyl vinyl phosphonate hybrid molecules as new antimalarials.
AID1327389Antiplasmodial activity against chloroquine-sensitive asexual erythrocyte stage form Plasmodium falciparum NF54 measured after 48 hrs by pLDH assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin.
AID1545820Antiproliferative activity against mouse P388 cells by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1545826Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1354693Inhibition of Plasmodium falciparum 3D7 6xHis-tagged PI3K helica domain expressed in Escherichia coli by Western blot analysis2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Plasmodial Kinase Inhibitors: License to Cure?
AID1888556Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as Cyp7a1 mRNA expression in liver in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1812456Antiplasmodial activity against synchronized ring stage Plasmodium falciparum 3D7 assessed as parasite reduction rate in lag phase by measuring time required to achieve maximum speed of action at 10 times IC50 concentration2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1274589Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis2015Journal of natural products, Dec-24, Volume: 78, Issue:12
Rotenoids, Flavonoids, and Chalcones from the Root Bark of Millettia usaramensis.
AID1890797Inhibition of Th1 cells differentiation in C57BL/6 mouse spleen CD4+ve Th cells assessed as decrease in IFNgamma production at low concentration measured after 4 days by flow cytometry analysis
AID1326737Cell cycle arrest in human HL60 cells assessed as accumulation at G1 phase at 1 uM after 24 hrs by propidium iodide-DNA fluorescence based FACS analysis (Rvb = 46 %)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1401026Antiproliferative activity against human PC3 cells after 96 hrs by MTT assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis, anticancer evaluation and pharmacokinetic study of novel 10-O-phenyl ethers of dihydroartemisinin.
AID1574646Antimalarial activity against Plasmodium falciparum Dd2 after 72 hrs by DAPI staining-based confocal imaging analysis2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Hydroxamic Acid Inhibitors Provide Cross-Species Inhibition of Plasmodium M1 and M17 Aminopeptidases.
AID1326739Cell cycle arrest in human HL60 cells assessed as accumulation at G2 phase at 1 uM after 24 hrs by propidium iodide-DNA fluorescence based FACS analysis (Rvb = 1 %)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1545817Antiproliferative activity against human MCF7 cells by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1626149Antimalarial activity against Plasmodium falciparum W22016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
ICI 56,780 Optimization: Structure-Activity Relationship Studies of 7-(2-Phenoxyethoxy)-4(1H)-quinolones with Antimalarial Activity.
AID1326727Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for human LS180 cells2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1779233Antimalarial activity against synchronous ring stage of Plasmodium falciparum 3D7 assessed as parasite growth inhibition incubated for 72 hrs by Griffith assay based fluorescence analysis2021European journal of medicinal chemistry, Oct-05, Volume: 221Discovery and development of 2-aminobenzimidazoles as potent antimalarials.
AID1504885Cytotoxicity against HEK293 cells after 72 hrs by resazurin dye based assay2017Journal of natural products, 12-22, Volume: 80, Issue:12
Pimentelamines A-C, Indole Alkaloids Isolated from the Leaves of the Australian Tree Flindersia pimenteliana.
AID1888557Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as Cyp46a1 mRNA expression in liver in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1545831Antiproliferative activity against human HepG2 cells by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1888575Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as increase in CD36 mRNA expression in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1546480Induction of apoptosis in human U937 cells assessed as increase in apoptotic cells at 60 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometric analysis relative to control2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Artemisia: a promising plant for the treatment of cancer.
AID1437503Growth inhibition of HEK293 cells at 20 uM after 72 hrs by PrestoBlue staining based fluorescence assay relative to control
AID1574648Growth inhibition of HEK293 cells at 10 uM after 72 hrs by resazurin dye based assay relative to control2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Hydroxamic Acid Inhibitors Provide Cross-Species Inhibition of Plasmodium M1 and M17 Aminopeptidases.
AID1673905Growth inhibition of human OVCAR3 cells incubated for 48 hrs by MTT assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Monomeric Targeted Protein Degraders.
AID1326744Induction of apoptosis in human HL60 cells assessed as loss of mitochondrial membrane potential at 0.2 uM after 24 hrs by Rh123 dye-based FACS analysis (Rvb = 5%)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1485911Cytotoxicity against HUVEC assessed as reduction in cell number after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis of nοvel artemisinin dimers with polyamine linkers and evaluation of their potential as anticancer agents.
AID1327387Thermal stability of the compound assessed as onset of decomposition temperature by thermogravimetric analysis2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin.
AID1648003Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as reduction in parasite rowth incubated for 72 hrs by DAPI staining based fluorescence assay2020Journal of natural products, 02-28, Volume: 83, Issue:2
A Meroisoprenoid, Heptenolides, and
AID1812457Antiplasmodial activity against synchronized ring stage Plasmodium falciparum 3D7 assessed as parasite reduction over one cycle upto 48 hrs at 10 times IC50 concentration2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1573776Antimalarial activity against ring stage Plasmodium falciparum 3D7 infected in type A-positive human erythrocytes after 72 hrs by SYBR green 1 dye-based fluorescence assay2019Bioorganic & medicinal chemistry, 01-01, Volume: 27, Issue:1
Synthesis of new betulinic acid/betulin-derived dimers and hybrids with potent antimalarial and antiviral activities.
AID1545822Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 24 hrs by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1354698Antiplasmodial activity Plasmodium berghei infected in ip dosed mouse2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Plasmodial Kinase Inhibitors: License to Cure?
AID1272412Permeability across basolateral to apical side in MDCK cells after 90 mins by LC-MS/MS analysis2016European journal of medicinal chemistry, Jan-27, Volume: 108Combating P-glycoprotein-mediated multidrug resistance with 10-O-phenyl dihydroartemisinin ethers in MCF-7 cells.
AID1401031Selectivity ratio of GI50 for human MCF7 cells to GI50 for human MCF7/ADR cells2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis, anticancer evaluation and pharmacokinetic study of novel 10-O-phenyl ethers of dihydroartemisinin.
AID1779232Antimalarial activity against Plasmodium falciparum 3D7 assessed as reduction in parasite growth measured after 72 hrs by Monash assay based fluorescence analysis2021European journal of medicinal chemistry, Oct-05, Volume: 221Discovery and development of 2-aminobenzimidazoles as potent antimalarials.
AID1504883Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs by DAPI staining based confocal microplate imaging method2017Journal of natural products, 12-22, Volume: 80, Issue:12
Pimentelamines A-C, Indole Alkaloids Isolated from the Leaves of the Australian Tree Flindersia pimenteliana.
AID1545818Antiproliferative activity against human Lu1 cells by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1888561Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as increase in Abcg8 protein expression in liver in liver at 150 mg/kg, ig for 4 weeks by western blot analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1326700Cytotoxicity against human HepG2 cells assessed as cell growth inhibition at 30 uM after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1888579Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as increase in ACACa protein expression in liver at 150 mg/kg, ig for 4 weeks by western blot analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1271048Antiproliferative activity against human A549 cells after 72 hrs by MTT assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Synthesis and in vitro antitumor evaluation of dihydroartemisinin-cinnamic acid ester derivatives.
AID1812435Cytotoxicity against human Hep-G2 cells assessed as inhibition of cell proliferation measured after 72 hrs by ATPlite assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1441261Antimalarial activity against Plasmodium yoelii YM infected in BALB/c mouse assessed as parasite cure level at 10 to 90 mg/kg, ip administered on days 1 post infection by Giemsa-stained microscopic analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Target Elucidation by Cocrystal Structures of NADH-Ubiquinone Oxidoreductase of Plasmodium falciparum (PfNDH2) with Small Molecule To Eliminate Drug-Resistant Malaria.
AID1708867Antiplasmodial activity against artemisinin-resistant ring stage Plasmodium falciparum 6320 infected in human erythrocytes assessed as reduction in parasite growth incubated for 72 hrs by Giemsa staining based light microscopic method2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Discovery of Novel
AID1326742Cell cycle arrest in human HL60 cells assessed as accumulation at S phase at 5 uM after 24 hrs by propidium iodide-DNA fluorescence based FACS analysis (Rvb = 53 %)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1271044Drug degradation at 2 to 4 mg at 210 to 220 degC by thermogravimetric analysis in the presence of nitrogen gas2016European journal of medicinal chemistry, Jan-01, Volume: 107Synthesis and in vitro antitumor evaluation of dihydroartemisinin-cinnamic acid ester derivatives.
AID1825886Antimalarial activity against asexual blood stage chloroquine-resistant Plasmodium falcipuram GB4 assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green I staining based fluorescence analysis
AID1327388Thermal stability of the compound assessed as melting point by thermogravimetric analysis2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin.
AID1639289Cytotoxicity against HEK293 cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence assay relative to control2019Journal of natural products, 04-26, Volume: 82, Issue:4
Acrotrione: An Oxidized Xanthene from the Roots of Acronychia pubescens.
AID1326717Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for human PC3 cells2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1676947Parasiticidal activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in RBC assessed as reduction in parasitemia at 50 nM incubated for 6 to 48 hrs followed by compound washout and then incubated for 96 hrs by Giemsa staining based micr2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Synthesis, Structure-Activity Relationship, and Antimalarial Efficacy of 6-Chloro-2-arylvinylquinolines.
AID1812444Inhibition of human recombinant HDAC3 using Tosyl-Gly-ProLys(Ac)-AMC as substrate measured after 60 mins by fluorescence assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1639283Antiplasmodial activity against drug-sensitive Plasmodium falciparum 3D7 ring stage forms assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis2019Journal of natural products, 04-26, Volume: 82, Issue:4
Acrotrione: An Oxidized Xanthene from the Roots of Acronychia pubescens.
AID1271046Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Synthesis and in vitro antitumor evaluation of dihydroartemisinin-cinnamic acid ester derivatives.
AID1395098Antiproliferative activity against human A549 cells after 72 hrs by CCK-8 assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Synthesis of novel ring-contracted artemisinin dimers with potent anticancer activities.
AID1401027Antiproliferative activity against human LNCAP cells after 96 hrs by MTT assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis, anticancer evaluation and pharmacokinetic study of novel 10-O-phenyl ethers of dihydroartemisinin.
AID1708857Antiplasmodial activity against synchronized ring stage Plasmodium falciparum 3D7 infected in human erythrocytes assessed as reduction in parasite growth incubated for 72 hrs by Giemsa staining based light microscopic method2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Discovery of Novel
AID1326738Cell cycle arrest in human HL60 cells assessed as accumulation at S phase at 1 uM after 24 hrs by propidium iodide-DNA fluorescence based FACS analysis (Rvb = 53 %)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1574645Antimalarial activity against Plasmodium falciparum 3D7 after 72 hrs by DAPI staining-based confocal imaging analysis2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Hydroxamic Acid Inhibitors Provide Cross-Species Inhibition of Plasmodium M1 and M17 Aminopeptidases.
AID1545823Antiproliferative activity against human A431 cells assessed as reduction in cell viability after 24 hrs by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 1831,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID1673894Selectivity ratio of IC50 for human IOSE144 cells to IC50 for human OVCAR3 cells2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Monomeric Targeted Protein Degraders.
AID1326728Cell cycle arrest in human HL60 cells assessed as accumulation at subG0 phase at 0.2 uM after 24 hrs by propidium iodide-DNA fluorescence based FACS analysis (Rvb = 5 %)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1782710Inhibition of recombinant Plasmodium falciparum falcipain-2 expressed in Escherichia coli M15 assessed as reduction in free AMC release using Z-FR-AMC as a substrate measured over 30 mins by Cheng-prusoff equation analysis2021European journal of medicinal chemistry, Aug-05, Volume: 220Combating multi-drug resistant malaria parasite by inhibiting falcipain-2 and heme-polymerization: Artemisinin-peptidyl vinyl phosphonate hybrid molecules as new antimalarials.
AID1673904Growth inhibition of human A2780 cells incubated for 48 hrs by MTT assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Monomeric Targeted Protein Degraders.
AID1326734Cell cycle arrest in human HL60 cells assessed as accumulation at S phase at 0.5 uM after 24 hrs by propidium iodide-DNA fluorescence based FACS analysis (Rvb = 53 %)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1777163Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 incubated for 72 hrs by spectrophotometry based parasite lactate dehydrogenase assay2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Enantioselective Synthesis and Profiling of Potent, Nonlinear Analogues of Antimalarial Tetraoxanes E209 and N205.
AID1497081Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13
Design, synthesis and biological evaluation of artemisinin derivatives containing fluorine atoms as anticancer agents.
AID1888569Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as decrease in Slc51b mRNA expression in Ileum in at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1546482Cytotoxicity against human U373 cells assessed as reduction in cell viability after 24 hrs by MTT assay2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Artemisia: a promising plant for the treatment of cancer.
AID1485903In vivo antiangiogenic activity in Leghorn chicken embryo chorioallantoic membrane assessed as decrease in total vessel length at 10 nmol/egg after 48 hrs relative to control2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis of nοvel artemisinin dimers with polyamine linkers and evaluation of their potential as anticancer agents.
AID1546479Induction of apoptosis in rat C6 cells assessed as apoptotic cells at 200 uM after 24 hr in presence of holo-transferrin by Annexin V-FITC/propidium iodide staining based flow cytometric analysis relative to control2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Artemisia: a promising plant for the treatment of cancer.
AID1441257Antimalarial activity against Plasmodium yoelii YM infected in BALB/c mouse assessed as mouse survival at 30 mg/kg, sc administered BID for 4 days starting at 96 hrs post infection, 8 hrs apart by Giemsa-staining based microscopic analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Target Elucidation by Cocrystal Structures of NADH-Ubiquinone Oxidoreductase of Plasmodium falciparum (PfNDH2) with Small Molecule To Eliminate Drug-Resistant Malaria.
AID1326730Cell cycle arrest in human HL60 cells assessed as accumulation at S phase at 0.2 uM after 24 hrs by propidium iodide-DNA fluorescence based FACS analysis (Rvb = 53 %)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1441259Antimalarial activity against Plasmodium yoelii YM infected in BALB/c mouse assessed as time duration for parasite cure at 90 mg/kg, sc administered BID for 4 days starting at 96 hrs post infection, 8 hrs apart by Giemsa-staining based microscopic analysi2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Target Elucidation by Cocrystal Structures of NADH-Ubiquinone Oxidoreductase of Plasmodium falciparum (PfNDH2) with Small Molecule To Eliminate Drug-Resistant Malaria.
AID1648004Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 assessed as reduction in parasite growth incubated for 72 hrs by DAPI staining based fluorescence assay2020Journal of natural products, 02-28, Volume: 83, Issue:2
A Meroisoprenoid, Heptenolides, and
AID1497084Cytotoxicity against human A375 cells assessed as reduction in cell viability after 72 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13
Design, synthesis and biological evaluation of artemisinin derivatives containing fluorine atoms as anticancer agents.
AID1326750Induction of apoptosis in human HL60 cells assessed as induction of apoptotic bodies at 0.5 uM after 24 hrs by hoechst 33258 staining-based microscopic analysis2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1770984Anticancer activity against human Jurkat cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 reagent assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Study on the structure-activity relationship of dihydroartemisinin derivatives: Discovery, synthesis, and biological evaluation of dihydroartemisinin-bile acid conjugates as potential anticancer agents.
AID1395102Antiproliferative activity against human L02 cells after 72 hrs by CCK-8 assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Synthesis of novel ring-contracted artemisinin dimers with potent anticancer activities.
AID1326736Cell cycle arrest in human HL60 cells assessed as accumulation at subG0 phase at 1 uM after 24 hrs by propidium iodide-DNA fluorescence based FACS analysis (Rvb = 5 %)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1326745Induction of apoptosis in human HL60 cells assessed as loss of mitochondrial membrane potential at 0.5 uM after 24 hrs by Rh123 dye-based FACS analysis (Rvb = 5%)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1825880Antimalarial activity against asexual blood stage chloroquine-resistant Plasmodium falciparum Dd2 assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green I staining based fluorescence analysis
AID1355623Antiviral activity against recombinant HCMV AD169 expressing GFP infected in human foreskin fibroblast assessed as reduction in virus-induced cytopathic effect after 7 days
AID1708865Antiplasmodial activity against Plasmodium falciparum CP286 infected in human erythrocytes assessed as reduction in parasite growth incubated for 72 hrs by Giemsa staining based light microscopic method2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Discovery of Novel
AID1853163Antimalarial activity against chloroquine sensitive Plasmodium falciparum 3D7 infected in human RBC assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green dye based fluorescence assay2022RSC medicinal chemistry, Dec-14, Volume: 13, Issue:12
Preparation, biological evaluation and QSAR analysis of urea substituted 2,4-diamino-pyrimidine anti-malarials.
AID1357961Cytotoxicity against human MDA-MB-231 cells after 96 hrs under normoxic condition by MTT assay
AID1437497Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human RBC after 72 hrs by DAPI staining based confocal microscopic method
AID1498471Cytotoxicity against human CEM/ADR5000 cells over-expressing P-gp assessed as reduction in cell viability after 72 hrs by resazurin dye based assay2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Access to new highly potent antileukemia, antiviral and antimalarial agents via hybridization of natural products (homo)egonol, thymoquinone and artemisinin.
AID1546484Induction of apoptosis in human HCT116 cells assessed as increase in apoptotic cells at 40 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometric analysis relative to control2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Artemisia: a promising plant for the treatment of cancer.
AID1812458Antiplasmodial activity against Plasmodium falciparum 3D7 assessed as time to kill initial parasite load at 10 times IC50 concentration2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1326707Cytotoxicity against human HL60 cells assessed as cell growth inhibition after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1676949Antiplasmodial activity against synchronous gametocyte late stage of Plasmodium falciparum 3D7 harboring luc7 incubated for 72 hrs by ONE-Glo luciferase assay2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Synthesis, Structure-Activity Relationship, and Antimalarial Efficacy of 6-Chloro-2-arylvinylquinolines.
AID1639290Selectivity ratio of IC50 for Plasmodium falciparum Dd2 ring stage forms to IC50 for Plasmodium falciparum 3D7 ring stage forms2019Journal of natural products, 04-26, Volume: 82, Issue:4
Acrotrione: An Oxidized Xanthene from the Roots of Acronychia pubescens.
AID1888559Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as increase in Abcg8 mRNA expression in liver in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1274587Cytotoxicity against HEK293 cells assessed as cell viability at 20 uM after 72 hrs by resazurin-based plate reader analysis2015Journal of natural products, Dec-24, Volume: 78, Issue:12
Rotenoids, Flavonoids, and Chalcones from the Root Bark of Millettia usaramensis.
AID1562838Elimination half-life in Sprague-Dawley rat at 10 mg/kg administered as iv bolus dose by EC-HPLC analysis2019European journal of medicinal chemistry, Sep-15, Volume: 178Synthesis of novel S-linked dihydroartemisinin derivatives and evaluation of their anticancer activity.
AID1504881Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 after 72 hrs by DAPI staining based confocal microplate imaging method2017Journal of natural products, 12-22, Volume: 80, Issue:12
Pimentelamines A-C, Indole Alkaloids Isolated from the Leaves of the Australian Tree Flindersia pimenteliana.
AID1812434Antiplasmodial activity against asynchronous asexual culture of Plasmodium falciparum NF54 assessed as parasite growth inhibition2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1441254Antimalarial activity against Plasmodium yoelii YM infected in BALB/c mouse assessed as mouse survival at 10 mg/kg, sc administered BID for 4 days starting at 96 hrs post infection, 8 hrs apart by Giemsa-staining based microscopic analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Target Elucidation by Cocrystal Structures of NADH-Ubiquinone Oxidoreductase of Plasmodium falciparum (PfNDH2) with Small Molecule To Eliminate Drug-Resistant Malaria.
AID1497079Cytotoxicity against human U87 cells assessed as reduction in cell viability after 72 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13
Design, synthesis and biological evaluation of artemisinin derivatives containing fluorine atoms as anticancer agents.
AID1825887Antimalarial activity against asexual blood stage sulfadoxine-pyrimethamine/mefloquine-resistant Plasmodium falcipuram CP286 assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green I staining based fluorescence analysis
AID1326754Lipophilicity, log P of the compound2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1639288Selectivity index, ratio of IC50 for HEK293 cells to IC50 for drug-sensitive Plasmodium falciparum 3D7 ring stage forms2019Journal of natural products, 04-26, Volume: 82, Issue:4
Acrotrione: An Oxidized Xanthene from the Roots of Acronychia pubescens.
AID1441255Antimalarial activity against Plasmodium yoelii YM infected in BALB/c mouse assessed as parasite growth inhibition at 30 mg/kg, sc administered BID for 4 days starting at 96 hrs post infection, 8 hrs apart by Giemsa-staining based microscopic analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Target Elucidation by Cocrystal Structures of NADH-Ubiquinone Oxidoreductase of Plasmodium falciparum (PfNDH2) with Small Molecule To Eliminate Drug-Resistant Malaria.
AID1638553Antimalarial activity against Plasmodium berghei infected in mouse inoculated with Plasmodium berghei infected RBCs dosed orally starting at 2 hrs after inoculation of infected RBCs followed by same dose administration for 3 more days after each 24 hrs pe2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
3,3'-Disubstituted 5,5'-Bi(1,2,4-triazine) Derivatives with Potent in Vitro and in Vivo Antimalarial Activity.
AID1326743Cell cycle arrest in human HL60 cells assessed as accumulation at G2 phase at 5 uM after 24 hrs by propidium iodide-DNA fluorescence based FACS analysis (Rvb = 1 %)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1812442Inhibition of human recombinant HDAC1 using Tosyl-Gly-ProLys(Ac)-AMC as substrate measured after 60 mins by fluorescence assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1649432Antimalarial activity against Plasmodium falciparum clinical isolates measured after 72 hrs by SYBR green dye based fluorescence assay2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials.
AID1441252Antimalarial activity against Plasmodium yoelii YM infected in BALB/c mouse assessed as parasite growth inhibition at 10 mg/kg, sc administered BID for 4 days starting at 96 hrs post infection, 8 hrs apart by Giemsa-staining based microscopic analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Target Elucidation by Cocrystal Structures of NADH-Ubiquinone Oxidoreductase of Plasmodium falciparum (PfNDH2) with Small Molecule To Eliminate Drug-Resistant Malaria.
AID1326712Cytotoxicity against human MIAPaCa2 cells assessed as cell growth inhibition after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1888567Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as increase in Slc10a1 mRNA expression in liver in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1888563Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as decrease in Abcg1 mRNA expression in liver in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1888562Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as increase in Abcg5 protein expression in liver in liver at 150 mg/kg, ig for 4 weeks by western blot analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1498470Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by resazurin dye based assay2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Access to new highly potent antileukemia, antiviral and antimalarial agents via hybridization of natural products (homo)egonol, thymoquinone and artemisinin.
AID1782707Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 24 hrs by WST-1 assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Combating multi-drug resistant malaria parasite by inhibiting falcipain-2 and heme-polymerization: Artemisinin-peptidyl vinyl phosphonate hybrid molecules as new antimalarials.
AID1888547Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as increase in HDL-C concentration in serum at 150 mg/kg, ig for 4 weeks2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1888580Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as increase in CD36 protein expression in liver at 150 mg/kg, ig for 4 weeks by western blot analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1498472Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes after 72 hrs by SYBR green dye fluorescence assay2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Access to new highly potent antileukemia, antiviral and antimalarial agents via hybridization of natural products (homo)egonol, thymoquinone and artemisinin.
AID1676942Antiplasmodial activity against synchronized chloroquine-resistant Plasmodium falciparum Dd2 reduction in microbial growth at 50 nM treated with compound at 42 hrs post infection measured after 12 hrs by YOYO-1 staining-based flow cytometric analysis2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Synthesis, Structure-Activity Relationship, and Antimalarial Efficacy of 6-Chloro-2-arylvinylquinolines.
AID1770985Anticancer activity against human 786-0 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 reagent assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Study on the structure-activity relationship of dihydroartemisinin derivatives: Discovery, synthesis, and biological evaluation of dihydroartemisinin-bile acid conjugates as potential anticancer agents.
AID1326699Cytotoxicity against human PC3 cells assessed as cell growth inhibition at 50 uM after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1546481Antitumour activity against human U937 cells xenografted in NOD/SCID mouse assessed as tumor growth inhibition at 50 mg/kg, ip for 20 days relative to control2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Artemisia: a promising plant for the treatment of cancer.
AID1326733Cell cycle arrest in human HL60 cells assessed as accumulation at G1 phase at 0.5 uM after 24 hrs by propidium iodide-DNA fluorescence based FACS analysis (Rvb = 46 %)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1812441Inhibition of Plasmodium falciparum NF54 HDAC using extract measured after 60 mins by fluorescence assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1888577Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as increase in Elovl6 mRNA expression in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1326729Cell cycle arrest in human HL60 cells assessed as accumulation at G1 phase at 0.2 uM after 24 hrs by propidium iodide-DNA fluorescence based FACS analysis (Rvb = 46 %)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1888549Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as decrease in number of lipid droplet concentration in liver at 150 mg/kg, ig for 4 weeks by H and E staining based assay2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1888565Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as increase in Abcb1a mRNA expression in liver in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1401030Antiproliferative activity against human MCF7/ADR cells after 96 hrs by MTT assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis, anticancer evaluation and pharmacokinetic study of novel 10-O-phenyl ethers of dihydroartemisinin.
AID1327393Cytotoxicity against CHO cells assessed as reduction in cell viability measured after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin.
AID1441253Antimalarial activity against Plasmodium yoelii YM infected in BALB/c mouse assessed as time duration for parasite cure at 10 mg/kg, sc administered BID for 4 days starting at 96 hrs post infection, 8 hrs apart by Giemsa-staining based microscopic analysi2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Target Elucidation by Cocrystal Structures of NADH-Ubiquinone Oxidoreductase of Plasmodium falciparum (PfNDH2) with Small Molecule To Eliminate Drug-Resistant Malaria.
AID1888545Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as TG concentration in serum at 150 mg/kg, ig for 4 weeks2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1626150Antimalarial activity against Plasmodium falciparum TM90-C2B2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
ICI 56,780 Optimization: Structure-Activity Relationship Studies of 7-(2-Phenoxyethoxy)-4(1H)-quinolones with Antimalarial Activity.
AID1888548Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as decrease in LDL-C concentration in serum at 150 mg/kg, ig for 4 weeks2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1812443Inhibition of human recombinant HDAC2 using Tosyl-Gly-ProLys(Ac)-AMC as substrate measured after 60 mins by fluorescence assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites.
AID1326726Cytotoxicity against human LS180 cells assessed as cell growth inhibition after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1326705Cytotoxicity against human HL60 cells assessed as cell growth inhibition at 1 uM after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1497083Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13
Design, synthesis and biological evaluation of artemisinin derivatives containing fluorine atoms as anticancer agents.
AID1497082Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 07-15, Volume: 28, Issue:13
Design, synthesis and biological evaluation of artemisinin derivatives containing fluorine atoms as anticancer agents.
AID1485912Cytotoxicity against HUVEC assessed as reduction in cell number at 10 uM after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis of nοvel artemisinin dimers with polyamine linkers and evaluation of their potential as anticancer agents.
AID1888570Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as decrease in Fabp6 mRNA expression in Ileum in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1888576Hypocholesterolemic activity in OVX-induced C57BL/6 mouse model assessed as increase in Elovl5 mRNA expression in liver at 150 mg/kg, ig for 4 weeks by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile.
AID1326746Induction of apoptosis in human HL60 cells assessed as loss of mitochondrial membrane potential at 1 uM after 24 hrs by Rh123 dye-based FACS analysis (Rvb = 5%)2016European journal of medicinal chemistry, Oct-21, Volume: 122Synthesis of a series of novel dihydroartemisinin monomers and dimers containing chalcone as a linker and their anticancer activity.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID674169Growth inhibition of human SF295 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID1126762Antibacterial activity against multidrug-resistant 1 ug/ml Mycobacterium tuberculosis clinical isolate 1256 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID1191135Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as inhibition of parasite proliferation after 96 hrs by SYBR Green I-based fluorescence method2015European journal of medicinal chemistry, Jan-27, Volume: 90Synthesis and in vitro biological evaluation of dihydroartemisinyl-chalcone esters.
AID323681Reduction of [3H]chloroquine uptake in chloroquine-resistant Plasmodium falciparum RSA11 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID558828Antimalarial activity against Plasmodium falciparum D6 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID1126759Antibacterial activity against drug-sensitive 1 ug/ml Mycobacterium tuberculosis clinical isolate 821 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID543636Antimicrobial activity against Echinococcus multilocularis metacestode assessed as increase in alkaline phosphatase activity at 40 uM after 8 days2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro and in vivo treatments of echinococcus protoscoleces and metacestodes with artemisinin and artemisinin derivatives.
AID323684Reduction of [3H]dihydroartemisinin uptake in chloroquine-sensitive Plasmodium falciparum 3D7 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID564237Antiplasmodial activity against Plasmodium falciparum harboring mutant pfmdr-1-86 gene after 18 hrs by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID425945Antimalarial activity as parasitaemia against Plasmodium berghei ANKA infected Swiss mice (Mus musculus) at 30 mg/kg intraperitoneal single dose 64 hrs post infection (Rvb=2.5%+/-0.5%)2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Pharmacodynamics of doxycycline in a murine malaria model.
AID1762668Cytotoxicity against mouse BV-2 cells assessed as reduction in cell viability incubated for 24 hrs by crystal violet dye based assay2021Bioorganic & medicinal chemistry, 06-01, Volume: 39Cannabidiol-dihydroartemisinin conjugates for ameliorating neuroinflammation with reduced cytotoxicity.
AID1212143Induction of CYP2B6 in human hepatocytes at 10 uM after 72 hrs relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID558836Antimalarial activity against Plasmodium falciparum IMT A4 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID1212133Inhibition of CYP2B6 in human liver microsomes incubated for 3 mins prior to NADPH addition measured after 10 mins by LC-MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID1191138Selectivity index, ratio of IC50 for human WI38 cells to IC50 for chloroquine-sensitive Plasmodium falciparum 3D72015European journal of medicinal chemistry, Jan-27, Volume: 90Synthesis and in vitro biological evaluation of dihydroartemisinyl-chalcone esters.
AID558840Antimalarial activity against Plasmodium falciparum IMT 10336 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID311446Antimalarial activity against Plasmodium falciparum K1 by microculture radioisotope assay2007Journal of natural products, Sep, Volume: 70, Issue:9
Antimalarial and antituberculous poly-O-acylated jatrophane diterpenoids from Pedilanthus tithymaloides.
AID676638Cytotoxicity against human HL60 cells after 48 hrs by MTT assay in presence of DFOM2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID564290Antimalarial activity against Plasmodium falciparum HB3 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID1212122Chemical stability of the compound in human hepatocyte culture medium assessed as compound remaining at 1 to 50 uM after 24 hrs2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID558846Antimalarial activity against Plasmodium falciparum IMT L1 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID674207Growth restoration activity in cdc2-1 rad9-deficient Saccharomyces cerevisiae assessed as growth zone at 12.5 to 400 ug/disc incubated at 37 degC for 6 hrs and 28 degC for 2 days2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID236038Bioavailability obtained after oral administration; Not determined2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID562271Antimalarial activity against Plasmodium falciparum isolates assessed as parasite growth inhibition after 72 hrs by ELISA based histidine-rich protein 2 in vitro drug susceptibility assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Antimalarial activity of tigecycline, a novel glycylcycline antibiotic.
AID564307Antimalarial activity against Plasmodium falciparum W2 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S and I356T mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID453388Antileishmanial activity against Leishmania donovani promastigotes after 48 hrs by alamar blue assay2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers.
AID338835Cytotoxicity against mouse EAC after 3 days by MTT assay1993Journal of natural products, Jun, Volume: 56, Issue:6
Cytotoxicity of artemisinin-related endoperoxides to Ehrlich ascites tumor cells.
AID755418Acute toxicity in bovine EBTr cells at 50 uM after 72 hrs2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Novel artemisinin derivatives with potential usefulness against liver/colon cancer and viral hepatitis.
AID576711Antimalarial activity against Plasmodium falciparum 7G8 harboring pfATP6 L263 mutant assessed as inhibition of [3H]hypoxanthine incorporation2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance.
AID428027Growth inhibition of adriamycin-resistant mouse P388 cells after 72 hrs by trypan blue exclusion assay2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Synthesis of a series of novel dihydroartemisinin derivatives containing a substituted chalcone with greater cytotoxic effects in leukemia cells.
AID453402Antibacterial activity against Escherichia coli ATCC 35218 by modified CLSI/NCCLS method2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers.
AID1212121Cytotoxicity against human hepatocytes assessed as cell viability relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID545362Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum C2 infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID1126748Antibacterial activity against duck Escherichia coli assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID1244911Cytotoxicity against human HL7702 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Sep-18, Volume: 102Antitumor activity of endoperoxide-iron chelator conjugates-design, synthesis and biological evaluation.
AID158856Inhibitory concentration against Plasmodium falciparum W2 Indochina1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Arteether, a new antimalarial drug: synthesis and antimalarial properties.
AID576724Antimalarial activity against Plasmodium falciparum D10 clone 1 assessed as inhibition of [3H]hypoxanthine incorporation2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance.
AID563111Antimalarial activity against Plasmodium falciparum IMT Vol harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scin2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID761774Antiplasmodial activity against Plasmodium falciparum K1 after 42 hrs by microdilution method2013Journal of natural products, Jul-26, Volume: 76, Issue:7
Bioactive compounds from the roots of Strophioblachia fimbricalyx.
AID636828Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 by microculture radioisotope technique2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Lanostane and hopane triterpenes from the entomopathogenic fungus Hypocrella sp. BCC 14524.
AID1186146Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Synthesis, biological evaluation and molecular docking of novel chalcone-coumarin hybrids as anticancer and antimalarial agents.
AID428117Antiparasitic activity as reduced parasitaemia after 36 hrs against Plasmodium berghei ANKA infected Swiss mice (Mus musculus) at 30 mg/kg intraperitoneal dosed 64 hrs post infection2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID676995Selectivity index, ratio of CC50 for human HeLa cells to IC50 for Plasmodium falciparum 3D7 ring stage cells2012Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17
Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy.
AID444497Anticancer activity against human A549 cells by sulforhodamine B assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and anticancer activity of novel amide derivatives of non-acetal deoxoartemisinin.
AID1212154Induction of CYP2D6 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID561064Antiplasmodial activity against Plasmodium falciparum D62009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID1126747Antibacterial activity against Escherichia coli assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID325364Antiparasitic activity against Leishmania donovani in hamster assessed as reduction of spleen parasite burden at 50 mg/kg, po2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Artemisinins inhibit Trypanosoma cruzi and Trypanosoma brucei rhodesiense in vitro growth.
AID1126754Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID1212157Induction of UGT2B7 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID1126744Antibacterial activity against Salmonella assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID564288Antimalarial activity against Plasmodium falciparum FCR3 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID444931Volume of distribution in Sprague-Dawley rat at 2.5 to 3.5 mg/kg, iv2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
The structure-activity relationship of the antimalarial ozonide arterolane (OZ277).
AID576719Antimalarial activity against Plasmodium falciparum 7G8 clone M1 assessed as inhibition of [3H]hypoxanthine incorporation2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance.
AID564299Antimalarial activity against Plasmodium falciparum IMT 10354 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID428019Growth inhibition of human HL60 cells at 1 uM after 72 hrs by trypan blue exclusion assay2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Synthesis of a series of novel dihydroartemisinin derivatives containing a substituted chalcone with greater cytotoxic effects in leukemia cells.
AID755419Antiviral activity against Bovine viral diarrhea virus Oregon C24V genotype 1 subgenotype b infected in bovine EBTr cells assesed as inhibition of virus-induced cytopathic effect at 20 to 100 uM after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Novel artemisinin derivatives with potential usefulness against liver/colon cancer and viral hepatitis.
AID1239475Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes assessed as parasite growth inhibition after 72 hrs by SYBR Green I assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Highly potent artemisinin-derived dimers and trimers: Synthesis and evaluation of their antimalarial, antileukemia and antiviral activities.
AID561053Cmax in Plasmodium falciparum-infected patient at 40 mg/kg, po2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID323685Reduction of [3H]dihydroartemisinin uptake in chloroquine-resistant Plasmodium falciparum RSA11 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID545360Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID674186Growth inhibition of human OVCAR3 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID1762619Antimalarial activity against multi drug-resistant Plasmodium falciparum K1 infected in human erythrocytes assessed as inhibition of [G-3H]hypoxanthine uptake preincubated for 24 hrs followed by [G-3H]hypoxanthine addition and measured after 18 hrs by sci
AID558843Antimalarial activity against Plasmodium falciparum IMT K14 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID1212158Induction of MDR1 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID425758Antimalarial activity as reduced parasitaemia after 24hrs against Plasmodium berghei ANKA infected Swiss mice (Mus musculus) at 30 mg/kg intraperitoneal single dose 64 hrs post infection2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Pharmacodynamics of doxycycline in a murine malaria model.
AID1252953Cytotoxicity against human MOLT3 cells after 48 hrs by XTT assay2015European journal of medicinal chemistry, Oct-20, Volume: 103Novel 1,4-naphthoquinone-based sulfonamides: Synthesis, QSAR, anticancer and antimalarial studies.
AID674197Growth inhibition of human MKN45 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID1752549Antimalarial activity against chloroquine-sensitive plasmodium falciparum 3D7 infected in human erythrocytes assessed as parasite growth inhibition measured after 72 hrs by SYBR green dye based fluorescence analysis2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Preparation, biological & cheminformatics-based assessment of N
AID564302Antimalarial activity against Plasmodium falciparum IMT K14 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID545393Half life in in children with uncomplicated falciparum malaria at 32 to 35 mg/kg, po2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID595427Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 assessed as reduction in uptake of [3H]-hypoxanthine by microculture radioisotope technique2011Journal of natural products, Apr-25, Volume: 74, Issue:4
Cytotoxic pentacyclic and tetracyclic aromatic sesquiterpenes from Phomopsis archeri.
AID361324Induction of apoptosis in human HL60 cells assessed as mitochondrial membrane depolarization at 10 uM after 24 hrs by flow cytometry in presence of Z-VAD-fmk2007The Journal of biological chemistry, Mar-30, Volume: 282, Issue:13
Evidence for the involvement of carbon-centered radicals in the induction of apoptotic cell death by artemisinin compounds.
AID84804Inhibitory activity against human umbilical vein endothelial cells (HUVEC) was assayed using MTT colorimetric proliferation assay2003Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21
Growth inhibition activity of thioacetal artemisinin derivatives against human umbilical vein endothelial cells.
AID380092Antimalarial activity against Plasmodium falciparum K1 by [3H]hypoxanthine uptake2006Journal of natural products, Feb, Volume: 69, Issue:2
A cyclopeptide from the Insect pathogenic fungus Cordyceps sp. BCC 1788.
AID414404Cytotoxicity against human HT29-AK cells after 72 hrs by MTT assay2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Antitumour and antimalarial activity of artemisinin-acridine hybrids.
AID311558Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 by microculture radioisotope assay2007Journal of natural products, Oct, Volume: 70, Issue:10
Antimalarial benzoquinones from an endophytic fungus, Xylaria sp.
AID547315Antimalarial activity against Plasmodium falciparum2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro activities of quinine and other antimalarials and pfnhe polymorphisms in Plasmodium isolates from Kenya.
AID545379Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 harboring D10 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of piperaquine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID453399Antifungal activity against Aspergillus fumigatus ATCC 90906 by modified CLSI/NCCLS method2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers.
AID1212152Induction of CYP2C19 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID279315Inhibition of Plasmodium falciparum AZ10011008 isolate in HRP2 ELISA2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
In vitro antimalarial activity of azithromycin, artesunate, and quinine in combination and correlation with clinical outcome.
AID564287Antimalarial activity against Plasmodium falciparum FCM29 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID237222Plasma half life period after intravenous administration ( 20 mg/kg )2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID158369In vitro antimalarial activity against Plasmodium falciparum FCR31995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Synthesis, characterization, and antimalarial activity of the glucuronides of the hydroxylated metabolites of arteether.
AID545371Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of piperaquine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID564230Antiplasmodial activity against multidrug-resistant Plasmodium falciparum VS/1 after 18 hrs by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1.
AID579482Cytotoxicity against CHO cells by MTT assay2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Synthesis, in vitro antimalarial and cytotoxicity of artemisinin-aminoquinoline hybrids.
AID325366Antiparasitic activity against Leishmania donovani in hamster assessed as reduction of liver parasite burden at 50 mg/kg, po2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Artemisinins inhibit Trypanosoma cruzi and Trypanosoma brucei rhodesiense in vitro growth.
AID453386Selectivity index, ratio of TC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for Plasmodium falciparum W22009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers.
AID1077199Antiplasmodial activity against asexual erythrocytic stage of chloroquine-sensitive Plasmodium falciparum NF54 assessed as parasite growth inhibition after 48 hrs by lactate dehydrogenase assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Synthesis, in vitro antiplasmodial activity and cytotoxicity of a series of artemisinin-triazine hybrids and hybrid-dimers.
AID564306Antimalarial activity against Plasmodium falciparum IMT Vol assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID403422Antifungal activity against Candida albicans ATCC 90028 at 50 ug/mL by modified NCCLS method2005Journal of natural products, Aug, Volume: 68, Issue:8
Antifungal activity of artemisinin derivatives.
AID511254Antimicrobial activity against chloroquine-resistant Plasmodium falciparum HB3 by ELISA2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
In vitro sensitivities of Plasmodium falciparum to different antimalarial drugs in Uganda.
AID563109Antimalarial activity against Plasmodium falciparum IMT K4 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S mutant gene, Pmdr1 S1034C, N1042D mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hr2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID361314Induction of apoptosis in human HL60 cells assessed as mitochondrial membrane depolarization by flow cytometry2007The Journal of biological chemistry, Mar-30, Volume: 282, Issue:13
Evidence for the involvement of carbon-centered radicals in the induction of apoptotic cell death by artemisinin compounds.
AID545377Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 harboring 7G8 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of piperaquine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID279313Inhibition of Plasmodium falciparum in HRP2 ELISA2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
In vitro antimalarial activity of azithromycin, artesunate, and quinine in combination and correlation with clinical outcome.
AID674187Growth inhibition of human OVCAR4 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID671462Antimalarial activity against asexual erythrocyte stage of chloroquine-resistant Plasmodium falciparum Dd2 by parasite lactate dehydrogenase assay2012Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15
Synthesis, antimalarial activity and cytotoxicity of 10-aminoethylether derivatives of artemisinin.
AID755431Cytotoxicity against human HepG2 cells after 72 hrs by formazan test2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Novel artemisinin derivatives with potential usefulness against liver/colon cancer and viral hepatitis.
AID561062Apparent oral clearance in Plasmodium falciparum-infected patient at 40 mg/kg, po2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID545392Half life in in adults with uncomplicated falciparum malaria at 32 to 35 mg/kg, po2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID151998In vitro antimalarial activity against Plasmodium falciparum D6 (Sierra Leone)1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Antimalarial activity of new water-soluble dihydroartemisinin derivatives. 2. Stereospecificity of the ether side chain.
AID576727Antimalarial activity against Plasmodium falciparum D10 clone M1 assessed as inhibition of [3H]hypoxanthine incorporation2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance.
AID558847Antimalarial activity against Plasmodium falciparum IMT Vol assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID674172Growth inhibition of human SNB78 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID449706NOVARTIS: Inhibition Frequency Index (IFI) - the number of HTS assays where a compound showed > 50% inhibition/induction, expressed as a percentage of the number of assays in which the compound was tested.2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID560762Stability of compound in presence of methoxyhemoglobin assessed as pseudo-first order degradation rate constant at 10 uM at 20degC over 24 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Stability of peroxide antimalarials in the presence of human hemoglobin.
AID1239480Resistance index, ratio of IC50 for human CEM/ADR5000 cells to IC50 for human CCRF-CEM cells2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Highly potent artemisinin-derived dimers and trimers: Synthesis and evaluation of their antimalarial, antileukemia and antiviral activities.
AID414407Antimalarial activity after 48 hrs against chloroquine-sensitive Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Antitumour and antimalarial activity of artemisinin-acridine hybrids.
AID641623Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 assessed as inhibition of [3H]-hypoxanthine incorporation2011Journal of natural products, Nov-28, Volume: 74, Issue:11
Cytotoxic and antimalarial azaphilones from Chaetomium longirostre.
AID1126746Antibacterial activity against Staphylococcus aureus assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID1186149Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 after 24 hrs by [3H]hypoxanthine incorporation assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Synthesis, biological evaluation and molecular docking of novel chalcone-coumarin hybrids as anticancer and antimalarial agents.
AID564296Antimalarial activity against Plasmodium falciparum IMT 8425 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID676620Induction of apoptosis in human HL60 cells assessed as caspase 8 activation at 1 uM after 12 hrs by spectrophotometric analysis2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID1252950Cytotoxicity against HuCCa1 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Oct-20, Volume: 103Novel 1,4-naphthoquinone-based sulfonamides: Synthesis, QSAR, anticancer and antimalarial studies.
AID539292Resistance index, ratio of IC50 for chloroquine-sensitive Plasmodium falciparum D10 to IC50 for chloroquine-resistant Plasmodium falciparum Dd22010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
Artemisinin-quinoline hybrid-dimers: synthesis and in vitro antiplasmodial activity.
AID158203In vitro antimalarial activity against Plasmodium falciparum D6 Sierra Leone1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Antimalarial activity of new water-soluble dihydroartemisinin derivatives.
AID1239477Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 72 hrs by resazurin assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Highly potent artemisinin-derived dimers and trimers: Synthesis and evaluation of their antimalarial, antileukemia and antiviral activities.
AID19482Partition coefficient (logP)1995Journal of medicinal chemistry, May-26, Volume: 38, Issue:11
Synthesis, characterization, and antimalarial activity of the glucuronides of the hydroxylated metabolites of arteether.
AID361320Induction of apoptosis in human HL60 cells assessed as activation of caspase 7 by Western blotting2007The Journal of biological chemistry, Mar-30, Volume: 282, Issue:13
Evidence for the involvement of carbon-centered radicals in the induction of apoptotic cell death by artemisinin compounds.
AID561056AUC in Plasmodium falciparum-infected patient at 40 mg/kg, po2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID414405Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Antitumour and antimalarial activity of artemisinin-acridine hybrids.
AID361317Induction of apoptosis in human HL60 cells assessed as increase in sub-G0/G1 population at 1 uM after 24 hrs by flow cytometry2007The Journal of biological chemistry, Mar-30, Volume: 282, Issue:13
Evidence for the involvement of carbon-centered radicals in the induction of apoptotic cell death by artemisinin compounds.
AID561066Antiplasmodial activity against Plasmodium falciparum K12009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID621890Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 assessed as [3H]-hypoxanthine uptake after 24 hrs by scintillation counting2011Journal of natural products, Oct-28, Volume: 74, Issue:10
Diarylpropanes and an arylpropyl quinone from Combretum griffithii.
AID543633Toxicity against Echinococcus multilocularis -infected in BALB/c mouse assessed as adverse effect2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro and in vivo treatments of echinococcus protoscoleces and metacestodes with artemisinin and artemisinin derivatives.
AID453400Antibacterial activity against Staphylococcus aureus ATCC 29213 by modified CLSI/NCCLS method2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers.
AID543627Antimicrobial activity against Echinococcus granulosus protoscoleces assessed as reduction in protoscoleces viability at 40 uM by trypan blue exclusion assay2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro and in vivo treatments of echinococcus protoscoleces and metacestodes with artemisinin and artemisinin derivatives.
AID674176Growth inhibition of human HCT15 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID151997In vitro antimalarial activity against Plasmodium falciparum W-2 Indochina1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Antimalarial activity of new water-soluble dihydroartemisinin derivatives. 2. Stereospecificity of the ether side chain.
AID158019In vitro antimalarial activity against chloroquine-sensitive Plasmodium falciparum K11999Journal of medicinal chemistry, Dec-30, Volume: 42, Issue:26
Novel, potent, semisynthetic antimalarial carba analogues of the first-generation 1,2,4-trioxane artemether.
AID676627Induction of apoptosis in human HL60 cells assessed as caspase 9 activation after 1 to 3 hrs by spectrophotometric analysis2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID323680Reduction of [3H]chloroquine uptake in chloroquine-resistant Plasmodium falciparum RSA11 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID564284Antimalarial activity against Plasmodium falciparum 3D7 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID1126761Antibacterial activity against multidrug-resistant 1 ug/ml Mycobacterium tuberculosis clinical isolate 1237 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID564301Antimalarial activity against Plasmodium falciparum IMT 16332 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID564232Antiplasmodial activity against Plasmodium falciparum clinical isolate after 18 hrs by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1.
AID674193Growth inhibition of human St-4 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID399045Cytotoxicity against human KB cells by SRB assay2005Journal of natural products, Nov, Volume: 68, Issue:11
Hirsutane sesquiterpenes from the fungus Lentinus connatus BCC 8996.
AID399044Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 after 42 hrs by [3H]hypoxanthine uptake2005Journal of natural products, Nov, Volume: 68, Issue:11
Hirsutane sesquiterpenes from the fungus Lentinus connatus BCC 8996.
AID677000Antiplasmodial activity against Plasmodium falciparum NF54 assessed as reduction in stage IV and V gametocyte formation at IC50 level incubated for 48 hrs measured 7 days post compound wash by Giemsa staining2012Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17
Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy.
AID425024Antiplasmodial activity against multidrug-resistant Plasmodium falciparum K12009Journal of natural products, May-22, Volume: 72, Issue:5
Biomimetic transformation and biological activities of Globiferin, a terpenoid benzoquinone from Cordia globifera.
AID674184Growth inhibition of human DMS114 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID564316Antimalarial activity against Plasmodium falciparum IMT A4 harboring Ppcrt M74I, N75E, K76T, A220H, Q271E, N326S and I356T mutant gene, Pmdr1 Y184F, N1042D, D1246Y mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation co2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID545378Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 harboring parental pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of piperaquine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID445035Blood clearance in Sprague-Dawley rat at 2.5 to 3.5 mg/kg, iv2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
The structure-activity relationship of the antimalarial ozonide arterolane (OZ277).
AID558838Antimalarial activity against Plasmodium falciparum IMT 8425 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID361322Induction of apoptosis in human HL60 cells assessed as pyknotic nuclear fragments at 10 uM after 24 hrs in presence of Z-VAD-fmk2007The Journal of biological chemistry, Mar-30, Volume: 282, Issue:13
Evidence for the involvement of carbon-centered radicals in the induction of apoptotic cell death by artemisinin compounds.
AID403421Antifungal activity against Cryptococcus neoformans ATCC 90113 by modified NCCLS method2005Journal of natural products, Aug, Volume: 68, Issue:8
Antifungal activity of artemisinin derivatives.
AID539289Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D102010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
Artemisinin-quinoline hybrid-dimers: synthesis and in vitro antiplasmodial activity.
AID641578Antimalarial activity against chloroquine-, mefloquine-, pyrimethamine-,atovaquone-resistant ring stage Plasmodium falciparum TM90-C2B infected in human A positive erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, antimalarial activity, and structure-activity relationship of 7-(2-phenoxyethoxy)-4(1H)-quinolones.
AID1126751Antibacterial activity against Staphylococcus aureus assessed as zone of inhibition at 2 ug/ml2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID560760Stability of compound in presence water assessed as pseudo-first order degradation rate constant at 10 uM at 20degC over 24 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Stability of peroxide antimalarials in the presence of human hemoglobin.
AID1126760Antibacterial activity against multidrug-resistant 1 ug/ml Mycobacterium tuberculosis clinical isolate 930 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID674178Growth inhibition of human NCI-H23 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID760423Selectivity index, ratio of IC50 for rat L6 cells to IC50 for erythrocytic stage of chloroquine-resistant Plasmodium falciparum IndoChina W22013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Design, Synthesis, and Antiplasmodial Activity of Hybrid Compounds Based on (2R,3S)-N-Benzoyl-3-phenylisoserine.
AID674192Growth inhibition of human ACHN cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID564291Antimalarial activity against Plasmodium falciparum 106/1 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID414403Cytotoxicity against human HL60 cells after 72 hrs by MTT assay2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Antitumour and antimalarial activity of artemisinin-acridine hybrids.
AID755432Antiviral activity against Bovine viral diarrhea virus Oregon C24V genotype 1 subgenotype b infected in bovine EBTr cells assesed as inhibition of virus-induced cytopathic effect at 50 uM after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Novel artemisinin derivatives with potential usefulness against liver/colon cancer and viral hepatitis.
AID444496Anticancer activity against human SK-MEL-2 cells by sulforhodamine B assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and anticancer activity of novel amide derivatives of non-acetal deoxoartemisinin.
AID558829Antimalarial activity against Plasmodium falciparum FCM29 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID674195Growth inhibition of human MKN7 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID563106Antimalarial activity against Plasmodium falciparum IMT 16332 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E mutant gene, Pmdr1 N86Y mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID576507Antiplasmodial activity against Plasmodium falciparum 3D7 infected in RBCs by firefly luciferase reporter gene assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Discovery of potent small-molecule inhibitors of multidrug-resistant Plasmodium falciparum using a novel miniaturized high-throughput luciferase-based assay.
AID545376Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of piperaquine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID563103Antimalarial activity against Plasmodium falciparum IMT 10336 harboring Pfcrt Q271E mutant gene and Ppcrt I371R mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID641577Antimalarial activity against chloroquine-, pyrimethamine-resistant ring stage Plasmodium falciparum W2 infected in human A positive erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Synthesis, antimalarial activity, and structure-activity relationship of 7-(2-phenoxyethoxy)-4(1H)-quinolones.
AID25398Half life was determined1998Bioorganic & medicinal chemistry letters, May-05, Volume: 8, Issue:9
Stability of acetal and non acetal-type analogs of artemisinin in simulated stomach acid.
AID563112Antimalarial activity against Plasmodium falciparum 3D7 harboring Ppcrt I371R mutant gene and Pfnhe-1 ms4760 microsatellite mutant assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID1126758Antibacterial activity against drug-sensitive 1 ug/ml Mycobacterium tuberculosis clinical isolate 760 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID674203Growth inhibition of human PC3 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID748940Half life in human2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
Recent advances in malaria drug discovery.
AID520094Induction of heme alkylation of Fe(II) heme assessed as adduct A472 absorbance change at completion of reaction at 10 uM in presence of 50% ACN-H2O with excess sodium dithionite under argon at 20 degC by spectrophotometry2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Relationship between antimalarial activity and heme alkylation for spiro- and dispiro-1,2,4-trioxolane antimalarials.
AID563110Antimalarial activity against Plasmodium falciparum IMT L1 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillatio2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID561054Tmax in Plasmodium falciparum-infected patient at 40 mg/kg, po2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID383954Cytotoxicity against human KB cells by colorimetric method2008Journal of natural products, May, Volume: 71, Issue:5
Aurocitrin and related polyketide metabolites from the wood-decay fungus Hypocrea sp. BCC 14122.
AID1212147Induction of CYP3A4 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID576728Antimalarial activity against Plasmodium falciparum D10 clone M2 assessed as inhibition of [3H]hypoxanthine incorporation2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance.
AID383806Cytotoxicity against mouse Ehrlich Ascites carcinoma by trypan blue exclusion assay2008European journal of medicinal chemistry, Feb, Volume: 43, Issue:2
Bioactive peroxides as potential therapeutic agents.
AID674179Growth inhibition of human NCI-H226 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID543630Antimicrobial activity against Echinococcus multilocularis metacestode assessed as increase in alkaline phosphatase activity at 10 uM2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro and in vivo treatments of echinococcus protoscoleces and metacestodes with artemisinin and artemisinin derivatives.
AID545363Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum C3 harboring Dd2 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID158685In vitro inhibitory activity against Plasmodium falciparum (sierra leone clone)1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Arteether, a new antimalarial drug: synthesis and antimalarial properties.
AID279314Inhibition of Plasmodium falciparum AZ10011003 isolate in HRP2 ELISA2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
In vitro antimalarial activity of azithromycin, artesunate, and quinine in combination and correlation with clinical outcome.
AID545361Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID576729Antimalarial activity against Plasmodium falciparum D10 clone M3 assessed as inhibition of [3H]hypoxanthine incorporation2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance.
AID561063Apparent volume of distribution in Plasmodium falciparum-infected patient at 40 mg/kg, po2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID323682Reduction of [3H]dihydroartemisinin uptake in chloroquine-sensitive Plasmodium falciparum FC27 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID558834Antimalarial activity against Plasmodium falciparum IMT Bres assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID755429Cytotoxicity against human SKHEP1 cells after 72 hrs by formazan test2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Novel artemisinin derivatives with potential usefulness against liver/colon cancer and viral hepatitis.
AID1160927Antimalarial activity against multi-drug-resistant Plasmodium falciparum W2 infected in human type A+ erythrocytes assessed as growth inhibition after 72 hrs by SYBR Green I assay2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium.
AID361319Induction of apoptosis in human HL60 cells assessed as activation of caspase 3 by Western blotting2007The Journal of biological chemistry, Mar-30, Volume: 282, Issue:13
Evidence for the involvement of carbon-centered radicals in the induction of apoptotic cell death by artemisinin compounds.
AID760425Antiplasmodial activity against erythrocytic stage of multidrug-resistant Plasmodium falciparum Thailand K1 infected in human A positive RBC after 48 hrs by [3H]hypoxanthine incorporation assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Design, Synthesis, and Antiplasmodial Activity of Hybrid Compounds Based on (2R,3S)-N-Benzoyl-3-phenylisoserine.
AID469264Antiplasmodial activity against multidrug-resistant Plasmodium falciparum K1 assessed as [G-3H]hypoxanthine uptake after 24 hrs by scintillation counting2009Journal of natural products, Oct, Volume: 72, Issue:10
Cytotoxic and antiplasmodial compounds from the roots of Strophioblachia fimbricalyx.
AID755430Cytotoxicity against human LS 174T cells after 72 hrs by formazan test2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Novel artemisinin derivatives with potential usefulness against liver/colon cancer and viral hepatitis.
AID1212138Inhibition of recombinant CYP3A4 (unknown origin) incubated for 3 mins prior to NADPH addition measured after 3 mins by LC-MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID564295Antimalarial activity against Plasmodium falciparum IMT 31 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID158863Intrinsic equimolar activity against Plasmodium falciparum W2 Indochina relative to QHS1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Arteether, a new antimalarial drug: synthesis and antimalarial properties.
AID594705Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D102011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Antiplasmodial and antitumor activity of dihydroartemisinin analogs derived via the aza-Michael addition reaction.
AID361318Induction of apoptosis in human HL60 cells assessed as increase in sub-G0/G1 population by flow cytometry2007The Journal of biological chemistry, Mar-30, Volume: 282, Issue:13
Evidence for the involvement of carbon-centered radicals in the induction of apoptotic cell death by artemisinin compounds.
AID564231Antiplasmodial activity against multidrug-sensitive Plasmodium falciparum 3D7 after 18 hrs by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1.
AID576714Antimalarial activity against Plasmodium falciparum D10 harboring pfATP6 263E mutant assessed as inhibition of [3H]hypoxanthine incorporation2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance.
AID477969Antimalarial activity against Plasmodium falciparum K1 assessed as [G-3H]hypoxanthine uptake after 24 hrs by scintillation counting2010Journal of natural products, Apr-23, Volume: 73, Issue:4
Bioactive metabolites from cultures of basidiomycete Favolaschia tonkinensis.
AID383952Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 by microculture radioisotope technique2008Journal of natural products, May, Volume: 71, Issue:5
Aurocitrin and related polyketide metabolites from the wood-decay fungus Hypocrea sp. BCC 14122.
AID1239481Antiviral activity against Human cytomegalovirus AD169 expressing GFP infected in HFF assessed as inhibition of viral replication after 7 days2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Highly potent artemisinin-derived dimers and trimers: Synthesis and evaluation of their antimalarial, antileukemia and antiviral activities.
AID755416Antiviral activity against Bovine viral diarrhea virus Oregon C24V genotype 1 subgenotype b assessed as reduction in viral RNA release at 50 uM by RT-PCR analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Novel artemisinin derivatives with potential usefulness against liver/colon cancer and viral hepatitis.
AID564308Antimalarial activity against Plasmodium falciparum D6 harboring Ppcrt I371R mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID576716Antimalarial activity against Plasmodium falciparum 7G8 clone 1 assessed as inhibition of [3H]hypoxanthine incorporation2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance.
AID1212159Induction of MRP1 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID676637Cytotoxicity against human HL60 cells after 48 hrs by MTT assay in absence of DFOM2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID579483Selectivity index, ratio of IC50 for CHO cells to IC50 for chloroquine-sensitive Plasmodium falciparum D102011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Synthesis, in vitro antimalarial and cytotoxicity of artemisinin-aminoquinoline hybrids.
AID674202Growth inhibition of human DU145 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID1252951Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Oct-20, Volume: 103Novel 1,4-naphthoquinone-based sulfonamides: Synthesis, QSAR, anticancer and antimalarial studies.
AID579481Resistance index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum Dd2 to IC50 for chloroquine-sensitive Plasmodium falciparum D102011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Synthesis, in vitro antimalarial and cytotoxicity of artemisinin-aminoquinoline hybrids.
AID1057261Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as parasite growth inhibition after 48 hrs by SYBR green-1 dye-based fluorescence assay2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Synthesis and evaluation of the antimalarial, anticancer, and caspase 3 activities of tetraoxane dimers.
AID676651Growth inhibition of human HBC5 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID562110Antiplasmodial activity against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid.
AID564286Antimalarial activity against Plasmodium falciparum D6 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID1252952Cytotoxicity against human A549 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Oct-20, Volume: 103Novel 1,4-naphthoquinone-based sulfonamides: Synthesis, QSAR, anticancer and antimalarial studies.
AID564314Antimalarial activity against Plasmodium falciparum IMT Bres harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S and I356T mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID283675Antimalarial activity against multidrug-resistant Plasmodium falciparum K12007Journal of natural products, Apr, Volume: 70, Issue:4
A xanthocillin-like alkaloid from the insect pathogenic fungus Cordyceps brunnearubra BCC 1395.
AID674183Growth inhibition of human DMS273 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID543634Antimicrobial activity against Echinococcus granulosus protoscoleces assessed as reduction in protoscoleces viability at 40 uM upto 2 days by trypan blue exclusion assay2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro and in vivo treatments of echinococcus protoscoleces and metacestodes with artemisinin and artemisinin derivatives.
AID760424Cytotoxicity against rat L6 cells after 70 hrs by Alamar Blue assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Design, Synthesis, and Antiplasmodial Activity of Hybrid Compounds Based on (2R,3S)-N-Benzoyl-3-phenylisoserine.
AID403420Antifungal activity against Candida albicans ATCC 90028 by modified NCCLS method2005Journal of natural products, Aug, Volume: 68, Issue:8
Antifungal activity of artemisinin derivatives.
AID676649Growth inhibition of human HBC4 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID362771Antimalarial activity against multidrug-resistant Plasmodium falciparum K12008Journal of natural products, Sep, Volume: 71, Issue:9
11-Hydroxymonocerin from the plant endophytic fungus Exserohilum rostratum.
AID564289Antimalarial activity against Plasmodium falciparum PA assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID671461Antimalarial activity against asexual erythrocyte stage of chloroquine-sensitive Plasmodium falciparum D10 by parasite lactate dehydrogenase assay2012Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15
Synthesis, antimalarial activity and cytotoxicity of 10-aminoethylether derivatives of artemisinin.
AID1186147Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Synthesis, biological evaluation and molecular docking of novel chalcone-coumarin hybrids as anticancer and antimalarial agents.
AID361303Cytotoxicity against human PBMC after 72 hrs by MTT assay2007The Journal of biological chemistry, Mar-30, Volume: 282, Issue:13
Evidence for the involvement of carbon-centered radicals in the induction of apoptotic cell death by artemisinin compounds.
AID1227982Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 assessed as reduction in parasite growth incubated for 24 hrs by [3H]hypoxanthine incorporation based microculture radioisotope technique based method2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Eremophilane Sesquiterpenes and Diphenyl Thioethers from the Soil Fungus Penicillium copticola PSU-RSPG138.
AID361321Induction of apoptosis in human HL60 cells assessed as pyknotic nuclear fragments at 10 uM after 24 hrs2007The Journal of biological chemistry, Mar-30, Volume: 282, Issue:13
Evidence for the involvement of carbon-centered radicals in the induction of apoptotic cell death by artemisinin compounds.
AID1212134Inhibition of recombinant CYP2B6 (unknown origin) incubated for 3 mins prior to NADPH addition measured after 10 mins by LC-MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID520093Antimalarial activity against chloroquine-resistant Plasmodium falciparum K12008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Relationship between antimalarial activity and heme alkylation for spiro- and dispiro-1,2,4-trioxolane antimalarials.
AID453385Antiplasmodial activity against Plasmodium falciparum W2 infected in RBCs by parasitic LDH release assay2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers.
AID674166Growth inhibition of human MDA-MB-231 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID676639Ratio of IC50 for human HL60 cells in presence of DFOM to IC50 for human HL60 cells in absence of DFOM2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID361323Reversal of induction of apoptosis in human HL60 cells assessed as inhibition of caspase 3 activation at 1 uM after 24 hrs by Western blotting in presence of Z-VAD-fmk2007The Journal of biological chemistry, Mar-30, Volume: 282, Issue:13
Evidence for the involvement of carbon-centered radicals in the induction of apoptotic cell death by artemisinin compounds.
AID674180Growth inhibition of human NCI-H522 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID543635Antimicrobial activity against Echinococcus granulosus protoscoleces assessed as reduction in protoscoleces viability at 40 uM after 6 days by trypan blue exclusion assay2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro and in vivo treatments of echinococcus protoscoleces and metacestodes with artemisinin and artemisinin derivatives.
AID470173Antiplasmodial activity against multidrug-resistant Plasmodium falciparum K1 assessed as [3H]hypoxanthine incorporation after 24 hrs by microtiter plate scintillation counting2009Journal of natural products, Nov, Volume: 72, Issue:11
Diterpenes, sesquiterpenes, and a sesquiterpene-coumarin conjugate from Jatropha integerrima.
AID539291Cytotoxicity against CHO cells by MTT assay2010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
Artemisinin-quinoline hybrid-dimers: synthesis and in vitro antiplasmodial activity.
AID564294Antimalarial activity against Plasmodium falciparum IMT A4 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID449705NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID564305Antimalarial activity against Plasmodium falciparum IMT L1 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID361304Cytotoxicity against human HL60 cells assessed as LDH release after 72 hrs2007The Journal of biological chemistry, Mar-30, Volume: 282, Issue:13
Evidence for the involvement of carbon-centered radicals in the induction of apoptotic cell death by artemisinin compounds.
AID428021Induction of apoptosis in human HL60 cells assessed as occurrence of nuclear shrinkage, blebbing and apoptotic bodies at 2 uM after 24 hrs by acridine orange and ethidium bromide staining2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Synthesis of a series of novel dihydroartemisinin derivatives containing a substituted chalcone with greater cytotoxic effects in leukemia cells.
AID368230Anticancer activity against human HL60 cells by MTT assay2009Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
Synthesis and biological evaluation of extraordinarily potent C-10 carba artemisinin dimers against P. falciparum malaria parasites and HL-60 cancer cells.
AID445034Plasma clearance in Sprague-Dawley rat at 2.5 to 3.5 mg/kg, iv2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
The structure-activity relationship of the antimalarial ozonide arterolane (OZ277).
AID333675Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 after 24 hrs by [3H]hypoxanthine uptake2004Journal of natural products, Nov, Volume: 67, Issue:11
10-membered macrolides from the insect pathogenic fungus Cordyceps militaris BCC 2816.
AID325363Antiparasitic activity against Leishmania donovani in hamster assessed as reduction of spleen parasite burden at 25 mg/kg, po2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Artemisinins inhibit Trypanosoma cruzi and Trypanosoma brucei rhodesiense in vitro growth.
AID453383Antiplasmodial activity against Plasmodium falciparum D6 infected in RBCs by parasitic LDH release assay2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers.
AID1126750Antibacterial activity against Pseudomonas aeruginosa assessed as zone of inhibition at 2 ug/ml2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID594699Cytotoxicity against human HeLa cells after 7 days by MTT assay2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Antiplasmodial and antitumor activity of dihydroartemisinin analogs derived via the aza-Michael addition reaction.
AID563107Antimalarial activity against Plasmodium falciparum IMT K14 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S mutant gene, Pmdr1 Y184F, S1034C, N1042D, D1246Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxant2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID1212144Induction of CYP3A4 in human hepatocytes at 10 uM after 72 hrs relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID545373Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum C2 infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of piperaquine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID576720Antimalarial activity against Plasmodium falciparum 7G8 clone M2 assessed as inhibition of [3H]hypoxanthine incorporation2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance.
AID558830Antimalarial activity against Plasmodium falciparum FCR3 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID539293Selectivity index, ratio of IC50 for CHO cells to IC50 of chloroquine-sensitive Plasmodium falciparum D102010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
Artemisinin-quinoline hybrid-dimers: synthesis and in vitro antiplasmodial activity.
AID511251Antimicrobial activity against Plasmodium falciparum by ELISA2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
In vitro sensitivities of Plasmodium falciparum to different antimalarial drugs in Uganda.
AID425948Antimalarial activity as parasitaemia nadir after 24 hrs against Plasmodium berghei ANKA infected Swiss mice (Mus musculus) at 30 mg/kg intraperitoneal single dose 64 hrs post infection2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Pharmacodynamics of doxycycline in a murine malaria model.
AID676608Growth restoration activity in cdc2-1 rad9-deficient Saccharomyces cerevisiae assessed as growth zone at 400 ug/disc2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID511252Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum W2 by ELISA2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
In vitro sensitivities of Plasmodium falciparum to different antimalarial drugs in Uganda.
AID576718Antimalarial activity against Plasmodium falciparum 7G8 clone M1 harboring pfATP6 L263 mutant assessed as inhibition of [3H]hypoxanthine incorporation2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance.
AID1186145Cytotoxicity against human HuCCa1 cells assessed as reduction in cell viability after 48 hrs by MTT assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Synthesis, biological evaluation and molecular docking of novel chalcone-coumarin hybrids as anticancer and antimalarial agents.
AID236290Volume distribution after intravenous administration of 20 mg/kg2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID279316Inhibition of Plasmodium falciparum AZ10011017 isolate in HRP2 ELISA2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
In vitro antimalarial activity of azithromycin, artesunate, and quinine in combination and correlation with clinical outcome.
AID674181Growth inhibition of human NCI-H460 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID545365Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID287083Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 by micro culture radioisotope technique2007Journal of natural products, May, Volume: 70, Issue:5
Bioactive compounds from Bauhinia purpurea possessing antimalarial, antimycobacterial, antifungal, anti-inflammatory, and cytotoxic activities.
AID1212137Inhibition of CYP3A4 in human liver microsomes incubated for 3 mins prior to NADPH addition measured after 3 mins by LC-MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID543637Antimicrobial activity against Echinococcus granulosus metacestode assessed as loss of multicellular structure of germinal layer by transmission electron microscopy2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro and in vivo treatments of echinococcus protoscoleces and metacestodes with artemisinin and artemisinin derivatives.
AID1057249Cytotoxicity against human HL60 cells assessed as cell viability after 24 hrs by MTT assay2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Synthesis and evaluation of the antimalarial, anticancer, and caspase 3 activities of tetraoxane dimers.
AID236183Plasma clearance after intravenous administration of 20 mg/kg2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.
AID453401Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 by modified CLSI/NCCLS method2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID576717Antimalarial activity against Plasmodium falciparum 7G8 clone 2 assessed as inhibition of [3H]hypoxanthine incorporation2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance.
AID576723Antimalarial activity against Plasmodium falciparum D10 clone 1 harboring pfATP6 L263 mutant assessed as inhibition of [3H]hypoxanthine incorporation2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance.
AID158873In vitro antimalarial activity against Plasmodium falciparum1995Journal of medicinal chemistry, Jun-23, Volume: 38, Issue:13
Mechanism-based development of new antimalarials: synthesis of derivatives of artemisinin attached to iron chelators.
AID449704NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID100410Antileishmanial activity of compound against leishmania donovani was determined in luciferase assay2003Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20
Structure-activity relationships of the antimalarial agent artemisinin. 8. design, synthesis, and CoMFA studies toward the development of artemisinin-based drugs against leishmaniasis and malaria.
AID549354Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID774658Antimalarial activity against asexual stage of Plasmodium falciparum 3D7 after 72 hrs by image-based HTS assay2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Approaches to protozoan drug discovery: phenotypic screening.
AID674168Growth inhibition of human SF268 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID545359Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum TM6 infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID1160928Antimalarial activity against multi-drug-resistant Plasmodium falciparum TM90-C2B infected in human type A+ erythrocytes assessed as growth inhibition after 72 hrs by SYBR Green I assay2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium.
AID676626Induction of apoptosis in human HL60 cells assessed as caspase 8 activation after 1 to 3 hrs by spectrophotometric analysis2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID1212149Induction of CYP1A2 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID606571Antimalarial activity against chloroquine, mefloquine, pyrimethamine and atovaquone-resistant Plasmodium falciparum TM90-C2B infected in human A positive erythrocytes after 72 hrs by SYBR Green I assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of 1,2,3,4-tetrahydroacridin-9(10H)-ones as antimalarials utilizing structure-activity and structure-property relationships.
AID1191134Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of parasite proliferation after 96 hrs by SYBR Green I-based fluorescence method2015European journal of medicinal chemistry, Jan-27, Volume: 90Synthesis and in vitro biological evaluation of dihydroartemisinyl-chalcone esters.
AID755417Acute toxicity in bovine EBTr cells infected with BVDV assessed as reduction in cell viability at 50 uM after 72 hrs2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Novel artemisinin derivatives with potential usefulness against liver/colon cancer and viral hepatitis.
AID545374Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum C3 harboring Dd2 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of piperaquine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID399048Cytotoxicity against african green monkey Vero cells by SRB assay2005Journal of natural products, Nov, Volume: 68, Issue:11
Hirsutane sesquiterpenes from the fungus Lentinus connatus BCC 8996.
AID576722Antimalarial activity against Plasmodium falciparum 7G8 clone M4 assessed as inhibition of [3H]hypoxanthine incorporation2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance.
AID576712Antimalarial activity against Plasmodium falciparum 7G8 harboring pfATP6 263E mutant assessed as inhibition of [3H]hypoxanthine incorporation2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance.
AID563102Antimalarial activity against Plasmodium falciparum IMT 9881 harboring Ppcrt I371R mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID1077196Cytotoxicity against CHO cells after 48 hrs by MTT assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Synthesis, in vitro antiplasmodial activity and cytotoxicity of a series of artemisinin-triazine hybrids and hybrid-dimers.
AID1186148Cytotoxicity against human MOLT3 cells assessed as reduction in cell viability after 48 hrs by XTT assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Synthesis, biological evaluation and molecular docking of novel chalcone-coumarin hybrids as anticancer and antimalarial agents.
AID558827Antimalarial activity against Plasmodium falciparum W2 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID674185Growth inhibition of human LOXIMVI cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID474052Antitumor activity against human HL60 cells after 72 hrs by MTT assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Design, synthesis and antimalarial/anticancer evaluation of spermidine linked artemisinin conjugates designed to exploit polyamine transporters in Plasmodium falciparum and HL-60 cancer cell lines.
AID564309Antimalarial activity against Plasmodium falciparum FCM29 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S and I356T mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID1212155Induction of CYP2E1 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID414406Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Antitumour and antimalarial activity of artemisinin-acridine hybrids.
AID452991Half life in Sprague-Dawley rat at 10 mg/kg, iv2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
The comparative antimalarial properties of weak base and neutral synthetic ozonides.
AID453397Antifungal activity against Candida krusei ATCC 6258 by modified CLSI/NCCLS method2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers.
AID453404Antibacterial activity against Mycobacterium intracellular ATCC 23068 by Franzblau method2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers.
AID558831Antimalarial activity against Plasmodium falciparum PA assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID564298Antimalarial activity against Plasmodium falciparum IMT 10336 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID325365Antiparasitic activity against Leishmania donovani in hamster assessed as reduction of liver parasite burden at 25 mg/kg, po2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Artemisinins inhibit Trypanosoma cruzi and Trypanosoma brucei rhodesiense in vitro growth.
AID558841Antimalarial activity against Plasmodium falciparum IMT 10500 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID558835Antimalarial activity against Plasmodium falciparum IMT Guy assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID545370Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum TM6 infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of piperaquine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID1252955Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 infected in human erythrocytes after 48 hrs by [3H]hypoxanthine incorporation assay2015European journal of medicinal chemistry, Oct-20, Volume: 103Novel 1,4-naphthoquinone-based sulfonamides: Synthesis, QSAR, anticancer and antimalarial studies.
AID1126753Antibacterial activity against duck Escherichia coli assessed as zone of inhibition at 2 ug/ml2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID676998Selectivity index, ratio of CC50 for human HeLa cells to IC50 for VSV-G pseudotyped HIV1 lentiviral particles2012Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17
Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy.
AID563104Antimalarial activity against Plasmodium falciparum IMT 10354 harboring Ppcrt M74I, N75E, K76T, A220S mutant gene, Pmdr1 D1246Y mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID1057250Cytotoxicity against human HT29-AK cells assessed as cell viability after 24 hrs by MTT assay2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Synthesis and evaluation of the antimalarial, anticancer, and caspase 3 activities of tetraoxane dimers.
AID1212146Induction of CYP2B6 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID676997Selectivity index, ratio of CC50 for human HeLa cells to IC50 for Plasmodium falciparum Dd2 ring stage cells2012Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17
Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy.
AID674194Growth inhibition of human MKN1 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID561058AUC (0 to infinity) in Plasmodium falciparum-infected patient at 40 mg/kg, po2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID579479Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 by lactate dehydrogenase assay2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Synthesis, in vitro antimalarial and cytotoxicity of artemisinin-aminoquinoline hybrids.
AID545366Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 harboring 7G8 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID676621Induction of apoptosis in human HL60 cells assessed as caspase 9 activation at 1 uM after 12 hrs by spectrophotometric analysis2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID399046Cytotoxicity against human BC cells by SRB assay2005Journal of natural products, Nov, Volume: 68, Issue:11
Hirsutane sesquiterpenes from the fungus Lentinus connatus BCC 8996.
AID383956Cytotoxicity against human NCI-H187 cells by colorimetric method2008Journal of natural products, May, Volume: 71, Issue:5
Aurocitrin and related polyketide metabolites from the wood-decay fungus Hypocrea sp. BCC 14122.
AID674173Growth inhibition of human HCC2998 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID558837Antimalarial activity against Plasmodium falciparum IMT 31 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID452994Oral bioavailability in Sprague-Dawley rat at 10 mg/kg2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
The comparative antimalarial properties of weak base and neutral synthetic ozonides.
AID674171Growth inhibition of human SNB75 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID1077197Resistance index, ratio of IC50 for asexual erythrocytic stage of chloroquine-resistant Plasmodium falciparum Dd2 to IC50 for asexual erythrocytic stage of chloroquine-sensitive Plasmodium falciparum NF542014European journal of medicinal chemistry, Apr-09, Volume: 76Synthesis, in vitro antiplasmodial activity and cytotoxicity of a series of artemisinin-triazine hybrids and hybrid-dimers.
AID564236Antiplasmodial activity against Plasmodium falciparum harboring wild type pfmdr-1-86 gene after 18 hrs by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1.
AID428025Induction of apoptosis in human HL60 cells assessed as DNA fragmentation at 4 uM after 24 hrs using ethidium bromide staining by DNA gel electrophoresis2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Synthesis of a series of novel dihydroartemisinin derivatives containing a substituted chalcone with greater cytotoxic effects in leukemia cells.
AID566771Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 by microculture radioisotope technique2010Journal of natural products, Dec-27, Volume: 73, Issue:12
Pyridone and tetramic acid alkaloids from the spider pathogenic fungus Torrubiella sp. BCC 2165.
AID664753Antimalarial activity against Plasmodium falciparum K1 infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation incubated for 24 hrs prior to hypoxanthine addition measured after 18 hrs by liquid scintillation counting2012Journal of natural products, Apr-27, Volume: 75, Issue:4
Bifunctionalized amphilectane diterpenes from the sponge Stylissa cf. massa.
AID159028Antimalarial activity against chloroquine-resistant, mefloquine-sensitive Plasmodium falciparum W22002Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
Structure-activity relationships of the antimalarial agent artemisinin. 6. The development of predictive in vitro potency models using CoMFA and HQSAR methodologies.
AID428115Antiparasitic activity as parasitaemia against Plasmodium berghei ANKA infected Swiss mice (Mus musculus) at 30 mg/kg intraperitoneal dose 64 hrs post infection2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria model.
AID676993Antiplasmodial activity against drug resistant Plasmodium falciparum Dd2 ring stage cells assessed as reduction parasitemia by Malstat assay2012Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17
Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy.
AID545368Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 harboring D10 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID674191Growth inhibition of human RXF631L cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID676619Induction of apoptosis in human HL60 cells assessed as caspase 3/7 activation at 1 uM after 12 hrs by spectrophotometric analysis2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID453403Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 by modified CLSI/NCCLS method2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers.
AID383955Cytotoxicity against human BC cells by colorimetric method2008Journal of natural products, May, Volume: 71, Issue:5
Aurocitrin and related polyketide metabolites from the wood-decay fungus Hypocrea sp. BCC 14122.
AID543632Antimicrobial activity against Echinococcus multilocularis -infected in BALB/c mouse assessed as parasite weight at 200 mg/kg body weight intragastrically administered 8 weeks post-infecion (Rvb = 5.71+/-1.79 g)2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro and in vivo treatments of echinococcus protoscoleces and metacestodes with artemisinin and artemisinin derivatives.
AID1212153Induction of CYP3A5 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID1335799Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 infected human erythrocytes assessed as reduction in parasite viability after 24 hrs by [3H]-hypoxanthine incorporation assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Evaluation of the anti-malarial activity and cytotoxicity of 2,4-diamino-pyrimidine-based kinase inhibitors.
AID560761Stability of compound in presence of oxyhemoglobin assessed as pseudo-first order degradation rate constant at 10 uM at 20degC over 24 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Stability of peroxide antimalarials in the presence of human hemoglobin.
AID453395Antifungal activity against Candida albicans ATCC 90028 by modified CLSI/NCCLS method2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers.
AID453398Antifungal activity against Cryptococcus neoformans ATCC 90113 by modified CLSI/NCCLS method2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers.
AID674175Growth inhibition of human HT-29 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID674170Growth inhibition of human SF539 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID674167Growth inhibition of human U251 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID676609Cytotoxicity against human HL60 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID262123Antiangiogenic activity at chorioallantoic membrane of chick embryo at 5 nmol per egg2006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Antiangiogenic activity of deoxoartemisinin derivatives on chorioallantoic membrane.
AID323683Reduction of [3H]dihydroartemisinin uptake in chloroquine-resistant Plasmodium falciparum K1 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID1186150Cytotoxicity against african green monkey Vero cells assessed as reduction in cell viability after 4 days by green fluorescent protein detection method2014European journal of medicinal chemistry, Oct-06, Volume: 85Synthesis, biological evaluation and molecular docking of novel chalcone-coumarin hybrids as anticancer and antimalarial agents.
AID325356Growth inhibition of Trypanosoma brucei rhodesiense trypomastigotes after 72 hrs by Alamar blue assay2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Artemisinins inhibit Trypanosoma cruzi and Trypanosoma brucei rhodesiense in vitro growth.
AID676650Growth inhibition of human BSY1 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID774663Antimalarial activity against early (1 to 3) gametocytic stage of Plasmodium falciparum after 72 hrs by image-based HTS assay2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Approaches to protozoan drug discovery: phenotypic screening.
AID279317Inhibition of Plasmodium falciparum AZ10011022 isolate in HRP2 ELISA2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
In vitro antimalarial activity of azithromycin, artesunate, and quinine in combination and correlation with clinical outcome.
AID1057256Induction of apoptosis in human HL60 cells assessed as activation of caspase-3 activity at 0.2 to 0.6 uM after 24 hrs by flow cytometric analysis2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Synthesis and evaluation of the antimalarial, anticancer, and caspase 3 activities of tetraoxane dimers.
AID427228Antimalarial activity against Plasmodium falciparum K1 by microculture radioisotope technique2009Journal of natural products, Jul, Volume: 72, Issue:7
Isocoumarin glucosides from the scale insect fungus Torrubiella tenuis BCC 12732.
AID561060Half life in Plasmodium falciparum-infected patient at 40 mg/kg, po2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID674189Growth inhibition of human OVCAR8 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID564235Antiplasmodial activity against Plasmodium falciparum harboring mutant pfcrt-76 gene after 18 hrs by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1.
AID558833Antimalarial activity against Plasmodium falciparum 106/1 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID158018In vitro antimalarial activity against chloroquine-sensitive Plasmodium falciparum HB31999Journal of medicinal chemistry, Dec-30, Volume: 42, Issue:26
Novel, potent, semisynthetic antimalarial carba analogues of the first-generation 1,2,4-trioxane artemether.
AID378813Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 by [3H]hypoxanthine uptake2006Journal of natural products, Oct, Volume: 69, Issue:10
Bioactive compounds from the seed fungus Menisporopsis theobromae BCC 3975.
AID453387Toxicity against african green monkey Vero cells2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers.
AID158855Inhibitory concentration against Plasmodium falciparum D6 (Sierra Leone)1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Arteether, a new antimalarial drug: synthesis and antimalarial properties.
AID545364Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum C6harboring 7G8 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID449703NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay 2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID576715Antimalarial activity against Plasmodium falciparum 7G8 clone 1 harboring pfATP6 L263 mutant assessed as inhibition of [3H]hypoxanthine incorporation2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance.
AID452993Blood clearance in Sprague-Dawley rat at 10 mg/kg, iv2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
The comparative antimalarial properties of weak base and neutral synthetic ozonides.
AID674190Growth inhibition of human SKOV3 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID545367Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 harboring parental pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID674188Growth inhibition of human OVCAR5 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID558845Antimalarial activity against Plasmodium falciparum IMT K4 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID444022Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 infected in erythrocytes after 48 hrs by [3H]hypoxanthine incorporation assay2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Transforming rhinacanthin analogues from potent anticancer agents into potent antimalarial agents.
AID760426Antiplasmodial activity against erythrocytic stage of chloroquine-resistant Plasmodium falciparum IndoChina W2 infected in human A positive RBC after 48 hrs by [3H]hypoxanthine incorporation assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Design, Synthesis, and Antiplasmodial Activity of Hybrid Compounds Based on (2R,3S)-N-Benzoyl-3-phenylisoserine.
AID564304Antimalarial activity against Plasmodium falciparum IMT K4 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID545369Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of piperaquine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID1126755Antibacterial activity against drug-sensitive 1 ug/ml Mycobacterium tuberculosis clinical isolate 741 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID1244907Cytotoxicity against human HL60 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Sep-18, Volume: 102Antitumor activity of endoperoxide-iron chelator conjugates-design, synthesis and biological evaluation.
AID564310Antimalarial activity against Plasmodium falciparum FCR3 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S and I356T mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs 2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID158646In vitro antimalarial activity against Plasmodium berghei2001Journal of medicinal chemistry, Jan-04, Volume: 44, Issue:1
Synthesis, antimalarial activity, biomimetic iron(II) chemistry, and in vivo metabolism of novel, potent C-10-phenoxy derivatives of dihydroartemisinin.
AID564318Antimalarial activity against Plasmodium falciparum IMT 8425 harboring Ppcrt I371R mutant gene and Pfnhe-1 ms4760 microsatellite mutant assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID158862Intrinsic equimolar activity against Plasmodium falciparum D6 (Sierra Leone) relative to QHS1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Arteether, a new antimalarial drug: synthesis and antimalarial properties.
AID325355Growth inhibition of Trypanosoma cruzi epimastigotes after 72 hrs by Alamar blue assay2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Artemisinins inhibit Trypanosoma cruzi and Trypanosoma brucei rhodesiense in vitro growth.
AID1252954Cytotoxicity against African green monkey Vero cells after 4 days by GFP detection method2015European journal of medicinal chemistry, Oct-20, Volume: 103Novel 1,4-naphthoquinone-based sulfonamides: Synthesis, QSAR, anticancer and antimalarial studies.
AID594702Resistance index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum Dd2 to IC50 for chloroquine-sensitive Plasmodium falciparum D102011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Antiplasmodial and antitumor activity of dihydroartemisinin analogs derived via the aza-Michael addition reaction.
AID428017Inhibition of human HL60 cell proliferation after 72 hrs by trypan blue exclusion assay2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Synthesis of a series of novel dihydroartemisinin derivatives containing a substituted chalcone with greater cytotoxic effects in leukemia cells.
AID1177057Antiprotozoan activity against Plasmodium falciparum infected in mouse assessed as reduction in parasite growth at 50 mg/kg, ip QD for 4 days2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.
AID323679Reduction of [3H]chloroquine uptake in chloroquine-sensitive Plasmodium falciparum 3D7 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID761652Antimalarial activity against Plasmodium falciparum K1 assessed as reduction in parasite growth measuring [3H]-hypoxanthine uptake by microculture radioisotope technique2013Journal of natural products, Jul-26, Volume: 76, Issue:7
Antiplasmodial and cytotoxic flavans and diarylpropanes from the stems of Combretum griffithii.
AID564297Antimalarial activity against Plasmodium falciparum IMT 9881 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID676992Antiplasmodial activity against Plasmodium falciparum 3D7 ring stage cells assessed as reduction parasitemia by Malstat assay2012Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17
Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy.
AID1126757Antibacterial activity against drug-sensitive 1 ug/ml Mycobacterium tuberculosis clinical isolate 758 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID323678Reduction of [3H]chloroquine uptake in chloroquine-sensitive Plasmodium falciparum FC27 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID144637Evaluated for the neurotoxicity against NB2a Neuroblastoma cells.2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Synthesis and antimalarial activity of sixteen dispiro-1,2,4, 5-tetraoxanes: alkyl-substituted 7,8,15,16-tetraoxadispiro[5.2.5. 2]hexadecanes.
AID674165Growth inhibition of human MCF7 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID1077195Selectivity index, ratio of IC50 for CHO cells to IC50 for asexual erythrocytic stage of chloroquine-sensitive Plasmodium falciparum NF542014European journal of medicinal chemistry, Apr-09, Volume: 76Synthesis, in vitro antiplasmodial activity and cytotoxicity of a series of artemisinin-triazine hybrids and hybrid-dimers.
AID564311Antimalarial activity against Plasmodium falciparum PA harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S and I356T mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID428023Cell cycle arrest in human HL60 cells assessed as accumulation at subG1 phase at 4 uM after 24 hrs using propidium iodide staining by flow cytometry2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Synthesis of a series of novel dihydroartemisinin derivatives containing a substituted chalcone with greater cytotoxic effects in leukemia cells.
AID1212145Induction of CYP2C9 in human hepatocytes at 10 uM after 72 hrs relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID131169Compound was tested in vivo for antimalarial activity against Plasmodium berghei in the mice (Mus musculus) model.1999Journal of medicinal chemistry, Dec-30, Volume: 42, Issue:26
Novel, potent, semisynthetic antimalarial carba analogues of the first-generation 1,2,4-trioxane artemether.
AID676994Antiviral activity against VSV-G pseudotyped HIV1 lentiviral particles infected in human HeLa cells incubated for 48 hrs by spectrofluorometry2012Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17
Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy.
AID564317Antimalarial activity against Plasmodium falciparum IMT 31 harboring Ppcrt I371R mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID1077198Antiplasmodial activity against asexual erythrocytic stage of chloroquine-resistant Plasmodium falciparum Dd2 assessed as parasite growth inhibition after 48 hrs by lactate dehydrogenase assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Synthesis, in vitro antiplasmodial activity and cytotoxicity of a series of artemisinin-triazine hybrids and hybrid-dimers.
AID543631Antimicrobial activity against Echinococcus multilocularis metacestode assessed as loss of multicellular structure of germinal layer by transmission electron microscopy2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro and in vivo treatments of echinococcus protoscoleces and metacestodes with artemisinin and artemisinin derivatives.
AID444495Anticancer activity against human XF498 cells by sulforhodamine B assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and anticancer activity of novel amide derivatives of non-acetal deoxoartemisinin.
AID606570Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum W2 infected in human A positive erythrocytes after 72 hrs by SYBR Green I assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of 1,2,3,4-tetrahydroacridin-9(10H)-ones as antimalarials utilizing structure-activity and structure-property relationships.
AID579480Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 by lactate dehydrogenase assay2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Synthesis, in vitro antimalarial and cytotoxicity of artemisinin-aminoquinoline hybrids.
AID377621Antimalarial activity after 42 hrs against Plasmodium falciparum K12006Journal of natural products, Jun, Volume: 69, Issue:6
Chromone derivatives from the filamentous fungus Lachnum sp. BCC 2424.
AID564315Antimalarial activity against Plasmodium falciparum IMT Guy harboring Ppcrt K76T, A220S, N326D and I371R mutant gene, Pmdr1 T184FN, 1042D and D1246Y, mutant gene and Pfmrp H191Y and S437A mutant gene and Pfnhe-1 ms4760 microsatellite mutant assessed as in2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID1126763Antibacterial activity against multidrug-resistant 1 ug/ml Mycobacterium tuberculosis clinical isolate 1259 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID558839Antimalarial activity against Plasmodium falciparum IMT 9881 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID561067Antiplasmodial activity against Plasmodium falciparum K1 assessed as inhibition of [3H]hypoxanthine incorporation by beta counting2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID1126745Antibacterial activity against Pseudomonas aeruginosa assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID576721Antimalarial activity against Plasmodium falciparum 7G8 clone M3 assessed as inhibition of [3H]hypoxanthine incorporation2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance.
AID1244908Cytotoxicity against human A549 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Sep-18, Volume: 102Antitumor activity of endoperoxide-iron chelator conjugates-design, synthesis and biological evaluation.
AID674174Growth inhibition of human KM12 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID425946Toxicity in Plasmodium berghei ANKA infected Swiss mice (Mus musculus) assessed as median time for adverse effect at 30 mg/kg, intraperitoneally administered as single dose 64 hrs after infection measured after 24 hrs2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Pharmacodynamics of doxycycline in a murine malaria model.
AID564292Antimalarial activity against Plasmodium falciparum IMT Bres assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID564313Antimalarial activity against Plasmodium falciparum 106/1 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S and I356T mutant gene, Pmdr1 N86Y mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID361302Cytotoxicity against human Jurkat cells after 72 hrs by MTT assay2007The Journal of biological chemistry, Mar-30, Volume: 282, Issue:13
Evidence for the involvement of carbon-centered radicals in the induction of apoptotic cell death by artemisinin compounds.
AID563108Antimalarial activity against Plasmodium falciparum IMT K2 harboring Ppcrt M74I, N75E, K76T, A220S, Q271E, N326S mutant gene, Pmdr1 S1034C, N1042D mutant gene and Pfmrp H191Y and S437A mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hr2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID444498Anticancer activity against human SKOV3 cells by sulforhodamine B assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and anticancer activity of novel amide derivatives of non-acetal deoxoartemisinin.
AID504298Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 by microculture radioisotope technique2010Journal of natural products, Sep-24, Volume: 73, Issue:9
Anthraquinone, cyclopentanone, and naphthoquinone derivatives from the sea fan-derived fungi Fusarium spp. PSU-F14 and PSU-F135.
AID545372Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of piperaquine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID1244912Selectivity ratio of IC50 for human HL7702 cells to IC50 for human SMMC7721 cells2015European journal of medicinal chemistry, Sep-18, Volume: 102Antitumor activity of endoperoxide-iron chelator conjugates-design, synthesis and biological evaluation.
AID311493Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 by microculture radioisotope assay2007Journal of natural products, Sep, Volume: 70, Issue:9
Cassane furanoditerpenoids from the seed kernels of Caesalpinia bonduc from Thailand.
AID399047Cytotoxicity against human NCI-H187 cells by SRB assay2005Journal of natural products, Nov, Volume: 68, Issue:11
Hirsutane sesquiterpenes from the fungus Lentinus connatus BCC 8996.
AID1244910Cytotoxicity against human SMMC7721 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Sep-18, Volume: 102Antitumor activity of endoperoxide-iron chelator conjugates-design, synthesis and biological evaluation.
AID1212117Induction of MRP2 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID511255Antimicrobial activity against chloroquine-resistant Plasmodium falciparum K1 by ELISA2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
In vitro sensitivities of Plasmodium falciparum to different antimalarial drugs in Uganda.
AID520092Induction of heme alkylation of Fe(II) heme assessed as loss of heme at 10 uM in presence of 50% ACN-H2O with excess sodium dithionite under argon at 20 degC by spectrophotometry2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Relationship between antimalarial activity and heme alkylation for spiro- and dispiro-1,2,4-trioxolane antimalarials.
AID1126756Antibacterial activity against drug-sensitive 1 ug/ml Mycobacterium tuberculosis clinical isolate 753 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID1212156Induction of UGT1A9 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID1126764Antibacterial activity against multidrug-resistant 1 ug/ml Mycobacterium tuberculosis clinical isolate 1288 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID543628Antimicrobial activity against Echinococcus granulosus protoscoleces assessed as reduction in protoscoleces viability at 10 uM by trypan blue exclusion assay2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro and in vivo treatments of echinococcus protoscoleces and metacestodes with artemisinin and artemisinin derivatives.
AID383957Cytotoxicity against african green monkey Vero cells by colorimetric method2008Journal of natural products, May, Volume: 71, Issue:5
Aurocitrin and related polyketide metabolites from the wood-decay fungus Hypocrea sp. BCC 14122.
AID563105Antimalarial activity against Plasmodium falciparum IMT 10500 harboring Pfcrt Q271E mutant gene and Ppcrt I371R mutant gene and Pfnhe-1 ms4760 microsatellite mutant assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID674182Growth inhibition of human A549 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID452992Volume of distribution in Sprague-Dawley rat at 10 mg/kg, iv2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
The comparative antimalarial properties of weak base and neutral synthetic ozonides.
AID676625Induction of apoptosis in human HL60 cells assessed as caspase 3/7 activation after 1 to 3 hrs by spectrophotometric analysis2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID558842Antimalarial activity against Plasmodium falciparum IMT 16332 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID755412Cytotoxicity against human HepG2(2.2.15) cells assessed as reduction in cell viability at 1 uM measured on day 21 by natural Red test2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Novel artemisinin derivatives with potential usefulness against liver/colon cancer and viral hepatitis.
AID561068Antiplasmodial activity against Plasmodium falciparum D6 isolated from po dosed patient with malaria2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID558826Antimalarial activity against Plasmodium falciparum 3D7 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID444500Anticancer activity against human HCT15 cells by sulforhodamine B assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and anticancer activity of novel amide derivatives of non-acetal deoxoartemisinin.
AID158215In vitro antimalarial activity against Plasmodium falciparum W-2 (Indochina)1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Antimalarial activity of new water-soluble dihydroartemisinin derivatives.
AID564303Antimalarial activity against Plasmodium falciparum IMT K2 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID564285Antimalarial activity against Plasmodium falciparum W2 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID674198Growth inhibition of human MKN74 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID576725Antimalarial activity against Plasmodium falciparum D10 clone 2 assessed as inhibition of [3H]hypoxanthine incorporation2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance.
AID558844Antimalarial activity against Plasmodium falciparum IMT K2 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
AID1126749Antibacterial activity against Salmonella assessed as zone of inhibition at 2 ug/ml2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID361301Cytotoxicity against human HL60 cells after 72 hrs by MTT assay2007The Journal of biological chemistry, Mar-30, Volume: 282, Issue:13
Evidence for the involvement of carbon-centered radicals in the induction of apoptotic cell death by artemisinin compounds.
AID1762667Antiinflammatory activity in mouse BV-2 cells assessed as reduction in LPS-induced nitric oxide production incubated for 24 hrs by 2, 3-diaminonaphthalene based assay2021Bioorganic & medicinal chemistry, 06-01, Volume: 39Cannabidiol-dihydroartemisinin conjugates for ameliorating neuroinflammation with reduced cytotoxicity.
AID478101Antimalarial activity against Plasmodium falciparum K1 after 24 hrs by [G-3H]hypoxanthine uptake assay2010Journal of natural products, Apr-23, Volume: 73, Issue:4
Hopane-type triterpenes and binaphthopyrones from the scale insect pathogenic fungus Aschersonia paraphysata BCC 11964.
AID428018Cytotoxicity against human HL60 cells after 72 hrs by trypan blue exclusion assay2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Synthesis of a series of novel dihydroartemisinin derivatives containing a substituted chalcone with greater cytotoxic effects in leukemia cells.
AID1239478Cytotoxicity against human CEM/ADR5000 cells assessed as cell viability after 72 hrs by resazurin assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Highly potent artemisinin-derived dimers and trimers: Synthesis and evaluation of their antimalarial, antileukemia and antiviral activities.
AID453396Antifungal activity against Candida glabrata ATCC 90030 by modified CLSI/NCCLS method2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers.
AID453384Selectivity index, ratio of TC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for Plasmodium falciparum D62009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers.
AID772516Antimalarial activity against mature gametocytic stage of Plasmodium falciparum assessed as inhibition of mature gamete exflagellation at 10 uM incubated for 24 hrs prior to exflagellation induction at 21 degC measured after 20 mins by microscopic analysi2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Using genetic methods to define the targets of compounds with antimalarial activity.
AID511253Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum D6 by ELISA2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
In vitro sensitivities of Plasmodium falciparum to different antimalarial drugs in Uganda.
AID545375Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum C6harboring 7G8 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation in presence of piperaquine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro.
AID674196Growth inhibition of human MKN28 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID564312Antimalarial activity against Plasmodium falciparum HB3 harboring Ppcrt I371R mutant gene and Pfmdr1 Y184F mutant gene assessed as incorporation of [3]H hypoxanthine after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID1182043Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 assessed as reduction in parasite growth by [3H]-hypoxanthine uptake assay2014Journal of natural products, Jul-25, Volume: 77, Issue:7
Triterpene lactones from cultures of Ganoderma sp. KM01.
AID361325Reversal of induction of apoptosis in human HL60 cells assessed as formation of sub-G0/G1 population at 10 uM after 24 hrs by flow cytometry in presence of Z-VAD-fmk2007The Journal of biological chemistry, Mar-30, Volume: 282, Issue:13
Evidence for the involvement of carbon-centered radicals in the induction of apoptotic cell death by artemisinin compounds.
AID423418Antiplasmodial activity after 24 hrs against Plasmodium falciparum K1 by [G-3H]hypoxanthine uptake2009Journal of natural products, Apr, Volume: 72, Issue:4
Isariotins E and F, spirocyclic and bicyclic hemiacetals from the entomopathogenic fungus Isaria tenuipes BCC 12625.
AID1212150Induction of CYP2A6 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID539290Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd22010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
Artemisinin-quinoline hybrid-dimers: synthesis and in vitro antiplasmodial activity.
AID1244909Cytotoxicity against human SW480 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Sep-18, Volume: 102Antitumor activity of endoperoxide-iron chelator conjugates-design, synthesis and biological evaluation.
AID676996Cytotoxicity against human HeLa cells by MTT assay2012Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17
Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy.
AID594704Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd22011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Antiplasmodial and antitumor activity of dihydroartemisinin analogs derived via the aza-Michael addition reaction.
AID325357Growth inhibition of Leishmania donovani promastigotes after 72 hrs by Alamar blue assay2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Artemisinins inhibit Trypanosoma cruzi and Trypanosoma brucei rhodesiense in vitro growth.
AID1212151Induction of CYP2C8 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID564300Antimalarial activity against Plasmodium falciparum IMT 10500 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID671464Resistance index ratio of IC50 for asexual erythrocyte stage of chloroquine-resistant Plasmodium falciparum Dd2 to IC50 for asexual erythrocyte stage of chloroquine-sensitive Plasmodium falciparum D102012Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15
Synthesis, antimalarial activity and cytotoxicity of 10-aminoethylether derivatives of artemisinin.
AID772517Antimalarial activity against sporozoite stage of Plasmodium yoelii assessed as invasion of human HepG2 cells expressing CD81 incubated for 2 hrs prior to inoculation measured after 1 hr by immunofluorescence assay in presence of penicillin/streptomycin2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Using genetic methods to define the targets of compounds with antimalarial activity.
AID1212148Induction of CYP2C9 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID561069Antiplasmodial activity against Plasmodium falciparum K1 isolated from po dosed patient with malaria2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
AID674177Growth inhibition of human HCT116 cells2012Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
Cleavage mechanism and anti-tumor activity of 3,6-epidioxy-1,10-bisaboladiene isolated from edible wild plants.
AID719099Cytotoxicity against human Caco2 cells assessed as cell viability after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Facile synthesis and anticancer activity of C-10 non-acetal deoxoartemisinin dimers.
AID604714Antimalarial activity against multidrug-resistance Plasmodium falciparum K1 assessed as growth inhibition by microdilution radioisotope technique2011Journal of natural products, May-27, Volume: 74, Issue:5
Kabiramides J and K, trisoxazole macrolides from the sponge Pachastrissa nux.
AID1191136Resistance index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum W2 to IC50 for chloroquine-sensitive Plasmodium falciparum 3D72015European journal of medicinal chemistry, Jan-27, Volume: 90Synthesis and in vitro biological evaluation of dihydroartemisinyl-chalcone esters.
AID1191137Cytotoxicity against human WI38 cells assessed as inhibition of proliferation after 24 hrs by SRB assay2015European journal of medicinal chemistry, Jan-27, Volume: 90Synthesis and in vitro biological evaluation of dihydroartemisinyl-chalcone esters.
AID576713Antimalarial activity against Plasmodium falciparum D10 harboring pfATP6 L263 mutant assessed as inhibition of [3H]hypoxanthine incorporation2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance.
AID563687Antimalarial activity against Plasmodium falciparum assessed as parasite growth inhibition after 48 hrs by [3H]hypoxanthin incorporation assay2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Plasmodium falciparum drug resistance in Madagascar: facing the spread of unusual pfdhfr and pfmdr-1 haplotypes and the decrease of dihydroartemisinin susceptibility.
AID444930Half life in Sprague-Dawley rat at 2.5 to 3.5 mg/kg, iv2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
The structure-activity relationship of the antimalarial ozonide arterolane (OZ277).
AID774661Antimalarial activity against late (4 to 5) gametocytic stage of Plasmodium falciparum after 72 hrs by image-based HTS assay2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Approaches to protozoan drug discovery: phenotypic screening.
AID1126752Antibacterial activity against Escherichia coli assessed as zone of inhibition at 2 ug/ml2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID428026Growth inhibition of mouse P388 cells after 72 hrs by trypan blue exclusion assay2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Synthesis of a series of novel dihydroartemisinin derivatives containing a substituted chalcone with greater cytotoxic effects in leukemia cells.
AID563688Antimalarial activity against Plasmodium falciparum assessed as resistant isolates2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Plasmodium falciparum drug resistance in Madagascar: facing the spread of unusual pfdhfr and pfmdr-1 haplotypes and the decrease of dihydroartemisinin susceptibility.
AID564293Antimalarial activity against Plasmodium falciparum IMT Guy assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum.
AID383712Antimalarial activity against Plasmodium falciparum K1 by microculture radioisotope assay2008Journal of natural products, May, Volume: 71, Issue:5
Phenolic glycosides from the filamentous fungus Acremonium sp. BCC 14080.
AID576726Antimalarial activity against Plasmodium falciparum D10 clone M1 harboring pfATP6 L263 mutant assessed as inhibition of [3H]hypoxanthine incorporation2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Investigations into the role of the Plasmodium falciparum SERCA (PfATP6) L263E mutation in artemisinin action and resistance.
AID755422Cytotoxicity against bovine EBTr cells at 20 to 100 uM after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Novel artemisinin derivatives with potential usefulness against liver/colon cancer and viral hepatitis.
AID558832Antimalarial activity against Plasmodium falciparum HB3 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,453)

TimeframeStudies, This Drug (%)All Drugs %
pre-199022 (1.51)18.7374
1990's87 (5.99)18.2507
2000's251 (17.27)29.6817
2010's744 (51.20)24.3611
2020's349 (24.02)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials0 (0.00%)5.53%
Trials279 (19.66%)5.53%
Reviews0 (0.00%)6.00%
Reviews9 (16.98%)6.00%
Reviews52 (3.66%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Case Studies19 (1.34%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Observational9 (0.63%)0.25%
Other7 (100.00%)84.16%
Other44 (83.02%)84.16%
Other1,060 (74.70%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (116)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
School-based Malaria Control: Impact of Intermittent Preventive Treatment on Malaria Morbidity and Cognitive Function in Ugandan School Children [NCT01231880]Phase 3740 participants (Actual)Interventional2011-02-28Completed
An Active Malaria Epidemiology Cohort Study With Evaluation of a 2 Day Versus 3 Day Treatment Regimen of Dihydroartemisinin (DHA)-Piperaquine for Patients With Uncomplicated Malaria [NCT01280162]222 participants (Actual)Interventional2010-09-30Completed
Comparison of the Efficacy and Safety of Two ACTs Plus Primaquine for Uncomplicated Plasmodium Vivax Malaria in North Sumatera, Indonesia: 1 Year Followup [NCT01288820]Phase 3331 participants (Actual)Interventional2011-01-31Completed
Efficacy, Safety and Tolerability of Dihydroartemisinin-Piperaquine for Treatment of Uncomplicated Falciparum Malaria in Pregnancy: an Open-label, Randomised Controlled, Non-inferiority Trial [NCT01231113]Phase 3417 participants (Actual)Interventional2011-07-31Completed
Intermittent Preventive Treatment in Pregnancy With Sulfadoxine-pyrimethamine Plus Dihydroartemisinin-piperaquine to Prevent Malaria Infection and Reduce Adverse Pregnancy Outcomes in Papua New Guinea - a Randomised Controlled Trial [NCT05426434]Phase 31,172 participants (Anticipated)Interventional2022-08-31Recruiting
A Phase II Double Blind, Placebo-controlled, Randomized Trial of Artesunate Suppositories for the Treatment of HIV-negative Patients With Anal High-grade Squamous Intraepithelial Lesions (Anal HSIL) [NCT05555862]Phase 248 participants (Anticipated)Interventional2023-02-10Recruiting
An Open-label Randomized Trial to Assess the Therapeutic Efficacy of Arterolane-piperaquine Versus Dihydroartemisinin-piperaquine for the Treatment of Uncomplicated Falciparum Malaria in Eastern Myanmar, an Area of Emerging Artemisinin-resistant Falciparu [NCT02461186]Phase 2/Phase 30 participants (Actual)Interventional2015-06-30Withdrawn(stopped due to Change of the study site due to the current political climate in Myanmar.)
Triple Antimalarial Combination (Imatinib-DHA-PPQ) to Accelerate the Parasite Clearance and to Prevent the Selection of Resistant Parasites [NCT03697668]Phase 250 participants (Anticipated)Interventional2017-09-17Recruiting
Prevention of Malaria in HIV-uninfected Pregnant Women and Infants [NCT02793622]Phase 3782 participants (Actual)Interventional2016-09-30Completed
Proof of Concept Study of Eurartesim® in Patients With Imported Uncomplicated Plasmodium Vivax Malaria [NCT02110784]Phase 227 participants (Actual)Interventional2014-06-18Terminated(stopped due to Low recruitment)
Clinical Investigation of In-vivo Susceptibility of P. Falciparum to Artesunate in Phuoc Long Hospital, Binh Phuoc Province, Vietnam [NCT01165372]Phase 2166 participants (Actual)Interventional2010-08-31Completed
Effects of Metronidazole Plus Intermittent Preventive Treatment of Malaria in Pregnancy on Birth Outcomes: a Randomised Controlled Trial in Zambia [NCT04189744]Phase 35,436 participants (Actual)Interventional2019-12-15Completed
Clinical Efficacy of Artemisinin-based Combination Therapy for Treatment of Uncomplicated Plasmodium Falciparum Malaria in North Sumatera, Indonesia and the Association of Molecular Markers With Treatment Outcomes [NCT02325180]Phase 4338 participants (Actual)Interventional2015-01-31Completed
Combination Momordica Charantia Extract and Primaquine Againts Plasmodium Falciparum Uncomplicated and Plasmodium Vivax Uncomplicated Treatment in Manokwari, West Papua [NCT06036030]Phase 250 participants (Actual)Interventional2019-01-11Completed
Dihydroartemisinin-Piperaquine or Sulphadoxine-Pyrimethamine for the Chemoprevention of Malaria in Children With Sickle Cell Anaemia in Eastern and Southern Africa: a Double Blind Randomised Trial (CHEMCHA) [NCT04844099]Phase 3723 participants (Actual)Interventional2021-04-09Completed
Observational Study to Evaluate the Clinical Safety After Introduction of the Fixed Dose Artemisinin-based Combination Therapy Eurartesim® (Dihydroartemisinin/Piperaquine [Dha/Pqp]) in Public Health Districts in Sub-Saharan Africa. [NCT02199951]10,000 participants (Anticipated)Observational2013-09-30Recruiting
Clinical Trial to Evaluate Efficacy and Safety of Sulfadoxine/Pyrimethamine-Amodiaquine and Dihydroartemsinin-Piperaquine Plus Ivermectin Administered Monthly as Intermittent Preventive Treatment in School-aged Children in Burkina Faso [NCT05946642]Phase 313,000 participants (Anticipated)Interventional2023-07-15Recruiting
A Randomised, Single-blinded Controlled Treatment Trial of Subclinical Vivax Infections With Primaquine in Nong Province, Laos [NCT02802813]Phase 1/Phase 241 participants (Actual)Interventional2016-06-14Completed
DPART Study: Dihydroartemisinin-Piperaquine in the Context of Antiretroviral Therapy [NCT04487145]Phase 4190 participants (Actual)Interventional2020-11-23Completed
The Tolerability and Safety of Low Dose Primaquine for Transmission Blocking in Symptomatic Falciparum Infected Cambodians [NCT02434952]Phase 4109 participants (Actual)Interventional2014-10-31Completed
Effectiveness and Safety of Intermittent Preventive Treatment for Malaria Using Either Dihydroartemisinin-piperaquine or Artesunate-amodiaquine in Reducing Malaria Related Morbidities and Improving Cognitive Ability in School-aged Children in Tanzania: A [NCT03640403]Phase 31,555 participants (Actual)Interventional2019-03-26Active, not recruiting
A Phase II, Multicenter, Randomized, Double-blind, Placebo-controlled Study to Investigate the Safety, Pharmacokinetics and Efficacy of Dihydroartemisinin Tablets in Patients With Systemic Lupus Erythematosus [NCT03396393]Phase 2120 participants (Anticipated)Interventional2018-03-31Not yet recruiting
Optimal Chemopreventive Regimens to Prevent Malaria and Improve Birth Outcomes in Uganda [NCT04336189]Phase 32,757 participants (Anticipated)Interventional2020-12-28Recruiting
Evaluating the Effectiveness and Feasibility of Reactive Focal Mass Drug Administration vs. Reactive Case Detection as a Community Level Intervention in Response to a Passively Identified Index Malaria Case in Swaziland [NCT02315690]Phase 34,000 participants (Actual)Interventional2015-09-30Completed
Open-Label Study to Evaluate Potential Pharmacokinetic and Pharmacodynamic Interactions of Orally Administered Mefloquine and Dihydroartemisinin-Piperaquine in Healthy Adult Subjects [NCT02324738]Phase 416 participants (Actual)Interventional2015-01-31Completed
A Phase II Double-blind, Placebo-controlled, Randomized Trial of Topical Artesunate Ointment for the Treatment of Patients With Vulvar High-grade Squamous Intraepithelial Lesions (Vulvar HSIL) [NCT06075264]Phase 227 participants (Anticipated)Interventional2023-12-06Recruiting
Evaluation of the Efficacy of Artemether-lumefantrine and Dihydroartemisinin-piperaquine in Children With Uncomplicated Clinical Malaria in Rural Rwanda [NCT04767217]Phase 4528 participants (Anticipated)Interventional2021-06-14Recruiting
A Double Blind Randomized Controlled Trial of Dihydroartemisinin-piperaquine Alone and in Combination With Single Dose Primaquine to Reduce Post-treatment Malaria Transmission. [NCT02259426]Phase 3120 participants (Actual)Interventional2014-10-31Completed
Efficacy and Safety of Artesunate-amodiaquine and Dihydroartemisinin-piperaquine for the Treatment of Uncomplicated Falciparum Malaria in Mainland Tanzania [NCT03431714]Phase 4333 participants (Actual)Interventional2017-07-14Completed
Phase I, Randomized, Parallel Group Study to Evaluate the Effect of Multiple Oral Doses of Eurartesim on the QT/QTc Interval Compared to Riamet, Placebo and Moxifloxacin in Healthy Male and Female Volunteers [NCT01103830]Phase 1287 participants (Actual)Interventional2010-02-28Completed
Comparison of the Electrocardiographic Effects in Relation to Pharmacokinetic Profile of Chloroquine and Piperaquine in Healthy Thai Subjects [NCT02192944]Phase 416 participants (Actual)Interventional2014-07-31Completed
Impact Tanzania in Vivo Efficacy 2010: Assessing the Efficacy of Artemisinin Combination Therapies for Treatment of Uncomplicated Malaria Infection in Children Aged 6-59 Months [NCT01082705]Phase 3323 participants (Actual)Interventional2010-04-30Completed
Mass Drug Administration of Ivermectin and Dihydroartemisinin-piperaquine as an Additional Intervention for Malaria Elimination [NCT03576313]Phase 34,939 participants (Actual)Interventional2018-08-11Completed
Evaluation of the Household-level Impact of a Single Round of Intermittent Preventive Treatment of Malaria in Schoolchildren: A Randomized Study [NCT04660110]Phase 31,500 participants (Anticipated)Interventional2021-01-28Recruiting
Evaluation of 4 Artemisinin-based Combinations for Treating Uncomplicated Malaria in African Children [NCT00393679]Phase 34,112 participants (Actual)Interventional2007-07-31Completed
A Randomized Controlled Trial of Monthly Dihydroartemisinin-piperaquine Versus Monthly Sulfadoxine-pyrimethamine Versus Daily Trimethoprim-sulfamethoxazole Versus No Therapy for the Prevention of Malaria [NCT00948896]Phase 3600 participants (Actual)Interventional2010-06-30Completed
Effectiveness of Seasonal Malaria Chemoprevention in Koulikoro, Mali [NCT04149106]Phase 34,556 participants (Anticipated)Interventional2019-07-01Active, not recruiting
[NCT00845533]Phase 40 participants Interventional2007-08-31Completed
Clinical Trial to Evaluate Intermittent Screening and Treatment and Intermittent Preventive Treatment of Malaria in Asymptomatic Schoolchildren to Decrease P. Falciparum Infection and Transmission: Phase 2 Comparing Drug Regimens [NCT05980156]Phase 4646 participants (Actual)Interventional2023-02-13Completed
[NCT00868465]600 participants (Anticipated)Interventional2009-04-30Completed
Open Label Randomized Study Evaluating the in Vivo Efficacies of Artemether-lumefantrine and Dihydroartemisinin-piperaquine in the Treatment of Uncomplicated Plasmodium Falciparum Malaria in Children Under Five Years of Age in Western Kenya [NCT05060198]340 participants (Actual)Interventional2016-06-17Completed
A Five-cohort, Randomized, Open-label, Parallel-group Study to Evaluate the Pharmacokinetics of a Single Dose of Tafenoquine (SB252263) 300mg When Co-administered With the Artemisinin-based Combination Therapies (ACT) Artemether + Lumefantrine (AL) and Di [NCT02184637]Phase 1120 participants (Actual)Interventional2014-07-31Completed
The Evaluation of the Effect of Dihydroartemisinin in Patients With Polycystic Ovary Syndrome [NCT05465135]Phase 420 participants (Anticipated)Interventional2022-07-01Recruiting
Operational Feasibility, Impact of Additional Screening Using Highly-sensitives RDTs Combined With High Coverage of IPTp on Placental Malaria and Low Birth Weight [NCT04147546]Phase 3340 participants (Actual)Interventional2020-08-31Completed
Malaria Chemoprevention With Monthly Treatment With Dihydroartemisinin-Piperaquine for the Post-discharge Management of Severe Anaemia in Children Less Than 5 Years in Malawi [NCT02721420]Phase 3375 participants (Anticipated)Interventional2016-03-24Recruiting
Effectiveness of Mass Drug Administration (MDA) for Reducing Seasonal Malaria Transmission Towards Its Elimination in Hotspot Areas in Zanzibar - a Cluster-randomised Controlled Trial [NCT02721186]22,500 participants (Actual)Interventional2016-04-30Completed
A Randomised Controlled Trial to Assess the Antimalarial Drug Susceptibility and Molecular Characterization of Plasmodium Vivax Isolates in Vietnam [NCT01887821]Phase 4330 participants (Actual)Interventional2013-02-28Completed
A Multi-site Cohort Observational Study for Molecular Assessment of Artemisinin Resistance Falciparum Malaria in Myanmar [NCT02792816]550 participants (Actual)Observational2009-06-30Completed
Chemoprevention With Monthly IPTp With Dihydroartemisinin-piperaquine for Malaria in HIV-infected Pregnant Participants on Daily Cotrimoxazole in Kenya and Malawi: a Multi-centre Placebo-controlled Trial [NCT04158713]Phase 3898 participants (Actual)Interventional2019-11-11Completed
Evaluation of the Safety of Primaquine in Combination With Dihydroartemisinin-piperaquine in G6PD Deficient Males in The Gambia [NCT02654730]Phase 2/Phase 361 participants (Actual)Interventional2015-12-31Terminated(stopped due to Enrollment took longer than anticipated; it was financially and logistically impossible to recruit the final cohort (G6PDd 0.4mg/kg PQ).)
Defining Effective, Appropriate, Implementable Strategies for Malaria Elimination in Military Forces in Cambodia as a Model for Mobile Populations [NCT02653898]Phase 41,050 participants (Actual)Interventional2016-01-31Active, not recruiting
Randomized Clinical Trial of the Efficacy and Safety of Dihydroartimisinine+Papiraquine (Artekin) Compared With First Line Drugs for Treatment of Vivax and Uncomplicated Falciparum Malaria in Afghanistan [NCT00682578]Phase 31,086 participants (Actual)Interventional2007-07-31Completed
IPT in Schoolchildren: Comparison of the Efficacy, Safety, and Tolerability of Antimalarial Regimens in Uganda [NCT00852371]Phase 3760 participants (Actual)Interventional2008-02-29Completed
Effectiveness and Safety of Artemether + Lumefantrine and Dihydroartemisinin + Piperaquine for the Treatment of Uncomplicated Malaria in Guinea-Bissau [NCT04897919]Phase 4474 participants (Actual)Interventional2015-08-01Completed
Malaria Chemoprevention With Monthly Treatment With Dihydroartemisinin-piperaquine for the Post-discharge Management of Severe Anaemia in Children Aged Less Than 5 Years in Uganda and Kenya: A Two-arm Randomised Placebo Controlled Trial [NCT02671175]Phase 31,049 participants (Actual)Interventional2016-05-20Completed
Enhancing Immunity to Malaria in Young Children With Effective Chemoprevention [NCT04978272]Phase 3924 participants (Actual)Interventional2022-02-08Active, not recruiting
A Multi-Site, Open-Label, Randomized Trial to Assess the Efficacy, Safety, and Tolerability of Dihydroartemisinin-Piperaquine Plus Mefloquine Compared to Dihydroartemisinin-Piperaquine or Artesunate-Mefloquine in Patients With Uncomplicated Falciparum Mal [NCT02612545]Phase 1216 participants (Actual)Interventional2015-11-20Completed
Safe and Efficacious Artemisinin-based Combination Treatments for African Pregnant Women With Malaria [NCT00852423]Phase 33,428 participants (Actual)Interventional2010-06-30Completed
The Efficacy and Safety of Pyronaridine-artesunate Combined With Low Dose Primaquine for Preventing Transmission of P. Falciparum Gametocytes in Sub-Saharan Africa [NCT04049916]Phase 2/Phase 3100 participants (Actual)Interventional2019-09-12Completed
[NCT01075945]Phase 4140 participants (Anticipated)Interventional2010-02-28Recruiting
Efficacy and Safety of Artemether-Lumefantrine and Dihydroartemisinin-Piperaquine for the Treatment of Uncomplicated Plasmodium Falciparum Malaria Among Children in the North Region of Cameroon [NCT05340153]Phase 4184 participants (Anticipated)Interventional2022-04-11Not yet recruiting
Electrocardiographic Safety Evaluation of Monthly Dihydroartemisinin-Piperaquine for the Use in Mass Treatment Campaigns to Block Malaria Transmission [NCT02605720]Phase 378 participants (Actual)Interventional2015-09-30Completed
In-vivo Efficacy and Safety of Artemether/Lumefantrine Vs Dihydroartemisinin-piperaquine for Treatment of Uncomplicated Malaria and Assessment of Parasite Genetic Factors Associated With Parasite Clearance or Treatment Failure [NCT02590627]Phase 4509 participants (Actual)Interventional2014-05-31Completed
Impact of Mass Screening and Selective Treatment With Dihydroartemisinin-piperaquine Plus Primaquine on Malaria Transmission in High Endemic Area, Belu Regency, Nusa Tenggara Timur Province, Indonesia: a Randomized Cluster Trial [NCT01878357]Phase 41,488 participants (Actual)Interventional2013-06-30Completed
Safety, Tolerability, Pharmacokinetics and Efficacy, Phase Iv, Open Label Study of Fixed Arco® and Eurartesim® Therapies in Adults and Children With Uncomplicated P. Falciparum Malaria in Tanzania [NCT01930331]Phase 460 participants (Actual)Interventional2014-01-07Completed
Interactions Between HIV and Malaria in African Children [NCT00527800]Phase 3351 participants (Actual)Interventional2007-08-31Completed
Efficacy and Safety of the Dispersible Formulation of Artemether-lumefantrine, Co-formulated Artesunate-amodiaquine and Co-formulated Dihydroartemisinin-piperaquine for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in Machinga District, Mal [NCT01326754]498 participants (Actual)Interventional2011-08-31Completed
Single Low Dose Tafenoquine to Reduce P. Falciparum Transmission in Mali (NECTAR2) [NCT04609098]Phase 280 participants (Actual)Interventional2020-10-29Completed
Effectiveness of Dihydroartemisinin-piperaquine as Seasonal Malaria Chemoprophylaxis in Extended High Transmission Settings of Tanzania: an Open Cluster Randomized Clinical Trial. [NCT05874869]13,800 participants (Actual)Interventional2020-07-01Completed
A Phase II, Open-label, Multicentre, Pharmacokinetic, Pharmacodynamics and Safety Study of a New Paediatric Eurartesim Dispersible Formulation and Crushed Film Coated Eurartesim Tablet, in Infant Patients With P. Falciparum Malaria [NCT01992900]Phase 2300 participants (Actual)Interventional2013-11-30Completed
Intermittent Screening and Treatment for the Control of Malaria in the First Year of Life in Papua, Indonesia: A Cluster Randomized Controlled Trial [NCT02001428]757 participants (Actual)Interventional2014-07-21Completed
'SCHOOL-BASED TREATMENT WITH ACT TO REDUCE TRANSMISSION' (START-IPT): Evaluation of the Community Impact of Intermittent Preventive Treatment for Malaria in Ugandan Children: a Cluster Randomised Trial [NCT02009215]Phase 410,746 participants (Actual)Interventional2014-02-28Completed
Comparison of Safety, Tolerability and Efficacy of Three Drug Combinations for Intermittent Preventive Treatment in Children Aged 1-5 Years in an Area of Seasonal Malaria Transmission in Upper River Division, The Gambia [NCT00561899]Phase 2/Phase 31,295 participants (Actual)Interventional2007-08-31Completed
Randomised Parallel Open Label Comparison Between 7 and 14 Day Primaquine Combined With 3-day Dihydroartemisinin-piperaquine or 3-day Chloroquine Regimens for Radical Cure of Plasmodium Vivax [NCT01640574]Phase 3680 participants (Actual)Interventional2012-02-29Completed
IPTp With Dihydroartemisinin-piperaquine and Azithromycin for Malaria, Sexually Transmitted and Reproductive Tract Infections in Pregnancy in High Sulphadoxine-pyrimethamine Resistance Areas in Kenya, Malawi and Tanzania [NCT03208179]Phase 34,680 participants (Actual)Interventional2018-03-29Completed
Effect of Imatinib on Suppression of Malaria Parasites in Patients With Uncomplicated Plasmodium Falciparum Malaria [NCT02614404]Phase 115 participants (Actual)Interventional2015-11-30Completed
Reactive Household-based Self-administered Treatment Against Residual Malaria Transmission: a Cluster Randomized Trial [NCT02878200]2,236 participants (Actual)Interventional2016-11-04Completed
Efficacy, Safety, and Pharmacokinetics of Sulphadoxine-pyrimethamine-amodiaquine (SP-AQ), SP-AQ Plus Primaquine, Dihydroartemisinin-piperaquine (DP), DP Plus Methylene Blue for Preventing Transmission of P. Falciparum Gametocytes in Mali [NCT02831023]Phase 280 participants (Actual)Interventional2016-07-31Completed
Evaluation of Impact Dihydroartemisinin-piperaquine Plus Primaquine on Malaria Transmission in Lempasing Village, Lampung Province, Southern Sumatra [NCT01389557]Phase 477 participants (Actual)Interventional2011-02-28Completed
Effectiveness of Dihydroartemisinin-piperaquine With or Without Primaquine on Gametocytes Plasmodium Falciparum in Mesoendemic Area of Indonesia [NCT01392014]Phase 4374 participants (Actual)Interventional2008-12-31Completed
Evaluation of the Implementation and Effectiveness of Intermittent Preventive Treatment for Malaria Using Dihydroartemisinin-piperaquine on Reducing Malaria Burden in School Aged Children in Tanzania [NCT04245033]Phase 44,100 participants (Actual)Interventional2020-07-20Active, not recruiting
A Randomised Open Label Trial Comparing Standard Dose of Dihydroartemisinin-piperaquine, Standard Fixed Artesunate-mefloquine Regimen and a Longer Regimen of Artemether-lumefantrine in the Treatment of Uncomplicated Malaria in Pregnancy [NCT01054248]Phase 3511 participants (Actual)Interventional2010-02-16Completed
Effectiveness of Momordica Charantia Extract Compared to the Standard Antimalarial Drug Combination Dihydroartemisinin Piperaquine-primaquine in Patients With Uncomplicated Falciparum Malaria, in Sumba Barat Daya District of Indonesia [NCT05829187]Phase 236 participants (Actual)Interventional2022-11-01Completed
Targeted Chemo-elimination (TCE) to Eradicate Malaria in Areas of Suspected or Proven Artemisinin Resistance in Southeast Asia and South Asia [NCT01872702]8,000 participants (Actual)Interventional2013-04-30Completed
Does Artemisinin Combination Treatment Reduce the Radical Curative Efficacy of High Dose Tafenoquine for Plasmodium Vivax Malaria? [NCT05788094]Phase 4388 participants (Anticipated)Interventional2023-06-26Recruiting
Mass Drug Administration of Monthly DHA-PQP to Accelerate Towards Malaria Elimination in Magude District, Southern Mozambique [NCT02914145]240,502 participants (Actual)Interventional2015-11-30Completed
Efficacy of Artemether Lumefantrine (AL) and Dihydroartemisinin-Piperaquine (DHP) for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in Siaya and Bungoma Counties, Kenya [NCT04767191]Phase 4400 participants (Actual)Interventional2021-03-15Completed
Cardiac Safety of Dihydroartemisinin-Piperaquine Amongst Pregnant Women in Tanzania [NCT02909712]Phase 2201 participants (Actual)Interventional2016-09-30Completed
Evaluation of the Safety and Efficacy of Dihydroartemisinin-piperaquine for Intermittent Preventive Treatment of Malaria in HIV-infected Pregnant Women [NCT03671109]Phase 3666 participants (Actual)Interventional2019-09-18Completed
Efficacy and Safety of Artemether + Lumefantrine and Dihydroartemisinin + Piperaquine for the Treatment of Uncomplicated Malaria in Guinea-Bissau. [NCT01704508]Phase 4346 participants (Actual)Interventional2012-11-30Completed
Randomized Trial of Effectiveness and Acceptability of Three Alternative Regimens for Malaria Seasonal Intermittent Preventive Treatment in Senegal [NCT00529620]Phase 31,833 participants (Actual)Interventional2007-09-30Completed
Efficacy and Safety of Artesunate-amodiaquine, Artemether-lumefantrine and Dihydroartemisinine-piperaquine in the Treatment of Uncomplicated Plasmodium Falciparum Malaria in the Democratic Republic of Congo: a Randomized Controlled Trial [NCT02940756]Phase 41,615 participants (Actual)Interventional2017-03-15Completed
Preventing Malaria in School Children to Protect the Whole Community in Rural Blantyre District, Malawi [NCT06083688]Phase 41,000 participants (Anticipated)Interventional2024-10-31Not yet recruiting
Phase III Study to Study the Clinical Response to ACT Fixed Dose Combination in 42 Days in Uncomplicated Malaria in Cameroon [NCT01845701]Phase 3720 participants (Actual)Interventional2010-03-31Completed
An Individually Randomised Trial of Seasonal Malaria Chemoprevention Versus a Long-acting Artemisinin Combination Therapy for the Prevention of Malaria and Anaemia in Children Living in an Area of Extended Seasonal Transmission in Ghana. [NCT01651416]Phase 42,400 participants (Actual)Interventional2012-07-31Completed
Evaluation of a Pilot Implementation of Intermittent Preventive Treatment With Dihydroartemisinin-piperaquine to Prevent Adverse Birth Outcomes in Papua, Indonesia [NCT05294406]Phase 41,420 participants (Anticipated)Interventional2022-02-07Active, not recruiting
Phase 2a Dose Escalation Study of the Efficacy, Safety, and Pharmacokinetics of Low Dose Primaquine for Gametocytocidal Activity Against P. Falciparum in Sub-Saharan Africa and South East Asia [NCT01743820]Phase 281 participants (Actual)Interventional2013-09-30Completed
Efficacy of Artesunate-amodiaquine, Dihydroartemisinin-piperaquine and Artemether-lumefantrine Combination Therapies for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in Children Aged 6 to 59 Months in Maradi, Niger 2012-13 [NCT01755559]Phase 4663 participants (Actual)Interventional2013-06-30Completed
Study 200894: A Double-blind, Double-dummy, Randomized, Parallel Group, Placebo-controlled Superiority Study to Evaluate the Efficacy and Safety of Tafenoquine (SB-252263, WR238605) Co-administered With Dihydroartemisinin-piperaquine (DHA-PQP) for the Rad [NCT02802501]Phase 3150 participants (Actual)Interventional2018-04-08Completed
Evaluation of Community-based Screening and Treatment for Malaria in the KEMRI/CDC Health and Demographic Surveillance System (HDSS) in Western Kenya [NCT02987270]Phase 390,000 participants (Actual)Interventional2013-04-30Completed
Adjunctive Ivermectin Mass Drug Administration for Malaria Control on the Bijagos Archipelago of Guinea Bissau: A Cluster-randomized Placebo-controlled Trial [NCT04844905]Phase 324,000 participants (Anticipated)Interventional2021-05-03Recruiting
Evaluation of Three Artemisinin-based Combinations for the Treatment of Uncomplicated Malaria in Childreen in Burkina Faso (CHIMIO2) [NCT04778813]Phase 41,050 participants (Anticipated)Interventional2021-06-01Not yet recruiting
Assessment of Antimalaria Drugs Susceptibility Testing for an Effective Management of Infected Patients in Sub-Sahara Africa [NCT02974348]Phase 3300 participants (Actual)Interventional2013-01-31Completed
Randomized Open-label Trial of Comparison Between DHA-Piperaquine and Mefloquine Artesunate Combinations 3 Day-regimens for the Treatment of Uncomplicated Plasmodium Falciparum Malaria on the Thai-Myanmar Border (RDM) [NCT01640587]76 participants (Actual)Interventional2013-11-30Terminated(stopped due to No adequate malaria patient)
Clinical Trial to Evaluate Intermittent Screening and Treatment and Intermittent Preventive Treatment of Malaria in Asymptomatic Schoolchildren to Decrease P. Falciparum Infection and Transmission [NCT05244954]Phase 4746 participants (Actual)Interventional2022-02-01Completed
A Prospective Randomized Open-Label Study on the Efficacy and Safety of Intermittent Preventive Treatment in Pregnancy (IPTp) With Dihydroartemisinin-Piperaquine (DP) Versus IPTp With Sulfadoxine-Pyrimethamine (SP) in Malawi [NCT03009526]Phase 3602 participants (Actual)Interventional2017-01-17Completed
Mass Drug Administration With Dihydroartemisinin-piperaquine and Primaquine to Reduce Malaria in a Moderate-low Transmission Setting in Senegal: A Cluster Randomized Controlled Trial [NCT04864444]10,715 participants (Actual)Interventional2021-06-19Completed
A Hybrid Effectiveness-implementation Study to Assess the Effectiveness and Chemoprevention Efficacy of Implementing Seasonal Malaria Chemoprevention in Five Districts in Karamoja Region, Uganda [NCT05323721]Phase 46,805 participants (Actual)Interventional2022-06-01Active, not recruiting
Efficacy and Safety of Dihydroartemisinin-piperaquine for the Treatment of Uncomplicated Plasmodium Falciparum and Plasmodium Vivax Malaria in Timika, Indonesia [NCT02353494]130 participants (Actual)Observational2015-03-31Completed
Boosting the Impact of Seasonal Malaria Chemoprevention (SMC) Through Simultaneous Screening and Treatment of SMC-Children's Roommates in Burkina Faso [NCT04816461]Phase 4789 participants (Anticipated)Interventional2021-07-31Not yet recruiting
Enhancing Preventive Therapy of Malaria In Children With Sickle Cell Anemia in East Africa (EPiTOMISE) [NCT03178643]Phase 4246 participants (Actual)Interventional2018-01-23Completed
Evaluation of the Efficacy of Artemisinin Combination Therapy in Kenya [NCT01899820]Phase 32,100 participants (Anticipated)Interventional2013-04-30Active, not recruiting
Field Study of the Pharmacokinetics and Pharmacodynamics of Artemisinin-based Combination Therapy for Gametocyte Clearance and Post-treatment Chemoprotection in Zambian Children With Uncomplicated Falciparum Malaria [NCT04009343]Phase 2/Phase 3182 participants (Anticipated)Interventional2019-06-19Active, not recruiting
Efficacy and Safety of High-dose Ivermectin for Reducing Malaria Transmission: A Dose Finding Study (IVERMAL) [NCT02511353]Phase 2141 participants (Actual)Interventional2015-07-31Completed
Reducing the Burden of Malaria in HIV-uninfected Pregnant Women and Infants (PROMOTE Birth Cohort 1) [NCT02163447]Phase 3300 participants (Actual)Interventional2014-06-23Completed
Reducing the Burden of Malaria in HIV-Infected Pregnant Women and Their HIV-Exposed Children (PROMOTE Birth Cohort 2) [NCT02282293]Phase 3200 participants (Actual)Interventional2014-12-09Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00948896 (4) [back to overview]Incidence of Any Adverse Events Defined as Severity Grade 3-4 That Are Possibly, Probably, or Definitely Related to Study Drugs
NCT00948896 (4) [back to overview]Incident Malaria Cases Per Person Year at Risk in HIV-unexposed Participants
NCT00948896 (4) [back to overview]Rebound Incidence of Malaria Defined as the Number of Treatments for New Episodes of Malaria Per Time at Risk
NCT00948896 (4) [back to overview]Incident Malaria Cases Per Person Year at Risk in HIV-exposed Participants
NCT02163447 (14) [back to overview]Prevalence of Parasitemia in Infants
NCT02163447 (14) [back to overview]Prevalence of Parasitemia at the Time of Monthly Routine Visits During Pregnancy
NCT02163447 (14) [back to overview]Prevalence of Gametocytemia in Pregnant Women
NCT02163447 (14) [back to overview]Prevalence of Gametocytemia in Infants
NCT02163447 (14) [back to overview]Number of Participants With Maternal Blood Samples Positive for Parasites by Microscopy and LAMP at Delivery
NCT02163447 (14) [back to overview]Prevalence of Anemia in Pregnant Women
NCT02163447 (14) [back to overview]Number of Participants With One or More Birth Outcomes: Congenital Malformations, Spontaneous Abortion, LBW (<2500g), Still Birth, Pre-term Delivery
NCT02163447 (14) [back to overview]Incidence of Malaria in Pregnant Women
NCT02163447 (14) [back to overview]Incidence of Malaria in Infants
NCT02163447 (14) [back to overview]Incidence of Malaria in Infants
NCT02163447 (14) [back to overview]Incidence of Hospital Admissions in Infants
NCT02163447 (14) [back to overview]Incidence of Complicated Malaria in Infants
NCT02163447 (14) [back to overview]Prevalence of Placental Malaria
NCT02163447 (14) [back to overview]Number of Participants With Blood Samples Positive for Parasites by Microscopy or LAMP
NCT02282293 (7) [back to overview]Composite Adverse Birth Outcome (Proportion With Low Birth Weight (<2500 gm), Spontaneous Abortion (<28 Weeks), Stillbirth (Fetal Demise ≥28 Weeks), Congenital Anomaly, or Preterm Delivery (<37 Weeks)
NCT02282293 (7) [back to overview]Incidence of Malaria, Pregnant Women
NCT02282293 (7) [back to overview]Number of Monthly Routine Visits With Positive Blood Samples for Parasites
NCT02282293 (7) [back to overview]Number of Participants With Placental Malaria
NCT02282293 (7) [back to overview]Number of Routine Visits Measured Every 8 Weeks During Pregnancy for Which the Participants Had Anemia
NCT02282293 (7) [back to overview]Maternal Parasitemia at Delivery by Microscopy and LAMP
NCT02282293 (7) [back to overview]Placental Parasitemia (Number of Women With Placental Blood Samples Positive for Malaria by Microscopy or PCR)
NCT02793622 (14) [back to overview]Prevalence of Maternal Malaria
NCT02793622 (14) [back to overview]Prevalence of Placental Malaria by Histology
NCT02793622 (14) [back to overview]Prevalence of Placental Parasitemia
NCT02793622 (14) [back to overview]Prevalence of Anemia in Infants
NCT02793622 (14) [back to overview]Incidence of Complicated Malaria in Infants
NCT02793622 (14) [back to overview]Incidence of Hospital Admissions in Infants
NCT02793622 (14) [back to overview]Incidence of Malaria in Infants
NCT02793622 (14) [back to overview]Infant Mortality Rate
NCT02793622 (14) [back to overview]Mean Gestational Age in Weeks at Birth
NCT02793622 (14) [back to overview]Number of Participants Who Deliver With a Composite Adverse Birth Outcome
NCT02793622 (14) [back to overview]Number of Participants With Adverse Events
NCT02793622 (14) [back to overview]Prevalence of Anemia in Pregnant Women
NCT02793622 (14) [back to overview]Prevalence of Asymptomatic Parasitemia in Infants
NCT02793622 (14) [back to overview]Prevalence of Asymptomatic Parasitemia in Pregnant Women
NCT02802501 (20) [back to overview]Change From Baseline in Methemoglobin/ Total Hemoglobin
NCT02802501 (20) [back to overview]Time to Relapse of P. Vivax Malaria
NCT02802501 (20) [back to overview]Time to Parasite Clearance
NCT02802501 (20) [back to overview]Time to Fever Clearance
NCT02802501 (20) [back to overview]Percentage of Participants With Relapse-free Efficacy at Six Months After Administration of Tafenoquine With DHA-PQP and Primaquine+DHA-PQP
NCT02802501 (20) [back to overview]Percentage of Participants With Relapse-free Efficacy at Six Months After Administration of Tafenoquine With DHA-PQP and DHA-PQP Alone
NCT02802501 (20) [back to overview]Percentage of Participants With Relapse-free Efficacy at Six Months After Administration of Primaquine With DHA-PQP and DHA-PQP Alone
NCT02802501 (20) [back to overview]Percentage of Participants With Relapse-free Efficacy at Four Months After Administration of Tafenoquine With DHA-PQP and DHA-PQP Alone
NCT02802501 (20) [back to overview]Number of Participants With Recrudescence
NCT02802501 (20) [back to overview]Number of Participants With Electrocardiogram (ECG) Values Outside Clinical Concern Range-QT Interval Corrected Using Fredericia's Formula (QTcF)
NCT02802501 (20) [back to overview]Number of Participants With Chemistry Values Outside Clinical Concern Range
NCT02802501 (20) [back to overview]Number of Participants With Gastrointestinal AEs
NCT02802501 (20) [back to overview]Number of Participants With Any Adverse Events (AEs) and Serious Adverse Events (SAEs) During the Double-blind Treatment Phase
NCT02802501 (20) [back to overview]Number of Participants With Hematology Values Outside Clinical Concern Range
NCT02802501 (20) [back to overview]Number of Participants With Protocol-defined SAE (Hemoglobin Drop)
NCT02802501 (20) [back to overview]Number of Participants With Worst Case Body Temperature Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT02802501 (20) [back to overview]Number of Participants With Worst Case Pulse Rate Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT02802501 (20) [back to overview]Number of Participants With Worst Case Respiratory Rate Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT02802501 (20) [back to overview]Number of Participants With Worst Case Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT02802501 (20) [back to overview]Change From Baseline in QT Interval Corrected by Fridericia's Formula (QTcF)
[back to top]

Incident Malaria Cases Per Person Year at Risk in HIV-unexposed Participants

The incidence of malaria, defined as the number of incident episodes per time at risk, during the period the intervention was given (6-24 mo of age). Treatments within 14d of a prior episode were not considered incident events. Time at risk was from the day following the initiation of study drugs to the last day of observation, minus 14 d after each treatment for malaria. (NCT00948896)
Timeframe: 6 to 24 months of age

,,,
InterventionEpisode per person year at risk (Number)
6-24 mo. of Age6-11 mo. of Age12-24 mo. of Age
HIV-unexposed & Daily TS5.213.276.32
HIV-unexposed & Monthly DP3.021.493.88
HIV-unexposed & Monthly SP6.735.517.41
HIV-unexposed & no Chemoprevention6.956.417.24

[back to top]

Rebound Incidence of Malaria Defined as the Number of Treatments for New Episodes of Malaria Per Time at Risk

(NCT00948896)
Timeframe: 24 months to 36 months of age

,,,,,,,
InterventionIncidence per person year at risk (Number)
All incident episodes of malariaComplicated malariaAll-cause hospital admissions
HIV-exposed & Daily TS8.130.1160.186
HIV-exposed & Monthly DP6.780.0440.089
HIV-exposed & Monthly SP6.750.1470.318
HIV-exposed & no Chemoprevention9.080.1610.459
HIV-unexposed & Daily TS10.900.0460.091
HIV-unexposed & Monthly DP10.7700.023
HIV-unexposed & Monthly SP11.980.1320.452
HIV-unexposed & no Chemoprevention10.850.0460.046

[back to top]

Incident Malaria Cases Per Person Year at Risk in HIV-exposed Participants

The primary outcome was the incidence of malaria, defined as the number of incident episodes per time at risk, during the period the intervention was given. Treatments within 14 days of a prior episode were not considered incident events. Time at risk was from the day following the initiation of study drugs to the last day of observation, minus 14 days after each treatment for malaria. (NCT00948896)
Timeframe: Randomization to 24 months of age

,,,
InterventionEpisodes per person year at risk (Number)
Randomization - 24 mo. of AgeRandomization -16 mo. of Age17-24 mo. of Age
HIV-exposed & Daily TS2.861.703.79
HIV-exposed & Monthly DP1.830.902.67
HIV-exposed & Monthly SP4.503.725.22
HIV-exposed & no Chemoprevention6.285.427.04

[back to top]

Prevalence of Parasitemia in Infants

Proportion of routine monthly samples positive for parasites by LAMP. Proportion of routine samples (LAMP or blood smears) positive for asexual parasites. (NCT02163447)
Timeframe: Birth up to 24 months of age or early study termination

InterventionPositive blood smears (Number)
3 Dose SP Pregnancy / 3 Monthly DP Infancy59
3 Dose DP Pregnancy / 3 Monthly DP Infancy25
3 Dose DP Pregnancy / Monthly DP Infancy7
Monthly DP Pregnancy / 3 Monthly DP Infancy52
Monthly DP Pregnancy / Monthly DP Infancy4

[back to top]

Prevalence of Parasitemia at the Time of Monthly Routine Visits During Pregnancy

Detection of malaria parasites by LAMP during pregnancy (NCT02163447)
Timeframe: After first dose of study drug through delivery or early termination

InterventionPositive specimens (Number)
Mothers - 3 Dose SP206
Mothers - 3 Dose DP74
Mothers - Monthly DP26

[back to top]

Prevalence of Gametocytemia in Pregnant Women

Proportion of urgent blood smears positive for gametocytes (NCT02163447)
Timeframe: Gestational age between 12-20 weeks (at study entry) up to delivery

InterventionPositive blood smears (Number)
Mothers - 3 Dose SP4
Mothers - 3 Dose DP1
Mothers - Monthly DP3

[back to top]

Prevalence of Gametocytemia in Infants

Proportion of routine blood smears positive for gametocytes (NCT02163447)
Timeframe: Birth up to 24 months of age or early study termination

InterventionPositive blood smears (Number)
3 Dose SP Pregnancy / 3 Monthly DP Infancy7
3 Dose DP Pregnancy / 3 Monthly DP Infancy1
3 Dose DP Pregnancy / Monthly DP Infancy0
Monthly DP Pregnancy / 3 Monthly DP Infancy4
Monthly DP Pregnancy / Monthly DP Infancy0

[back to top]

Number of Participants With Maternal Blood Samples Positive for Parasites by Microscopy and LAMP at Delivery

Prevalence of maternal parasitemia at delivery by microscopy and LAMP (NCT02163447)
Timeframe: At delivery

,,
Interventionparticipants (Number)
MicroscopyLAMP
Mothers - 3 Dose DP13
Mothers - 3 Dose SP525
Mothers - Monthly DP01

[back to top]

Prevalence of Anemia in Pregnant Women

Prevalence of routine hemoglobin measurements < 11 g/dL (NCT02163447)
Timeframe: After first dose of study drugs up to delivery or early termination

Interventionhemoglobin measurements taken every 12wk (Number)
Mothers - 3 Dose SP94
Mothers - 3 Dose DP72
Mothers - Monthly DP61

[back to top]

Number of Participants With One or More Birth Outcomes: Congenital Malformations, Spontaneous Abortion, LBW (<2500g), Still Birth, Pre-term Delivery

Congenital malformations, spontaneous abortion, LBW (<2500g), still birth, pre-term delivery (NCT02163447)
Timeframe: Delivery

InterventionParticipants (Count of Participants)
Mothers - 3 Dose SP19
Mothers - 3 Dose DP19
Mothers - Monthly DP9

[back to top]

Incidence of Malaria in Pregnant Women

Incidence of malaria, defined as the number of incident episodes per time at risk. Incident cases will include all treatments for malaria not proceeded by another treatment in the previous 14 days. (NCT02163447)
Timeframe: Time at risk will begin after first dose of study drug and will end when study participants deliver or early study termination

Interventionevents per person years (Number)
Mothers - 3 Dose SP0.95
Mothers - 3 Dose DP0.31
Mothers - Monthly DP0

[back to top]

Incidence of Malaria in Infants

Incident cases will include all treatments for malaria not proceeded by another treatment in the previous 14 days. The study investigators will test the hypotheses that A) infants born to mothers randomized to receive IPTp with 3 dose DP or monthly DP will have a lower incidence of malaria during the first 24 months of life compared to infants born to mothers who were randomized to receive IPTp with 3 doses of SP, and, B) infants randomized to receive monthly DP between 2-24 months of age will have a lower incidence of malaria between 24-36 months of age after the intervention is stopped compared to infants randomized q 3 monthly DP between 2-24 months of age. (NCT02163447)
Timeframe: Time at risk will begin at birth and will end when study participants reaches 24 months of age or early study termination (if prior to 24 months of age)

InterventionEvents per person years (Number)
3 Dose SP Pregnancy / 3 Monthly DP Infancy0.26
3 Dose DP Pregnancy / 3 Monthly DP Infancy0.30
3 Dose DP Pregnancy / Monthly DP Infancy0.00
Monthly DP Pregnancy / 3 Monthly DP Infancy0.43
Monthly DP Pregnancy / Monthly DP Infancy0.03

[back to top]

Incidence of Malaria in Infants

Incident cases will include all treatments for malaria not proceeded by another treatment in the previous 14 days. The study investigators will test the hypotheses that A) infants born to mothers randomized to receive IPTp with 3 dose DP or monthly DP will have a lower incidence of malaria during the first 24 months of life compared to infants born to mothers who were randomized to receive IPTp with 3 doses of SP, and, B) infants randomized to receive monthly DP between 2-24 months of age will have a lower incidence of malaria between 24-36 months of age after the intervention is stopped compared to infants randomized q 3 monthly DP between 2-24 months of age. (NCT02163447)
Timeframe: Time at risk will begin at 24 months of age and will end when study participants reaches 36 months of age or termination

InterventionEvents per person years (Number)
3 Dose SP Pregnancy / 3 Monthly DP Infancy0.87
3 Dose DP Pregnancy / 3 Monthly DP Infancy0.88
3 Dose DP Pregnancy / Monthly DP Infancy0.83
Monthly DP Pregnancy / 3 Monthly DP Infancy1.24
Monthly DP Pregnancy / Monthly DP Infancy0.64

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Incidence of Hospital Admissions in Infants

Admission to a hospital for pediatric inpatient care for any reason (NCT02163447)
Timeframe: Birth up to 24 months of age or early study termination

InterventionEvents per person years (Number)
3 Dose SP Pregnancy / 3 Monthly DP Infancy0.043
3 Dose DP Pregnancy / 3 Monthly DP Infancy0.036
3 Dose DP Pregnancy / Monthly DP Infancy0.089
Monthly DP Pregnancy / 3 Monthly DP Infancy0.082
Monthly DP Pregnancy / Monthly DP Infancy0.043

[back to top]

Incidence of Complicated Malaria in Infants

Any treatment for malaria meeting criteria for severe malaria or danger signs (NCT02163447)
Timeframe: Birth up to 24 months of age or early study termination

InterventionEvents per person years (Number)
3 Dose SP Pregnancy / 3 Monthly DP Infancy0.022
3 Dose DP Pregnancy / 3 Monthly DP Infancy0.024
3 Dose DP Pregnancy / Monthly DP Infancy0.000
Monthly DP Pregnancy / 3 Monthly DP Infancy0.035
Monthly DP Pregnancy / Monthly DP Infancy0.000

[back to top]

Prevalence of Placental Malaria

Prevalence of placental malaria based on placental histopathology dichotomized into any evidence of placental infection (parasites or pigment) vs. no evidence and by histopathology as a categorical variable based on Rogerson et al criteria. (NCT02163447)
Timeframe: Delivery

InterventionParticipants (Count of Participants)
Mothers - 3 Dose SP49
Mothers - 3 Dose DP30
Mothers - Monthly DP26

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Number of Participants With Blood Samples Positive for Parasites by Microscopy or LAMP

Prevalence of placental blood samples positive for parasites by microscopy or LAMP (NCT02163447)
Timeframe: Delivery

,,
InterventionParticipants (Count of Participants)
Micropscopic assessment of placental bloodLAMP assessment of placental blood
Mothers - 3 Dose DP33
Mothers - 3 Dose SP519
Mothers - Monthly DP02

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Composite Adverse Birth Outcome (Proportion With Low Birth Weight (<2500 gm), Spontaneous Abortion (<28 Weeks), Stillbirth (Fetal Demise ≥28 Weeks), Congenital Anomaly, or Preterm Delivery (<37 Weeks)

Proportion with low birth weight (<2500 gm), spontaneous abortion (<28 weeks), stillbirth (fetal demise ≥28 weeks), congenital anomaly, or preterm delivery (<37 weeks) (NCT02282293)
Timeframe: At delivery

InterventionParticipants (Count of Participants)
TS + DP Placebo Pregnancy15
Daily TS + Monthly DP Pregnancy20

[back to top]

Incidence of Malaria, Pregnant Women

The primary outcome will be the incidence of malaria, defined as the number of incident episodes per time at risk. Incident cases will include all treatments for malaria not proceeded by another treatment in the previous 14 days. (NCT02282293)
Timeframe: Time at risk will begin following administration of first dose of study drug to delivery

InterventionEvents per person-year (Number)
TS + DP Placebo Pregnancy0.03
Daily TS + Monthly DP Pregnancy0.00

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Number of Monthly Routine Visits With Positive Blood Samples for Parasites

Proportion of monthly routine blood samples positive by LAMP for parasites (NCT02282293)
Timeframe: Following administration of first dose of study drug to delivery

Interventionvisits with positive blood sample (Count of Units)
TS + DP Placebo Pregnancy12
Daily TS + Monthly DP Pregnancy5

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Number of Participants With Placental Malaria

The primary outcome will be the prevalence of placental malaria based on placental histopathology and dichotomized into any evidence of placental infection (parasites or pigment) vs. no evidence of placental infection. (NCT02282293)
Timeframe: at delivery estimated to be within 10 to 30 weeks of study entry

InterventionParticipants (Count of Participants)
TS + DP Placebo Pregnancy3
Daily TS + Monthly DP Pregnancy6

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Number of Routine Visits Measured Every 8 Weeks During Pregnancy for Which the Participants Had Anemia

Anemia (hemoglobin less than 11g/dL) measured every 8 weeks during pregnancy (NCT02282293)
Timeframe: Following administration of first dose of study drugs to delivery

InterventionRoutine visit done every 8 weeks (Count of Units)
TS + DP Placebo Pregnancy65
Daily TS + Monthly DP Pregnancy51

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Maternal Parasitemia at Delivery by Microscopy and LAMP

Proportion of women with parasitemia detected by microscopy or LAMP at delivery (NCT02282293)
Timeframe: At delivery

,
InterventionParticipants (Count of Participants)
MicroscopyLAMP
Daily TS + Monthly DP Pregnancy14
TS + DP Placebo Pregnancy02

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Placental Parasitemia (Number of Women With Placental Blood Samples Positive for Malaria by Microscopy or PCR)

Proportion of placental blood samples positive for malaria by microscopy or PCR (NCT02282293)
Timeframe: At delivery

,
InterventionParticipants (Count of Participants)
Microscopy of placental bloodLAMP analysis of placental blood
Daily TS + Monthly DP Pregnancy13
TS + DP Placebo Pregnancy01

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Prevalence of Maternal Malaria

Maternal blood positive for malaria parasites by microscopy. (NCT02793622)
Timeframe: Gestational age between 12-20 weeks (at study entry) up to delivery

InterventionParticipants (Count of Participants)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy28
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy1

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Prevalence of Placental Malaria by Histology

Any evidence of placental infection (parasites or pigment). Number of participants with placental tissue positive for malaria parasites or pigment. (NCT02793622)
Timeframe: Delivery

InterventionParticipants (Count of Participants)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy197
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy94

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Prevalence of Placental Parasitemia

Proportion of placental blood samples positive for parasites by Loop-mediated isothermal amplification (LAMP) or microscopy (NCT02793622)
Timeframe: Delivery

,
InterventionParticipants (Count of Participants)
LAMPMicroscopy
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy71
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy7129

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Prevalence of Anemia in Infants

"Defined as the proportion with hemoglobin < 10 g/dL measure routinely at 12, 28, and 52 weeks of age. Number of cases per person year (PPY).~This is a prevalence measure but are repeated measures during infancy. In other words we measured this outcome up to 3 times for each participant during infancy (at 12, 28 and 52 weeks of age)." (NCT02793622)
Timeframe: Birth up to 12 months of age or early termination

Interventionroutine hemoglobin measurement (Count of Units)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy222
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy216

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Incidence of Complicated Malaria in Infants

Complicated malaria defined as an episode of malaria with danger signs (any of the following: less than 3 convulsions over 24 h, inability to sit or stand, vomiting everything, unable to breastfeed or drink) or the meeting standardized criteria for severe malaria. (NCT02793622)
Timeframe: Birth up to 12 months of age or early termination

InterventionParticipants (Count of Participants)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy44
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy24

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Incidence of Hospital Admissions in Infants

Admission to the pediatric ward for any cause (NCT02793622)
Timeframe: Birth up to 12 months of age or early termination

InterventionParticipants (Count of Participants)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy19
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy8

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Incidence of Malaria in Infants

episodes per person year (NCT02793622)
Timeframe: Time at risk will begin at birth and end when study participants reaches 12 months of age or early study termination

Interventionepisodes per person year (Number)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy1.98
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy1.71

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Infant Mortality Rate

Any deaths occurring after birth (NCT02793622)
Timeframe: Birth up to 12 months of age

InterventionParticipants (Count of Participants)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy9
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy7

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Mean Gestational Age in Weeks at Birth

Gestational age in weeks determined by ultrasound dating (gold standard) and by the metabolic profiling outcome from biological specimens including placental tissue and placental blood. (NCT02793622)
Timeframe: At the time of delivery

Interventionweeks (Mean)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy39.4
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy39.6

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Number of Participants Who Deliver With a Composite Adverse Birth Outcome

Composite adverse birth outcome defined as any one of the following: 1) Low birth weight (< 2500 gm); 2) Preterm delivery (< 37 weeks gestational age); 3) Small for gestational age (< 10th percentile relative to an external growth reference) (NCT02793622)
Timeframe: Delivery

InterventionParticipants (Count of Participants)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy60
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy54

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Number of Participants With Adverse Events

All grade 3 and 4 adverse events (NCT02793622)
Timeframe: Starting at the time of their first study drug administration, approximately gestational age between 12-20 weeks, up to one month post-delivery

InterventionParticipants (Count of Participants)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy54
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy43

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Prevalence of Anemia in Pregnant Women

hemoglobin < 11 g/dL (NCT02793622)
Timeframe: Starting at the time of their first study drug administration, approximately gestational age between 12-20 weeks, up to one month post-delivery

InterventionParticipants (Count of Participants)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy28
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy8

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Prevalence of Asymptomatic Parasitemia in Infants

Proportion of routine monthly samples positive for parasites by microscopy and LAMP (NCT02793622)
Timeframe: Birth up to 12 months of age or early termination

Interventionblood smears (Count of Units)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy344
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy357

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Prevalence of Asymptomatic Parasitemia in Pregnant Women

Proportion of routine monthly samples positive for parasites by microscopy and LAMP (NCT02793622)
Timeframe: Starting at the time of their first study drug administration, approximately gestational age between 12-20 weeks, up to one month post-delivery

Interventionblood smears (Count of Units)
Monthly Sulfadoxine-Pyrimethamine (SP) During Pregnancy519
Monthly Dihydroartemisinin-Piperaquine (DP) During Pregnancy9

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Change From Baseline in Methemoglobin/ Total Hemoglobin

Blood samples were collected for the assessment of methemoglobin/Total Hemoglobin (Hb). Methemoglobin is a type of Hb in the form of metalloprotein that cannot bind with oxygen, measured as percentage of methemoglobin in total hemoglobin. Change from Baseline is calculated as Post-Dose Visit Value minus Baseline value. Day 1 was considered as Baseline. (NCT02802501)
Timeframe: Baseline (Day 1) and Days 2,3,4,5,6,7,8,9,10,11,12,13,14,15,16,18,20,21,22,24,26,28 and 60

,,
InterventionPercentage of Methemoglobin in total Hb (Mean)
Day 2, n=48, 50, 50Day 3, n=48, 50, 50Day 4, n=48, 50, 50Day 5, n=48, 50, 50Day 6, n=46, 49, 50Day 7, n=48, 50, 50Day 8, n=46, 48, 48Day 9, n=46, 47, 47Day 10, n=47, 45, 49Day 11, n=47, 44, 49Day 12, n=47, 47, 50Day 13, n=48, 48, 48Day 14, n=48, 50, 50Day 15, n=17, 22, 14Day 16, n=43, 48, 47Day 18, n=46, 48, 49Day 20, n=42, 49, 48Day 21, n=43, 48, 48Day 22, n=45, 49, 48Day 24, n=41, 46, 47Day 26, n=44, 45, 47Day 28, n=47, 50, 50Day 60, n=47, 50, 49
DHA-PQP Only-0.13-0.16-0.16-0.18-0.15-0.19-0.12-0.13-0.16-0.13-0.13-0.14-0.18-0.08-0.12-0.12-0.09-0.07-0.13-0.11-0.17-0.15-0.11
Primaquine+DHA-PQP-0.060.010.280.620.911.201.411.531.691.821.922.022.012.131.841.290.800.690.490.410.190.08-0.01
Tafenoquine+ DHA-PQP-0.07-0.040.060.120.160.190.230.240.240.180.180.180.120.000.120.110.060.030.010.030.030.01-0.07

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Time to Relapse of P. Vivax Malaria

Relapse is defined by a positive blood smear with or without vivax symptoms. Relapse is described as any recurrence of P. vivax malaria after clearance of the initial infection. The time to relapse (number of days between the date of first positive count and date of Study Day 1) was analyzed by the Kaplan-Meier method. The median number of days to relapse along with 95 percent (%) confidence interval (CI) has been presented for each treatment group. (NCT02802501)
Timeframe: Up to Day 180

InterventionDays (Median)
DHA-PQP Only81.5
Tafenoquine+ DHA-PQP96.0
Primaquine+DHA-PQPNA

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Time to Parasite Clearance

Parasite clearance time is defined as time needed to clear asexual parasite from the blood that is, parasite numbers falling below the limit of detection in the thick blood smear and remaining undetectable after >= 6 hours later. The time to achieve parasite clearance was analyzed by Kaplan-Meier method. (NCT02802501)
Timeframe: Up to Day 8

InterventionHours (Median)
DHA-PQP Only18.1
Tafenoquine+ DHA-PQP18.1
Primaquine+DHA-PQP18.0

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Time to Fever Clearance

Time to fever clearance is defined as time from first dose of treatment to the time when body temperature falls to normal and remains normal for at least 48 hours up to the Day 7 visit. Fever clearance is considered to have been achieved once an initial temperature of greater than 37.4 degree Celsius is reduced to a value less than or equal to 37.4 degree Celsius, in the absence of value greater than 37.4 degree Celsius in the following 48 hours up to Day 7 visit. The time taken to achieve fever clearance was analyzed by Kaplan-Meier method. (NCT02802501)
Timeframe: Up to Day 7

InterventionHours (Median)
DHA-PQP Only16.5
Tafenoquine+ DHA-PQP15.8
Primaquine+DHA-PQP16.8

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Percentage of Participants With Relapse-free Efficacy at Six Months After Administration of Tafenoquine With DHA-PQP and Primaquine+DHA-PQP

A participant was considered to have demonstrated relapse-free efficacy at 6 months if: a) Participant had non-zero P. vivax asexual parasite count at Baseline (Day 1), b) Participant demonstrated initial clearance of P.vivax parasitemia, c) Participant had no positive asexual P.vivax parasite count at any assessment prior to or on study Day 180 following initial parasite clearance, d) Participants did not take a concomitant medication with anti-malarial activity (excluding study treatment) at any point between Study Day 1 and their last parasite assessment, e) Participant was parasite-free at 6 months. The percentage of participants who were relapse-free at 6 months post dose has been presented. (NCT02802501)
Timeframe: 6 months post-dose

InterventionPercentage of participants (Number)
Tafenoquine+ DHA-PQP22
Primaquine+DHA-PQP52

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Percentage of Participants With Relapse-free Efficacy at Six Months After Administration of Tafenoquine With DHA-PQP and DHA-PQP Alone

A participant was considered to have demonstrated relapse-free efficacy at 6 months if: a) Participant had non-zero Plasmodium vivax (P.vivax) asexual parasite count at Baseline (Day 1), b) Participant demonstrated initial clearance of P.vivax parasitemia, c) Participant had no positive asexual P.vivax parasite count at any assessment prior to or on study Day 180 following initial parasite clearance, d) Participants did not take a concomitant medication with anti-malarial activity (excluding study treatment) at any point between Study Day 1 and their last parasite assessment, e) Participant was parasite-free at 6 months. The percentage of participants who were relapse-free at 6 months post dose has been presented. (NCT02802501)
Timeframe: 6 months post-dose

InterventionPercentage of participants (Number)
DHA-PQP Only12
Tafenoquine+ DHA-PQP22

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Percentage of Participants With Relapse-free Efficacy at Six Months After Administration of Primaquine With DHA-PQP and DHA-PQP Alone

A participant was considered to have demonstrated relapse-free efficacy at 6 months if: a) Participant had non-zero P. vivax asexual parasite count at Baseline (Day 1), b) Participant demonstrated initial clearance of P.vivax parasitemia, c) Participant had no positive asexual P.vivax parasite count at any assessment prior to or on study Day 180 following initial parasite clearance, d) Participants did not take a concomitant medication with anti-malarial activity (excluding study treatment) at any point between Study Day 1 and their last parasite assessment, e) Participant was parasite-free at 6 months. The percentage of participants who were relapse-free at 6 months post dose has been presented. (NCT02802501)
Timeframe: 6 months post-dose

InterventionPercentage of participants (Number)
DHA-PQP Only12
Primaquine+DHA-PQP52

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Percentage of Participants With Relapse-free Efficacy at Four Months After Administration of Tafenoquine With DHA-PQP and DHA-PQP Alone

A participant was considered to have demonstrated recurrence-free efficacy at 4 months if: a) Participant had non-zero P. vivax asexual parasite count at Baseline, b) Participant demonstrated initial clearance of P.vivax parasitemia, c) Participant had no positive asexual P.vivax parasite count at any assessment prior to or on Study Day 135 following initial parasite clearance, d) Participants did not take a concomitant medication with anti-malarial activity (excluding study treatment) at any point between Study Day 1 and their first parasite assessment after Study Day 105 (up to and including Study Day 135), e) Participant was parasite-free at 4 months. The rate of relapse-free efficacy was estimated by Kaplan-Meier methodology. The percentage of participants who were relapse-free at 4 months post dose has been presented. (NCT02802501)
Timeframe: 4 months post-dose

InterventionPercentage of participants (Number)
DHA-PQP Only16
Tafenoquine+ DHA-PQP28

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Number of Participants With Recrudescence

Recrudescence was defined as blood stage treatment failure. A participant was considered to have had a recrudescence if both of the following were true: 1) if participant had a positive P. vivax asexual parasite count at Baseline and demonstrated clearance (i.e. two negative asexual P. vivax parasite counts, with at least 6 hours between the counts, and no positive counts in the interval); 2) Participant had a positive genetically homologous asexual P. vivax parasite count on or before Study Day 14, after their zero count in days 1 to 5. (NCT02802501)
Timeframe: Up to Day 14

InterventionParticipants (Count of Participants)
DHA-PQP Only0
Tafenoquine+ DHA-PQP0
Primaquine+DHA-PQP0

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Number of Participants With Electrocardiogram (ECG) Values Outside Clinical Concern Range-QT Interval Corrected Using Fredericia's Formula (QTcF)

12-lead ECG was obtained at indicated time points using an automated ECG machine that measured QTcF. Clinical concern range included:absolute QTcF interval (upper: >480 milliseconds) and increase from Baseline in QTcF (upper: >=60 milliseconds). Data for maximum post-Baseline increase >=60 and >480 milliseconds has been presented. (NCT02802501)
Timeframe: Up to Day 28

InterventionParticipants (Count of Participants)
DHA-PQP Only2
Tafenoquine+ DHA-PQP3
Primaquine+DHA-PQP1

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Number of Participants With Chemistry Values Outside Clinical Concern Range

Blood samples were collected at indicated time points to analyze following chemistry parameters: alanine aminotransferase (ALT), Alkaline Phosphatase (ALP), Aspartate Aminotransferase (AST), Bilirubin, Creatine Kinase, Creatinine, Indirect Bilirubin and Urea. Clinical concern range for the parameters included ALT and AST (high: >3 times Upper Limit of Normal [ULN]), ALP (high: >2.5 times ULN), bilirubin and indirect bilirubin (high: >1.5 times ULN), creatine kinase (high: >5 times ULN), creatinine (high: >3 times ULN) and urea (high: >11.067 millimoles per Liter [mmol/L]. Data for any time on treatment has been presented. (NCT02802501)
Timeframe: Up to Day 120

,,
InterventionParticipants (Count of Participants)
ALT, HighALP, HighAST, HighBilirubin, HighCreatine Kinase, HighCreatinine, HighIndirect bilirubin, HighUrea, High
DHA-PQP Only11047010
Primaquine+DHA-PQP00046010
Tafenoquine+ DHA-PQP30166010

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Number of Participants With Gastrointestinal AEs

The number of participants with gastrointestinal AEs: nausea, vomiting, diarrhea, dyspepsia, abdominal distension, abdominal discomfort and constipation has been presented. (NCT02802501)
Timeframe: Up to Day 180

,,
InterventionParticipants (Count of Participants)
NauseaVomitingDiarrheaDyspepsiaAbdominal distensionAbdominal discomfortConstipation
DHA-PQP Only5652100
Primaquine+DHA-PQP3124120
Tafenoquine+ DHA-PQP4523101

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Number of Participants With Any Adverse Events (AEs) and Serious Adverse Events (SAEs) During the Double-blind Treatment Phase

An AE is any untoward medical occurrence in a participant or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. A SAE is defined as as any untoward medical occurrence that, at any dose results in death, is life-threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, is a congenital anomaly/birth defect, is associated with liver injury and impaired liver function, other important medical events that may jeopardize the participant or may require medical or surgical intervention to prevent one of the other outcomes listed before. (NCT02802501)
Timeframe: Up to Day 180

,,
InterventionParticipants (Count of Participants)
Any AEsAny SAEs
DHA-PQP Only411
Primaquine+DHA-PQP342
Tafenoquine+ DHA-PQP412

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Number of Participants With Hematology Values Outside Clinical Concern Range

Blood samples were collected to analyze the following hematology parameters: Hemoglobin, lymphocytes and Platelet count. The clinical concern ranges for the parameters included: hemoglobin (low: <7 grams per deciliter), lymphocytes: (low: <0.5x10^9 cells per liter and high: >4x10^9 cells per liter),and platelets (low: <50x10^9 cells per liter). Data for any time on treatment has been presented. (NCT02802501)
Timeframe: Up to Day 120

,,
InterventionParticipants (Count of Participants)
Hemoglobin, LowLymphocytes, HighLymphocytes, LowPlatelets, Low
DHA-PQP Only0300
Primaquine+DHA-PQP0210
Tafenoquine+ DHA-PQP0401

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Number of Participants With Protocol-defined SAE (Hemoglobin Drop)

Blood samples were collected at indicated time points to analyze the hemoglobin level. Hemoglobin drop is defined as any one of the following occurring in the first 15 days of the study: a relative hemoglobin decrease of >=30% from Baseline, or an absolute hemoglobin decrease of >3 grams per liter from Baseline, or a drop in absolute hemoglobin to <7.0 grams per decilter (g/dL). Number of participants with a protocol-defined hemoglobin SAEs has been presented. (NCT02802501)
Timeframe: Days 3, 5, 7, and 14

,,
InterventionParticipants (Count of Participants)
Day 3Day 5Day 7Day 14
DHA-PQP Only0000
Primaquine+DHA-PQP0000
Tafenoquine+ DHA-PQP0000

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Number of Participants With Worst Case Body Temperature Results Relative to Normal Range Post-Baseline Relative to Baseline

"Body temperature was measured with participants in semi-supine position after 5 minutes of rest. Data was categorized as: body temperature 'low: <36.5 degrees celsius', 'high: >37.3 degrees celsius' and 'To Normal or No change'. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose vital sign value category was unchanged (e.g.,High to High), or whose value became normal, are recorded in the To Normal or No Change category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. Day 1 was considered as Baseline." (NCT02802501)
Timeframe: Baseline (Day 1) and up to Day 180

,,
InterventionParticipants (Count of Participants)
To LowTo Normal or No changeTo High
DHA-PQP Only42310
Primaquine+DHA-PQP4256
Tafenoquine+ DHA-PQP38714

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Number of Participants With Worst Case Pulse Rate Results Relative to Normal Range Post-Baseline Relative to Baseline

"Pulse rate was measured with participants in semi-supine position after 5 minutes of rest. Data was categorized as: pulse rate low: <60 beats per minute [bpm], high: >100 bpm and 'To normal or No change'. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose vital sign value category was unchanged (e.g.,High to High), or whose value became normal, are recorded in the To Normal or No Change category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. Day 1 was considered as Baseline." (NCT02802501)
Timeframe: Baseline (Day 1) and up to Day 180

,,
InterventionParticipants (Count of Participants)
To LowTo Normal or No changeTo High
DHA-PQP Only19257
Primaquine+DHA-PQP23263
Tafenoquine+ DHA-PQP26236

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Number of Participants With Worst Case Respiratory Rate Results Relative to Normal Range Post-Baseline Relative to Baseline

"Respiratory rate was measured with participants in semi-supine position after 5 minutes of rest. Data was categorized as: respiratory rate low: <12 breaths per minute', high: >18 breaths per minute and 'To normal or No change'. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose vital sign value category was unchanged (e.g.,High to High), or whose value became normal, are recorded in the To Normal or No Change category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%.Day 1 was considered as Baseline. Day 1 was considered as Baseline." (NCT02802501)
Timeframe: Baseline (Day 1) and up to Day 180

,,
InterventionParticipants (Count of Participants)
To LowTo Normal or No changeTo High
DHA-PQP Only0419
Primaquine+DHA-PQP04010
Tafenoquine+ DHA-PQP0419

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Number of Participants With Worst Case Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) Results Relative to Normal Range Post-Baseline Relative to Baseline

"SBP and DBP were measured with participants in semi-supine position after 5 minutes of rest. Data was categorized as: systolic blood pressure (SBP) (low: <90 and high: >120 millimeters of mercury [mmHg]); diastolic blood pressure (DBP) (low: <60 and high: >80 mmHg); and 'To Normal or No change'. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose vital sign value category was unchanged (e.g.,High to High), or whose value became normal, are recorded in the To Normal or No Change category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. Day 1 was considered as Baseline." (NCT02802501)
Timeframe: Baseline (Day 1) and up to Day 180

,,
InterventionParticipants (Count of Participants)
SBP, To LowSBP, To Normal or No changeSBP, To HighDBP, To LowDBP, To Normal or No changeDBP, To High
DHA-PQP Only01931111628
Primaquine+DHA-PQP02525151628
Tafenoquine+ DHA-PQP1212992025

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Change From Baseline in QT Interval Corrected by Fridericia's Formula (QTcF)

12-lead ECG was obtained at indicated time points using an automated ECG machine that measured QTcF interval. Change from Baseline is calculated as Post-Dose Visit Value minus Baseline value. Day 1 was considered as Baseline. (NCT02802501)
Timeframe: Baseline (Day 1), Day 3: 4 hours post DHA-PQP dose, Days 7 and 28

,,
InterventionMilliseconds (Mean)
Day 3: 4 hours post DHA-PQP doseDay 7Day 28
DHA-PQP Only35.311.52.4
Primaquine+DHA-PQP40.816.510.2
Tafenoquine+ DHA-PQP44.512.27.5

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