Page last updated: 2024-10-30

mefloquine hydrochloride and Infections, Plasmodium

mefloquine hydrochloride has been researched along with Infections, Plasmodium in 27 studies

[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol : An organofluorine compound that consists of quinoline bearing trifluoromethyl substituents at positions 2 and 8 as well as a (2-piperidinyl)hydroxymethyl substituent at position 4.

Research Excerpts

ExcerptRelevanceReference
"This study represents the first phase III trial of the safety, tolerability, and effectiveness of tafenoquine for malaria prophylaxis."9.14Randomized, double-blind study of the safety, tolerability, and efficacy of tafenoquine versus mefloquine for malaria prophylaxis in nonimmune subjects. ( Brennan, L; Edstein, MD; Harris, IE; Kerr, C; Kitchener, SJ; Leggat, PA; Nasveld, PE; Ohrt, C; Pickford, P; Prescott, W; Reid, M, 2010)
"Sixteen new artemisinin-derived 2-carbon-linked trioxane dimers were prepared to study chemical structure/antimalarial activity relationships (SAR)."7.80The survival times of malaria-infected mice are prolonged more by several new two-carbon-linked artemisinin-derived dimer carbamates than by the trioxane antimalarial drug artemether. ( Conyers, RC; Mazzone, JR; Mott, BT; Posner, GH; Siegler, MA; Sullivan, DJ; Tripathi, AK, 2014)
"Reports of potential drug-resistant strains of Plasmodium malariae in western Indonesia raise concerns that chloroquine resistance may be emerging in P."7.77In vivo and in vitro efficacy of chloroquine against Plasmodium malariae and P. ovale in Papua, Indonesia. ( Anstey, NM; Chalfein, F; Ebsworth, EP; Kenangalem, E; Marfurt, J; Piera, KA; Prasetyorini, B; Price, RN; Ratcliff, A; Russell, B; Siswantoro, H; Tjitra, E; Wuwung, M, 2011)
"In an attempt to augment the efficacy of 7-chloro 4-aminoquinoline analogs and also to overcome resistance to antimalarial agents, we synthesized three cyclen (1,4,7,10-tetraazacyclododecane) analogs of chloroquine [a bisquinoline derivative, 7-chloro-4-(1,4,7,10-tetraaza-cyclododec-1-yl)-quinoline HBr, and a 7-chloro-4-(1,4,7,10-tetraaza-cyclododec-1-yl)-quinoline-Zn(2+) complex]."7.75Synthesis and antimalarial activities of cyclen 4-aminoquinoline analogs. ( Borne, RF; Khan, MO; Khan, SI; Kimura, E; Levi, MS; Tekwani, BL, 2009)
"The synthesis of deoxycholic acid (DCA)- and cholic acid (CA)-derived mixed tetraoxanes revealed that N-(2-dimethylamino)ethyl derivatives are potent antimalarials in vitro and in vivo."7.74Deoxycholic acid-derived tetraoxane antimalarials and antiproliferatives(1). ( Milhous, WK; Milić, D; Opsenica, D; Smith, KS; Solaja, BA; Terzić, N; Tinant, B, 2007)
"Using easily accessible keto-trioxanes 7a-g as the starting materials, a series of new variously functionalized 1,2,4-trioxanes 10-36 have been prepared and evaluated for antimalarial activity against multi-drug-resistant Plasmodium yoelii nigeriensis in mice in the dose range of 24 mg/kg x 4 days to 96 mg/kg x 4 days by oral route."7.73Orally active 1,2,4-trioxanes: synthesis and antimalarial assessment of a new series of 9-functionalized 3-(1-arylvinyl)-1,2,5-trioxaspiro[5.5]undecanes against multi-drug-resistant plasmodium yoelii nigeriensis in mice. ( Malik, H; Puri, SK; Singh, C, 2006)
"Febrifugine is an alkaloid isolated from Dichroa febrifuga Lour as the active component against Plasmodium falciparum, but exhibits toxic side effects."5.38Febrifugine analogue compounds: synthesis and antimalarial evaluation. ( Chandrashekar, G; Chatterji, D; Meng, L; Robinson, K; Zhu, S, 2012)
"This study represents the first phase III trial of the safety, tolerability, and effectiveness of tafenoquine for malaria prophylaxis."5.14Randomized, double-blind study of the safety, tolerability, and efficacy of tafenoquine versus mefloquine for malaria prophylaxis in nonimmune subjects. ( Brennan, L; Edstein, MD; Harris, IE; Kerr, C; Kitchener, SJ; Leggat, PA; Nasveld, PE; Ohrt, C; Pickford, P; Prescott, W; Reid, M, 2010)
"Chloroquine (CQ) has been used as first line malaria therapeutic drug for decades."3.81Antimalarial activity of 4-amidinoquinoline and 10-amidinobenzonaphthyridine derivatives. ( Caridha, D; Gerena, L; Korotchenko, V; Kreishman-Deitrick, M; Li, Q; Lin, AJ; Sathunuru, R; Smith, PL, 2015)
"Sixteen new artemisinin-derived 2-carbon-linked trioxane dimers were prepared to study chemical structure/antimalarial activity relationships (SAR)."3.80The survival times of malaria-infected mice are prolonged more by several new two-carbon-linked artemisinin-derived dimer carbamates than by the trioxane antimalarial drug artemether. ( Conyers, RC; Mazzone, JR; Mott, BT; Posner, GH; Siegler, MA; Sullivan, DJ; Tripathi, AK, 2014)
"Reports of potential drug-resistant strains of Plasmodium malariae in western Indonesia raise concerns that chloroquine resistance may be emerging in P."3.77In vivo and in vitro efficacy of chloroquine against Plasmodium malariae and P. ovale in Papua, Indonesia. ( Anstey, NM; Chalfein, F; Ebsworth, EP; Kenangalem, E; Marfurt, J; Piera, KA; Prasetyorini, B; Price, RN; Ratcliff, A; Russell, B; Siswantoro, H; Tjitra, E; Wuwung, M, 2011)
"Drug resistance against dihydrofolate reductase (DHFR) inhibitors-such as pyrimethamine (PM)-has now spread to almost all regions where malaria is endemic, rendering antifolate-based malaria treatments highly ineffective."3.76Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate. ( Brun, R; Chitnumsub, P; Dartois, V; Diagana, TT; Goh, A; Kamchonwongpaisan, S; Keller, TH; Kiara, SM; Lakshminarayana, SB; Ma, NL; Maneeruttanarungroj, C; Nzila, A; Rottmann, M; Taweechai, S; Weaver, M; Wittlin, S; Wong, J; Yeung, BK; Yuthavong, Y; Zou, B, 2010)
"In an attempt to augment the efficacy of 7-chloro 4-aminoquinoline analogs and also to overcome resistance to antimalarial agents, we synthesized three cyclen (1,4,7,10-tetraazacyclododecane) analogs of chloroquine [a bisquinoline derivative, 7-chloro-4-(1,4,7,10-tetraaza-cyclododec-1-yl)-quinoline HBr, and a 7-chloro-4-(1,4,7,10-tetraaza-cyclododec-1-yl)-quinoline-Zn(2+) complex]."3.75Synthesis and antimalarial activities of cyclen 4-aminoquinoline analogs. ( Borne, RF; Khan, MO; Khan, SI; Kimura, E; Levi, MS; Tekwani, BL, 2009)
"The synthesis of deoxycholic acid (DCA)- and cholic acid (CA)-derived mixed tetraoxanes revealed that N-(2-dimethylamino)ethyl derivatives are potent antimalarials in vitro and in vivo."3.74Deoxycholic acid-derived tetraoxane antimalarials and antiproliferatives(1). ( Milhous, WK; Milić, D; Opsenica, D; Smith, KS; Solaja, BA; Terzić, N; Tinant, B, 2007)
" Their antimalarial effects have been characterized in parasite assays using chloroquine-sensitive and -resistant strains of Plasmodium, alone or in drug combination, and in the Plasmodium berghei rodent model."3.74Antimalarial dual drugs based on potent inhibitors of glutathione reductase from Plasmodium falciparum. ( Becker, K; Davioud-Charvet, E; Friebolin, W; Furrer, J; Jannack, B; Lanzer, M; Oeser, T; Sanchez, CP; Wenzel, N; Yardley, V, 2008)
"Using easily accessible keto-trioxanes 7a-g as the starting materials, a series of new variously functionalized 1,2,4-trioxanes 10-36 have been prepared and evaluated for antimalarial activity against multi-drug-resistant Plasmodium yoelii nigeriensis in mice in the dose range of 24 mg/kg x 4 days to 96 mg/kg x 4 days by oral route."3.73Orally active 1,2,4-trioxanes: synthesis and antimalarial assessment of a new series of 9-functionalized 3-(1-arylvinyl)-1,2,5-trioxaspiro[5.5]undecanes against multi-drug-resistant plasmodium yoelii nigeriensis in mice. ( Malik, H; Puri, SK; Singh, C, 2006)
"Febrifugine is an alkaloid isolated from Dichroa febrifuga Lour as the active component against Plasmodium falciparum, but exhibits toxic side effects."1.38Febrifugine analogue compounds: synthesis and antimalarial evaluation. ( Chandrashekar, G; Chatterji, D; Meng, L; Robinson, K; Zhu, S, 2012)
"Malaria is one of the leading causes of severe infectious disease worldwide; yet, our ability to maintain effective therapy to combat the illness is continually challenged by the emergence of drug resistance."1.37Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice. ( Bathurst, I; Buckner, FS; Burrows, J; Charman, SA; Charman, WN; Creason, S; Deng, X; El Mazouni, F; Floyd, DM; Gujjar, R; Matthews, D; Phillips, MA; Rathod, PK; Shackleford, DM; White, J; White, KL, 2011)
" The orally bioavailable lead imidazolopiperazine confers complete causal prophylactic protection (15 milligrams/kilogram) in rodent models of malaria and shows potent in vivo blood-stage therapeutic activity."1.37Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery. ( Barnes, SW; Bonamy, GM; Bopp, SE; Borboa, R; Bright, AT; Chatterjee, A; Che, J; Cohen, S; Dharia, NV; Diagana, TT; Fidock, DA; Froissard, P; Gagaring, K; Gettayacamin, M; Glynne, RJ; Gordon, P; Groessl, T; Kato, N; Kuhen, KL; Lee, MC; Mazier, D; McNamara, CW; Meister, S; Nagle, A; Nam, TG; Plouffe, DM; Richmond, W; Roland, J; Rottmann, M; Sattabongkot, J; Schultz, PG; Tuntland, T; Walker, JR; Winzeler, EA; Wu, T; Zhou, B; Zhou, Y, 2011)
" The optimized spiroindolone NITD609 shows pharmacokinetic properties compatible with once-daily oral dosing and has single-dose efficacy in a rodent malaria model."1.36Spiroindolones, a potent compound class for the treatment of malaria. ( Beck, HP; Brun, R; Cohen, SB; Dartois, V; Dharia, NV; Diagana, TT; Fidock, DA; Goh, A; González-Páez, GE; Jegla, T; Keller, TH; Lakshminarayana, SB; Lee, MC; McNamara, C; Nosten, F; Plouffe, DM; Renia, L; Rottmann, M; Russell, B; Schmitt, EK; Seitz, P; Spencer, KR; Suwanarusk, R; Tan, J; Winzeler, EA; Yeung, BK; Zou, B, 2010)

Research

Studies (27)

TimeframeStudies, this research(%)All Research%
pre-19901 (3.70)18.7374
1990's0 (0.00)18.2507
2000's12 (44.44)29.6817
2010's14 (51.85)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
Brossi, A1
Venugopalan, B1
Dominguez Gerpe, L1
Yeh, HJ1
Flippen-Anderson, JL1
Buchs, P1
Luo, XD1
Milhous, W2
Peters, W2
Avery, MA1
Alvim-Gaston, M1
Vroman, JA1
Wu, B1
Ager, A2
Robinson, BL1
Charman, W1
Nallan, L1
Bauer, KD1
Bendale, P1
Rivas, K1
Yokoyama, K1
Hornéy, CP1
Pendyala, PR1
Floyd, D1
Lombardo, LJ1
Williams, DK1
Hamilton, A1
Sebti, S1
Windsor, WT1
Weber, PC1
Buckner, FS2
Chakrabarti, D1
Gelb, MH1
Van Voorhis, WC1
Zhang, Q1
Guan, J1
Sacci, J1
Ellis, W1
Kyle, D1
Lin, AJ2
Singh, C1
Malik, H1
Puri, SK1
Terzić, N1
Opsenica, D3
Milić, D1
Tinant, B1
Smith, KS2
Milhous, WK2
Solaja, BA3
Friebolin, W1
Jannack, B1
Wenzel, N1
Furrer, J1
Oeser, T1
Sanchez, CP1
Lanzer, M1
Yardley, V1
Becker, K1
Davioud-Charvet, E1
Plouffe, D2
Brinker, A1
McNamara, C2
Henson, K1
Kato, N2
Kuhen, K2
Nagle, A3
Adrián, F1
Matzen, JT1
Anderson, P1
Nam, TG2
Gray, NS1
Chatterjee, A2
Janes, J1
Yan, SF1
Trager, R1
Caldwell, JS1
Schultz, PG2
Zhou, Y2
Winzeler, EA3
Dow, GS1
Chen, Y1
Andrews, KT1
Caridha, D3
Gerena, L3
Gettayacamin, M4
Johnson, J2
Li, Q3
Melendez, V2
Obaldia, N1
Tran, TN1
Kozikowski, AP1
Opsenica, I2
Lanteri, CA2
Anova, L1
Khan, MO1
Levi, MS1
Tekwani, BL1
Khan, SI1
Kimura, E1
Borne, RF1
O'Neill, PM2
Park, BK2
Shone, AE2
Maggs, JL2
Roberts, P2
Stocks, PA2
Biagini, GA1
Bray, PG2
Gibbons, P1
Berry, N2
Winstanley, PA2
Mukhtar, A1
Bonar-Law, R1
Hindley, S2
Bambal, RB2
Davis, CB2
Bates, M2
Hart, TK1
Gresham, SL2
Lawrence, RM1
Brigandi, RA2
Gomez-delas-Heras, FM1
Gargallo, DV2
Ward, SA2
Stanford, D1
Nixon, G1
Asadollahy, E1
Biagini, G1
Davies, J1
Hall, C1
Rimmer, K1
Gomez-de-Las-Heras, FM1
Parapini, S1
Vivas, L1
Lander, H1
Taramelli, D2
Nasveld, PE1
Edstein, MD1
Reid, M1
Brennan, L1
Harris, IE1
Kitchener, SJ1
Leggat, PA1
Pickford, P1
Kerr, C1
Ohrt, C1
Prescott, W1
Nzila, A1
Rottmann, M4
Chitnumsub, P1
Kiara, SM1
Kamchonwongpaisan, S1
Maneeruttanarungroj, C1
Taweechai, S1
Yeung, BK2
Goh, A3
Lakshminarayana, SB3
Zou, B2
Wong, J1
Ma, NL1
Weaver, M1
Keller, TH2
Dartois, V3
Wittlin, S1
Brun, R3
Yuthavong, Y1
Diagana, TT3
Lee, MC2
Russell, B2
Seitz, P1
Plouffe, DM2
Dharia, NV2
Tan, J1
Cohen, SB1
Spencer, KR1
González-Páez, GE1
Suwanarusk, R1
Jegla, T1
Schmitt, EK1
Beck, HP1
Nosten, F1
Renia, L1
Fidock, DA2
Siswantoro, H1
Ratcliff, A1
Prasetyorini, B1
Chalfein, F1
Marfurt, J1
Kenangalem, E1
Wuwung, M1
Piera, KA1
Ebsworth, EP1
Anstey, NM1
Tjitra, E1
Price, RN1
Burnett, JC1
Gussio, R1
Todorović, N1
Sciotti, RJ1
Basilico, N1
Nuss, JE1
Wanner, L1
Panchal, RG1
Bavari, S1
Gujjar, R1
El Mazouni, F1
White, KL2
White, J1
Creason, S1
Shackleford, DM2
Deng, X1
Charman, WN1
Bathurst, I2
Burrows, J1
Floyd, DM1
Matthews, D1
Charman, SA2
Phillips, MA1
Rathod, PK1
Ndakala, AJ1
Gessner, RK1
Gitari, PW1
October, N1
Hudson, A1
Fakorede, F1
Kaiser, M1
Yeates, C1
Chibale, K1
Wu, T2
Gagaring, K2
Borboa, R2
Francek, C1
Chen, Z1
Wu, J1
Ang, HQ1
Zeng, P1
Kang, ML1
Tan, W1
Tan, M1
Ye, N1
Lin, X1
Caldwell, C1
Ek, J1
Skolnik, S1
Liu, F1
Wang, J1
Chang, J1
Li, C1
Hollenbeck, T1
Tuntland, T2
Isbell, J1
Fischli, C1
Keller, T1
Diagana, T1
Winzeler, E1
Glynne, R1
Tully, DC1
Chatterjee, AK1
Milner, E1
Gardner, S1
Moon, J1
Grauer, K1
Auschwitz, J1
Kozar, M1
Lee, P1
Leed, S1
McCalmont, W1
Roncal, N1
Sciotti, R1
Smith, B1
Sousa, J1
Tungtaeng, A1
Wipf, P1
Dow, G1
Sá, MS1
de Menezes, MN1
Krettli, AU1
Ribeiro, IM1
Tomassini, TC1
Ribeiro dos Santos, R1
de Azevedo, WF1
Soares, MB1
Meister, S1
Kuhen, KL1
Bonamy, GM1
Barnes, SW1
Bopp, SE1
Bright, AT1
Che, J1
Cohen, S1
Gordon, P1
Groessl, T1
McNamara, CW1
Richmond, W1
Roland, J1
Zhou, B1
Froissard, P1
Glynne, RJ1
Mazier, D1
Sattabongkot, J1
Walker, JR1
Zhu, S1
Chandrashekar, G1
Meng, L1
Robinson, K1
Chatterji, D1
Conyers, RC1
Mazzone, JR1
Siegler, MA1
Tripathi, AK1
Sullivan, DJ1
Mott, BT1
Posner, GH1
Korotchenko, V1
Sathunuru, R1
Kreishman-Deitrick, M1
Smith, PL1

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Safety, Tolerability and Pharmacokinetics of Tafenoquine After Weekly and Escalating Monthly Doses of Tafenoquine in Healthy Vietnamese Volunteers[NCT05203744]Phase 4200 participants (Anticipated)Interventional2022-05-10Not yet recruiting
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
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trials

1 trial available for mefloquine hydrochloride and Infections, Plasmodium

ArticleYear
Randomized, double-blind study of the safety, tolerability, and efficacy of tafenoquine versus mefloquine for malaria prophylaxis in nonimmune subjects.
    Antimicrobial agents and chemotherapy, 2010, Volume: 54, Issue:2

    Topics: Adult; Aminoquinolines; Antimalarials; Australia; Double-Blind Method; Female; Humans; Malaria; Male

2010
Randomized, double-blind study of the safety, tolerability, and efficacy of tafenoquine versus mefloquine for malaria prophylaxis in nonimmune subjects.
    Antimicrobial agents and chemotherapy, 2010, Volume: 54, Issue:2

    Topics: Adult; Aminoquinolines; Antimalarials; Australia; Double-Blind Method; Female; Humans; Malaria; Male

2010
Randomized, double-blind study of the safety, tolerability, and efficacy of tafenoquine versus mefloquine for malaria prophylaxis in nonimmune subjects.
    Antimicrobial agents and chemotherapy, 2010, Volume: 54, Issue:2

    Topics: Adult; Aminoquinolines; Antimalarials; Australia; Double-Blind Method; Female; Humans; Malaria; Male

2010
Randomized, double-blind study of the safety, tolerability, and efficacy of tafenoquine versus mefloquine for malaria prophylaxis in nonimmune subjects.
    Antimicrobial agents and chemotherapy, 2010, Volume: 54, Issue:2

    Topics: Adult; Aminoquinolines; Antimalarials; Australia; Double-Blind Method; Female; Humans; Malaria; Male

2010

Other Studies

26 other studies available for mefloquine hydrochloride and Infections, Plasmodium

ArticleYear
Arteether, a new antimalarial drug: synthesis and antimalarial properties.
    Journal of medicinal chemistry, 1988, Volume: 31, Issue:3

    Topics: Animals; Antimalarials; Artemisinins; Magnetic Resonance Spectroscopy; Malaria; Mice; Models, Molecu

1988
Structure-activity relationships of the antimalarial agent artemisinin. 7. Direct modification of (+)-artemisinin and in vivo antimalarial screening of new, potential preclinical antimalarial candidates.
    Journal of medicinal chemistry, 2002, Sep-12, Volume: 45, Issue:19

    Topics: Administration, Oral; Animals; Antimalarials; Artemisinins; Drug Evaluation, Preclinical; Drug Resis

2002
Protein farnesyltransferase inhibitors exhibit potent antimalarial activity.
    Journal of medicinal chemistry, 2005, Jun-02, Volume: 48, Issue:11

    Topics: Alkyl and Aryl Transferases; Animals; Antimalarials; Cells, Cultured; Electrophoresis, Polyacrylamid

2005
Unambiguous synthesis and prophylactic antimalarial activities of imidazolidinedione derivatives.
    Journal of medicinal chemistry, 2005, Oct-06, Volume: 48, Issue:20

    Topics: Administration, Oral; Animals; Antimalarials; Carbamates; Guanidines; Imidazoles; Imidazolidines; Ma

2005
Orally active 1,2,4-trioxanes: synthesis and antimalarial assessment of a new series of 9-functionalized 3-(1-arylvinyl)-1,2,5-trioxaspiro[5.5]undecanes against multi-drug-resistant plasmodium yoelii nigeriensis in mice.
    Journal of medicinal chemistry, 2006, May-04, Volume: 49, Issue:9

    Topics: Administration, Oral; Amination; Animals; Antimalarials; Artemisinins; Drug Resistance, Multiple; He

2006
Deoxycholic acid-derived tetraoxane antimalarials and antiproliferatives(1).
    Journal of medicinal chemistry, 2007, Oct-18, Volume: 50, Issue:21

    Topics: Animals; Antimalarials; Antineoplastic Agents; Cell Line, Tumor; Crystallography, X-Ray; Cyclohexane

2007
Antimalarial dual drugs based on potent inhibitors of glutathione reductase from Plasmodium falciparum.
    Journal of medicinal chemistry, 2008, Mar-13, Volume: 51, Issue:5

    Topics: Animals; Antimalarials; Biological Transport; Cell Line, Tumor; Chloroquine; Drug Resistance; Drug T

2008
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
    Proceedings of the National Academy of Sciences of the United States of America, 2008, Jul-01, Volume: 105, Issue:26

    Topics: Animals; Antimalarials; Cluster Analysis; Computational Biology; Drug Evaluation, Preclinical; Drug

2008
Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors.
    Antimicrobial agents and chemotherapy, 2008, Volume: 52, Issue:10

    Topics: Animals; Antimalarials; Aotidae; Drug Resistance; Enzyme Inhibitors; Histone Deacetylase Inhibitors;

2008
New chimeric antimalarials with 4-aminoquinoline moiety linked to a tetraoxane skeleton.
    Journal of medicinal chemistry, 2008, Oct-09, Volume: 51, Issue:19

    Topics: Aminoquinolines; Animals; Antimalarials; Binding Sites; Disease Models, Animal; Dose-Response Relati

2008
Synthesis and antimalarial activities of cyclen 4-aminoquinoline analogs.
    Antimicrobial agents and chemotherapy, 2009, Volume: 53, Issue:4

    Topics: Aminoquinolines; Animals; Antimalarials; Chloroquine; Cyclams; Hemeproteins; Heterocyclic Compounds;

2009
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
    Journal of medicinal chemistry, 2009, Mar-12, Volume: 52, Issue:5

    Topics: Aminoquinolines; Amodiaquine; Animals; Antimalarials; Benzylamines; Cytochrome P-450 Enzyme Inhibito

2009
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
    Journal of medicinal chemistry, 2009, Apr-09, Volume: 52, Issue:7

    Topics: Aminoquinolines; Amodiaquine; Animals; Antimalarials; Cell Survival; Chloroquine; Dogs; Drug Resista

2009
Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate.
    Antimicrobial agents and chemotherapy, 2010, Volume: 54, Issue:6

    Topics: Administration, Oral; Animals; Antimalarials; Biological Availability; Drug Resistance; Female; Foli

2010
Spiroindolones, a potent compound class for the treatment of malaria.
    Science (New York, N.Y.), 2010, Sep-03, Volume: 329, Issue:5996

    Topics: Adenosine Triphosphatases; Animals; Antimalarials; Cell Line; Drug Discovery; Drug Resistance; Eryth

2010
In vivo and in vitro efficacy of chloroquine against Plasmodium malariae and P. ovale in Papua, Indonesia.
    Antimicrobial agents and chemotherapy, 2011, Volume: 55, Issue:1

    Topics: Adolescent; Adult; Antimalarials; Child; Child, Preschool; Chloroquine; Female; Humans; Indonesia; M

2011
A chemotype that inhibits three unrelated pathogenic targets: the botulinum neurotoxin serotype A light chain, P. falciparum malaria, and the Ebola filovirus.
    Journal of medicinal chemistry, 2011, Mar-10, Volume: 54, Issue:5

    Topics: Animals; Anopheles; Anti-Bacterial Agents; Antimalarials; Antiviral Agents; Botulinum Toxins, Type A

2011
Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice.
    Journal of medicinal chemistry, 2011, Jun-09, Volume: 54, Issue:11

    Topics: Animals; Antimalarials; Dihydroorotate Dehydrogenase; Disease Models, Animal; Drug Design; Drug Disc

2011
Antimalarial pyrido[1,2-a]benzimidazoles.
    Journal of medicinal chemistry, 2011, Jul-14, Volume: 54, Issue:13

    Topics: Administration, Oral; Animals; Antimalarials; Benzimidazoles; Drug Resistance, Multiple; Humans; In

2011
Imidazolopiperazines: hit to lead optimization of new antimalarial agents.
    Journal of medicinal chemistry, 2011, Jul-28, Volume: 54, Issue:14

    Topics: Amino Acids; Aniline Compounds; Animals; Antimalarials; Benzene Derivatives; Cell Line; Drug Resista

2011
Structure-activity relationships of 4-position diamine quinoline methanols as intermittent preventative treatment (IPT) against Plasmodium falciparum.
    Journal of medicinal chemistry, 2011, Sep-22, Volume: 54, Issue:18

    Topics: Animals; Antimalarials; Cell Line; Cell Membrane Permeability; Dimerization; Dogs; Drug Resistance;

2011
Antimalarial activity of physalins B, D, F, and G.
    Journal of natural products, 2011, Oct-28, Volume: 74, Issue:10

    Topics: Animals; Antimalarials; Immunosuppressive Agents; Malaria; Mice; Mice, Inbred BALB C; Parasitemia; P

2011
Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
    Science (New York, N.Y.), 2011, Dec-09, Volume: 334, Issue:6061

    Topics: Animals; Antimalarials; Cell Line, Tumor; Drug Discovery; Drug Evaluation, Preclinical; Drug Resista

2011
Febrifugine analogue compounds: synthesis and antimalarial evaluation.
    Bioorganic & medicinal chemistry, 2012, Jan-15, Volume: 20, Issue:2

    Topics: Animals; Antimalarials; Aotus trivirgatus; Drug Evaluation, Preclinical; Malaria; Piperidines; Plasm

2012
The survival times of malaria-infected mice are prolonged more by several new two-carbon-linked artemisinin-derived dimer carbamates than by the trioxane antimalarial drug artemether.
    Bioorganic & medicinal chemistry letters, 2014, Mar-01, Volume: 24, Issue:5

    Topics: Animals; Antimalarials; Artemether; Artemisinins; Carbamates; Carbon; Crystallography, X-Ray; Dimeri

2014
Antimalarial activity of 4-amidinoquinoline and 10-amidinobenzonaphthyridine derivatives.
    Journal of medicinal chemistry, 2015, Apr-23, Volume: 58, Issue:8

    Topics: Animals; Antimalarials; Hep G2 Cells; Humans; Malaria; Malaria, Falciparum; Male; Mice; Naphthyridin

2015