Page last updated: 2024-11-11

pafuramidine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

pafuramidine: a prodrug of furamidine [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5480200
CHEMBL ID319669
SCHEMBL ID12348156
MeSH IDM0504256

Synonyms (20)

Synonym
186953-56-0
CHEMBL319669
pafuramidine
n'-methoxy-4-[5-[4-[(z)-n'-methoxycarbamimidoyl]phenyl]furan-2-yl]benzenecarboximidamide
unii-h1vg379j2x
db289 cpd
h1vg379j2x ,
pafuramidine [inn]
benzenecarboximidamide, 4,4'-(2,5-furandiyl)bis(n-methoxy-
4,4'-(furan-2,5-diyl)bis(n-methoxybenzenecarboximidamide)
HY-14932
CS-1470
SCHEMBL12348156
AKOS030526680
n'-methoxy-4-[5-[4-(n'-methoxycarbamimidoyl)phenyl]furan-2-yl]benzenecarboximidamide
DB06532
4,4'-(furan-2,5-diyl)bis(n-methoxybenzimidamide)
A926868
F84953
MS-25808

Research Excerpts

Overview

Pafuramidine is an orally bioavailable prodrug of furamidine (DB75) It is less toxic than previous diamidines such as pentamidine.

ExcerptReferenceRelevance
"Pafuramidine (DB289) is an orally bioavailable prodrug of furamidine (DB75), an investigational diamidine that is less toxic than previous diamidines such as pentamidine."( Pafuramidine for Pneumocystis jiroveci pneumonia in HIV-infected individuals.
Aberg, JA; Chen, D; Marsh, R, 2007
)
2.5
"Pafuramidine is a novel orally active antimalarial. "( Interactions of DB75, a novel antimalarial agent, with other antimalarial drugs in vitro.
Meshnick, SR; Purfield, AE; Tidwell, RR, 2008
)
1.79

Treatment

ExcerptReferenceRelevance
"Pafuramidine for the treatment of first stage HAT was comparable in efficacy to pentamidine after 10 days of dosing. "( Efficacy, Safety, and Dose of Pafuramidine, a New Oral Drug for Treatment of First Stage Sleeping Sickness, in a Phase 2a Clinical Study and Phase 2b Randomized Clinical Studies.
Allen, JL; Bernhard, SC; Bilenge, CM; Blum, J; Burri, C; Josenando, T; Lubaki, JP; Lutumba, P; Manuel, F; Merolle, A; Mesu, VK; Mpanya, A; Mpoto, AM; Munungu, BF; Olson, CA; Pohlig, G; Serge, KK; Thompson, M; Tidwell, RR; Yeramian, PD, 2016
)
2.17

Toxicity

ExcerptReferenceRelevance
" The primary safety outcome was the rate of occurrence of World Health Organization Toxicity Scale Grade 3 or higher adverse events."( Efficacy, Safety, and Dose of Pafuramidine, a New Oral Drug for Treatment of First Stage Sleeping Sickness, in a Phase 2a Clinical Study and Phase 2b Randomized Clinical Studies.
Allen, JL; Bernhard, SC; Bilenge, CM; Blum, J; Burri, C; Josenando, T; Lubaki, JP; Lutumba, P; Manuel, F; Merolle, A; Mesu, VK; Mpanya, A; Mpoto, AM; Munungu, BF; Olson, CA; Pohlig, G; Serge, KK; Thompson, M; Tidwell, RR; Yeramian, PD, 2016
)
0.72
" In Phase 2b, the percentage of patients with at least 1 treatment-emergent adverse event was notably higher after pentamidine treatment (93%) than pafuramidine treatment for 5 days (25%) and 10 days (57%)."( Efficacy, Safety, and Dose of Pafuramidine, a New Oral Drug for Treatment of First Stage Sleeping Sickness, in a Phase 2a Clinical Study and Phase 2b Randomized Clinical Studies.
Allen, JL; Bernhard, SC; Bilenge, CM; Blum, J; Burri, C; Josenando, T; Lubaki, JP; Lutumba, P; Manuel, F; Merolle, A; Mesu, VK; Mpanya, A; Mpoto, AM; Munungu, BF; Olson, CA; Pohlig, G; Serge, KK; Thompson, M; Tidwell, RR; Yeramian, PD, 2016
)
0.92
" The primary safety outcome was the frequency and severity of adverse events."( Efficacy and Safety of Pafuramidine versus Pentamidine Maleate for Treatment of First Stage Sleeping Sickness in a Randomized, Comparator-Controlled, International Phase 3 Clinical Trial.
Bernhard, SC; Bilenge, CM; Blum, J; Burri, C; Dala, A; Deo, GK; Dituvanga, ND; Franco, JR; Kuikumbi, FM; Lubaki, JP; Macharia, S; Mesu, VK; Mintwo, AF; Mpanya, A; Mpoto, AM; Munungi, AK; Munungu, BF; Mutantu, PN; N'tombe, PM; Olson, CA; Pohlig, G; Tidwell, RR, 2016
)
0.74

Bioavailability

ExcerptReferenceRelevance
" However, DB75 does not exhibit significant oral bioavailability and has proved to be ineffective against mouse models of late-stage sleeping sickness regardless of administration route."( Distribution and quantitation of the anti-trypanosomal diamidine 2,5-bis(4-amidinophenyl)furan (DB75) and its N-methoxy prodrug DB289 in murine brain tissue.
Bagnell, CR; Brock, JL; Hall, JE; Sturk, LM; Tidwell, RR, 2004
)
0.32
" Oral doses were well absorbed (approximately 50-70%) and effectively converted to DB75 in both species but subject to first-pass metabolism and hepatic retention, limiting its systemic bioavailability to 10 to 20%."( Pharmacokinetics and metabolism of the prodrug DB289 (2,5-bis[4-(N-methoxyamidino)phenyl]furan monomaleate) in rat and monkey and its conversion to the antiprotozoal/antifungal drug DB75 (2,5-bis(4-guanylphenyl)furan dihydrochloride).
Boykin, DW; Cybulski, ZR; Fitzpatrick, K; Henderson, SJ; Houchen, TL; John, BA; McBurney, A; Midgley, I; Taylor, LM; Trendler, KL; Wright, SJ, 2007
)
0.34
" Pafuramidine (DB289) is an orally bioavailable prodrug of furamidine (DB75), an investigational diamidine that is less toxic than previous diamidines such as pentamidine."( Pafuramidine for Pneumocystis jiroveci pneumonia in HIV-infected individuals.
Aberg, JA; Chen, D; Marsh, R, 2007
)
2.69
" An orally bioavailable prodrug of CPD-0801, DB868, is metabolized primarily in the liver to the active form."( Application of monoclonal antibodies to measure metabolism of an anti-trypanosomal compound in vitro and in vivo.
Generaux, CN; Goldsmith, RB; Gray, DR; Reisner, HM; Tidwell, RR; Yan, Z, 2010
)
0.36

Dosage Studied

ExcerptRelevanceReference
" Compound 6a produced cures at an oral dosage of 5 mg/kg."( Synthesis and antiprotozoal activity of aza-analogues of furamidine.
Boykin, DW; Brun, R; Easterbrook, JD; Ismail, MA; Tanious, FA; Wilson, WD, 2003
)
0.32
" Although effective treatments for early-stage sleeping sickness exist, these drugs usually require extended dosing schedules and intravenous administration."( Distribution and quantitation of the anti-trypanosomal diamidine 2,5-bis(4-amidinophenyl)furan (DB75) and its N-methoxy prodrug DB289 in murine brain tissue.
Bagnell, CR; Brock, JL; Hall, JE; Sturk, LM; Tidwell, RR, 2004
)
0.32
" In addition, TMP-SMX has a moderate pill burden with three- to four-times daily dosing schedule."( Pafuramidine for Pneumocystis jiroveci pneumonia in HIV-infected individuals.
Aberg, JA; Chen, D; Marsh, R, 2007
)
1.78
" Complete cures were achieved with oral dosing of the prodrug DB289 in all three models without any overt toxicity."( Efficacy of the diamidine DB75 and its prodrug DB289, against murine models of human African trypanosomiasis.
Brun, R; Kagira, JM; Karanja, SM; Mdachi, RE; Ngotho, JM; Thuita, JK; Tidwell, R; Wenzler, T, 2008
)
0.35
" Sixteen healthy volunteers were dosed and challenged in a single cohort."( Phase I/II evaluation of the prophylactic antimalarial activity of pafuramidine in healthy volunteers challenged with Plasmodium falciparum sporozoites.
Bakshi, RP; Hendrix, CW; Kumar, N; Nyunt, MM; Shapiro, TA, 2009
)
0.59
" The amidoxime and N-methoxyamidine of 5a were the only produgs to provide cures (1/4 cures) in the same mouse model on oral dosage at 4x25mg/kg."( Synthesis and antiprotozoal activity of 2,5-bis[amidinoaryl]thiazoles.
Boykin, DW; Branowska, D; Brun, R; Farahat, AA; Kumar, A; Liu, Y; Wenzler, T; Wilson, WD, 2010
)
0.36
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (118)

Assay IDTitleYearJournalArticle
AID555924Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as change in packed cell volume at 10 mg/kg, po administered on day 28 post infection for 10 days measured on day 28 post treatment2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555490Antimicrobial activity against Trypanosoma brucei rhodesiense infected in vervet monkeys assessed as cure from infection at 3 mg/kg, po administered on day 7 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555694Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 482 assessed as time to detect parasitemia at 3 mg/kg, po administered on day 7 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555485Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as body weight change at 3 mg/kg, po administered on day 7 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID249181Apparent permeability determined across the Caco-2 cell monolayers in both basolateral (BL) to apical (AP) directions2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
O-alkoxyamidine prodrugs of furamidine: in vitro transport and microsomal metabolism as indicators of in vivo efficacy in a mouse model of Trypanosoma brucei rhodesiense infection.
AID555722Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as body weight change at 1 mg/kg, po administered on day 7 post infection for 5 days measured on day 28 post treatment2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID269499Antiprotozoal activity in mouse infected with Trypanosoma brucei rhodesiense STIB900 measured as average days of survival at 25 mg/kg, po2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis, DNA affinity, and antiprotozoal activity of linear dications: Terphenyl diamidines and analogues.
AID625276FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
AID555689Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 484 assessed as time to detect CSF parasitosis at 1 mg/kg, po administered on day 7 post infection for 5 days measured after 7 to 14 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555699Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 483 assessed as time to detect CSF parasitosis at 3 mg/kg, po administered on day 7 post infection for 5 days measured after 7 to 14 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID562711Antitrypanosomal activity against Trypanosoma brucei brucei GVR35 infected in NMRI mouse CNS model assessed as survival of mouse at 100 mg/kg, po for 5 days2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID445265Antiplasmodial activity against Plasmodium vivax infected in mice (Mus musculus) assessed as inhibition of parasitaemia at 30 mg/kg, subcutaneous for 4 days2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Synthesis and antiprotozoal activity of cationic 1,4-diphenyl-1H-1,2,3-triazoles.
AID555711Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 488 assessed as time to detect parasitemia in wet films of blood at 10 mg/kg, po administered on day 14 post infection for 5 days measured after 7 to 14 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID562709Antitrypanosomal activity against Trypanosoma brucei brucei GVR35 infected in NMRI mouse CNS model assessed as cure from infection at 25 mg/kg, po for 10 days2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID555718Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 501 assessed as time to detect CSF parasitosis at 10 mg/kg, po administered on day 28 post infection for 10 days measured after 7 to 14 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID269501Half life in B6C3F1 mouse liver microsome2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis, DNA affinity, and antiprotozoal activity of linear dications: Terphenyl diamidines and analogues.
AID322580Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected mouse model assessed as survival at 25 mg/kg, po after 4 days2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis and antiprotozoal activity of novel bis-benzamidino imidazo[1,2-a]pyridines and 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridines.
AID555709Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 478 assessed as cure from infection at 10 mg/kg, po administered on day 7 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID562510Antitrypanosomal activity against wild-type Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as survival of mouse at 50 mg/kg, po for 4 days2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID555696Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 482 assessed as time to detect CSF parasitosis at 3 mg/kg, po administered on day 7 post infection for 5 days measured after 14 to 21 days by microscopy2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555704Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 486 assessed as cure from infection at 10 mg/kg, po administered on day 7 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID625293Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in LTKB-BD2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID555720Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 520 assessed as time to detect CSF parasitosis at 10 mg/kg, po administered on day 28 post infection for 10 days measured after 7 to 14 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID249180Apparent permeability determined across the Caco-2 cell monolayers in both apical (AP) to basolateral (BL) directions2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
O-alkoxyamidine prodrugs of furamidine: in vitro transport and microsomal metabolism as indicators of in vivo efficacy in a mouse model of Trypanosoma brucei rhodesiense infection.
AID555495Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 463 assessed as time to detect CSF parasitosis at 1 mg/kg, po administered on day 7 post infection for 5 days measured after 7 to 14 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555919Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as change in packed cell volume at 10 mg/kg, po administered on day 28 post infection for 10 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555703Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 468 assessed as cure from infection at 10 mg/kg, po administered on day 7 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID382515Antimicrobial activity against Pneumocystis carinii in immunosuppressed rat assessed as number of cysts/g of lung at 22.0 umol/kg/day, iv relative to control2008European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
Carbamate prodrugs of N-alkylfuramidines.
AID779099Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as cured animal at 10 mg/kg, ip administered on day 3 post infection for 4 days measured up to 60 days2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues.
AID555922Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as change in packed cell volume at 10 mg/kg, po administered on day 7 post infection for 5 days measured on day 28 post treatment2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID562713Antitrypanosomal activity against Trypanosoma brucei brucei GVR35 infected in NMRI mouse CNS model assessed as survival of mouse at 25 mg/kg, po for 5 days2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID555710Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 488 assessed as time to detect parasitemia at 10 mg/kg, po administered on day 14 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555701Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 411 assessed as cure from infection at 3 mg/kg, po administered on day 7 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID779110Half life in mouse liver microsomes by UV-HPLC analysis2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues.
AID555727Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as change in packed cell volume at 1 mg/kg, po administered on day 7 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555719Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 520 assessed as time to detect parasitemia at 10 mg/kg, po administered on day 28 post infection for 10 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555725Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as body weight change at 10 mg/kg, po administered on day 14 post infection for 5 days measured on day 28 post treatment2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID246019In vivo effect (cures) determined by number of mice that survived (2) and are parasite free (4) for 60 days upon intraperitoneal dose, observed in STIB900 mouse model2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
O-alkoxyamidine prodrugs of furamidine: in vitro transport and microsomal metabolism as indicators of in vivo efficacy in a mouse model of Trypanosoma brucei rhodesiense infection.
AID555730Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as change in packed cell volume at 10 mg/kg, po administered on day 14 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555715Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 490 assessed as time to detect CSF parasitosis at 10 mg/kg, po administered on day 28 post infection for 10 days measured after 14 to 21 days by microscopy2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555724Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as body weight change at 10 mg/kg, po administered on day 7 post infection for 5 days measured on day 28 post treatment2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555921Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as change in packed cell volume at 3 mg/kg, po administered on day 7 post infection for 5 days measured on day 28 post treatment2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID252574In vivo effect on average days of survival was measured upon oral dose at 100 mg/kg in STIB900 mouse model2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
O-alkoxyamidine prodrugs of furamidine: in vitro transport and microsomal metabolism as indicators of in vivo efficacy in a mouse model of Trypanosoma brucei rhodesiense infection.
AID555729Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as change in packed cell volume at 10 mg/kg, po administered on day 7 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555492Antimicrobial activity against Trypanosoma brucei rhodesiense infected in vervet monkeys assessed as cure from infection at 10 mg/kg, po administered on day 7 post infection for 10 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555497Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 484 assessed as time to detect parasitemia at 1 mg/kg, po administered on day 7 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555697Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 483 assessed as time to detect parasitemia at 3 mg/kg, po administered on day 7 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555493Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 463 assessed as time to detect parasitemia at 1 mg/kg, po administered on day 7 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID562712Antitrypanosomal activity against Trypanosoma brucei brucei GVR35 infected in NMRI mouse CNS model assessed as survival of mouse at 50 mg/kg, po for 5 days2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID213471In vitro inhibitory activity against Trypanosoma brucei rhodesiense2004Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
Novel dicationic imidazo[1,2-a]pyridines and 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridines as antiprotozoal agents.
AID118272Number of mice (out of 4) cured from Trypanosoma brucei rhodesiense infection which are parasite free for 60 days was determined at p.o. dose of 100 mg/kg2004Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
Novel dicationic imidazo[1,2-a]pyridines and 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridines as antiprotozoal agents.
AID555695Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 482 assessed as time to detect parasitemia in wet films of blood at 3 mg/kg, po administered on day 7 post infection for 5 days by hematocrit centrifugation techniq2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555702Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 454 assessed as cure from infection at 10 mg/kg, po administered on day 7 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555688Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 484 assessed as time to detect parasitemia in wet films of blood at 1 mg/kg, po administered on day 7 post infection for 5 days by hematocrit centrifugation techniq2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID779097Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as mouse survival at 25 mg/kg, ip administered on day 3 post infection for 4 days measured up to 60 days2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues.
AID1426420Antimalarial activity against Plasmodium falciparum in infected patient assessed as cure rate at 100 mg, po bid administered for 5 days measured every 12 hrs up to day 7, and on day 10, 14, 21, and 28 by Giemsa staining-based assay relative to control2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID382522Toxicity against immunosuppressed rat pneumocystis model at 33.0 umol/kg/day, po2008European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
Carbamate prodrugs of N-alkylfuramidines.
AID158689In vitro inhibitory activity for Plasmodium falciparum2004Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
Novel dicationic imidazo[1,2-a]pyridines and 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridines as antiprotozoal agents.
AID555717Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 501 assessed as time to detect parasitemia in wet films of blood at 10 mg/kg, po administered on day 28 post infection for 10 days by hematocrit centrifugation tech2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID252576In vivo effect on average days of survival was measured upon oral dose at 400 mg/kg in STIB900 mouse model2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
O-alkoxyamidine prodrugs of furamidine: in vitro transport and microsomal metabolism as indicators of in vivo efficacy in a mouse model of Trypanosoma brucei rhodesiense infection.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID445264Antiplasmodial activity against Plasmodium falciparum infected in mice (Mus musculus) assessed as inhibition of parasitaemia at 30 mg/kg, subcutaneous for 4 days2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Synthesis and antiprotozoal activity of cationic 1,4-diphenyl-1H-1,2,3-triazoles.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID555716Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 501 assessed as time to detect parasitemia at 10 mg/kg, po administered on day 28 post infection for 10 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555487Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as body weight change at 10 mg/kg, po administered on day 14 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID246018In vivo effect (cures) determined by number of mice that survived (1) and are parasite free (4) for 60 days upon intraperitoneal dose, observed in STIB900 mouse model2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
O-alkoxyamidine prodrugs of furamidine: in vitro transport and microsomal metabolism as indicators of in vivo efficacy in a mouse model of Trypanosoma brucei rhodesiense infection.
AID555700Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 483 assessed as time to detect CSF parasitosis at 3 mg/kg, po administered on day 7 post infection for 5 days measured after 14 to 21 days by microscopy2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555723Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as body weight change at 3 mg/kg, po administered on day 7 post infection for 5 days measured on day 28 post treatment2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555706Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 471 assessed as time to detect parasitemia in wet films of blood at 1 mg/kg, po administered on day 14 post infection for 5 days by hematocrit centrifugation techni2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID562707Antitrypanosomal activity against Trypanosoma brucei brucei GVR35 infected in NMRI mouse CNS model assessed as cure from infection at 25 mg/kg, po for 5 days2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID555693Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 485 assessed as time to detect CSF parasitosis at 1 mg/kg, po administered on day 7 post infection for 5 days measured after 14 to 21 days by microscopy2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID481849Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 in infected mouse model assessed as host survival time at 25 mg/kg, po for 4 days2010Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10
Synthesis and antiprotozoal activity of 2,5-bis[amidinoaryl]thiazoles.
AID382516Antimicrobial activity against Pneumocystis carinii in immunosuppressed rat assessed as number of cysts/g of lung at 33.0 umol/kg/day, po relative to control2008European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
Carbamate prodrugs of N-alkylfuramidines.
AID562507Antitrypanosomal activity against wild-type Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as cure from infection at 50 mg/kg, po for 4 days2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID555489Antimicrobial activity against Trypanosoma brucei rhodesiense infected in vervet monkeys assessed as cure from infection at 1 mg/kg, po administered on day 7 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555707Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 471 assessed as time to detect CSF parasitosis at 10 mg/kg, po administered on day 14 post infection for 5 days measured after 7 to 14 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID562706Antitrypanosomal activity against Trypanosoma brucei brucei GVR35 infected in NMRI mouse CNS model assessed as cure from infection at 50 mg/kg, po for 5 days2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID779112Half life in human liver microsomes by UV-HPLC analysis2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues.
AID779094Antitrypanosomal activity against Trypanosoma brucei brucei GVR35 infected in NMRI mouse assessed as mouse survival at 100 mg/kg, po administered on day 21 post infection for 5 days measured up to 180 days2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues.
AID555491Antimicrobial activity against Trypanosoma brucei rhodesiense infected in vervet monkeys assessed as cure from infection at 10 mg/kg, po administered on day 7 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID162418In vitro binding affinity towards Poly (dA-dT)22004Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
Novel dicationic imidazo[1,2-a]pyridines and 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridines as antiprotozoal agents.
AID382525Toxicity against immunosuppressed rat pneumocystis model at 22.0 umol/kg/day, iv2008European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
Carbamate prodrugs of N-alkylfuramidines.
AID555713Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 488 assessed as time to detect CSF parasitosis at 10 mg/kg, po administered on day 28 post infection for 10 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555923Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as change in packed cell volume at 10 mg/kg, po administered on day 14 post infection for 5 days measured on day 28 post treatment2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555920Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as change in packed cell volume at 1 mg/kg, po administered on day 7 post infection for 5 days measured on day 28 post treatment2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID124389No. of mice that survived T.b. rhodesiense infection and are parasite free for 60 days was determined at dose of 50 mg/kg by p.o. administration; 5 animals tested2003Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
Synthesis and antiprotozoal activity of aza-analogues of furamidine.
AID246020In vivo effect (cures) determined by number of mice that survived (4) and are parasite free (4) for 60 days upon intraperitoneal dose, observed in STIB900 mouse model2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
O-alkoxyamidine prodrugs of furamidine: in vitro transport and microsomal metabolism as indicators of in vivo efficacy in a mouse model of Trypanosoma brucei rhodesiense infection.
AID124116In vivo average survival rate of mouse infected by T.b. rhodesiense was determined for a period of 60 days at dose of 50 mg/kg by p.o. administration2003Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
Synthesis and antiprotozoal activity of aza-analogues of furamidine.
AID555488Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as body weight change at 10 mg/kg, po administered on day 28 post infection for 10 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555728Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as change in packed cell volume at 3 mg/kg, po administered on day 7 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555494Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 463 assessed as time to detect parasitemia in wet films of blood at 1 mg/kg, po administered on day 7 post infection for 5 days by hematocrit centrifugation techniq2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555691Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 485 assessed as time to detect parasitemia in wet films of blood at 1 mg/kg, po administered on day 7 post infection for 5 days by hematocrit centrifugation techniq2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555484Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as body weight change at 1 mg/kg, po administered on day 7 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID562716Antitrypanosomal activity against Trypanosoma brucei brucei GVR35 infected in NMRI mouse CNS model assessed as survival of mouse at 25 mg/kg, po for 10 days2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID555705Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 471 assessed as time to detect parasitemia at 10 mg/kg, po administered on day 14 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555714Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 490 assessed as time to detect parasitemia at 10 mg/kg, po administered on day 28 post infection for 10 days measured after 7 to 14 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID117934In vivo average survival days of mice infected by Trypanosoma brucei rhodesiense was determined for a period of 60 days at p.o. dose of 100 mg/kg2004Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
Novel dicationic imidazo[1,2-a]pyridines and 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridines as antiprotozoal agents.
AID562508Antitrypanosomal activity against wild-type Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as cure from infection at 25 mg/kg, po for 4 days2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID555486Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as body weight change at 10 mg/kg, po administered on day 7 post infection for 5 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555692Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 485 assessed as time to detect CSF parasitosis at 1 mg/kg, po administered on day 7 post infection for 5 days measured after 7 to 14 days2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID481846Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 in infected mouse model assessed as parasitemia cure in host at 5 mg/kg, ip for 4 days2010Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10
Synthesis and antiprotozoal activity of 2,5-bis[amidinoaryl]thiazoles.
AID779100Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as cured animal at 25 mg/kg, ip administered on day 3 post infection for 4 days measured up to 60 days2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues.
AID555698Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 483 assessed as time to detect parasitemia in wet films of blood at 3 mg/kg, po administered on day 7 post infection for 5 days by hematocrit centrifugation techniq2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID779096Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as mouse survival at 10 mg/kg, ip administered on day 3 post infection for 4 days measured up to 60 days2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues.
AID237672Half-life in human liver microsomes was determined2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
O-alkoxyamidine prodrugs of furamidine: in vitro transport and microsomal metabolism as indicators of in vivo efficacy in a mouse model of Trypanosoma brucei rhodesiense infection.
AID481848Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 in infected mouse model assessed as host survival time at 5 mg/kg, ip for 4 days2010Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10
Synthesis and antiprotozoal activity of 2,5-bis[amidinoaryl]thiazoles.
AID555496Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 463 assessed as time to detect CSF parasitosis at 1 mg/kg, po administered on day 7 post infection for 5 days measured after 14 to 21 days by microscopy2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID562715Antitrypanosomal activity against Trypanosoma brucei brucei GVR35 infected in NMRI mouse CNS model assessed as survival of mouse at 50mg/kg, po for 10 days2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID555690Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 484 assessed as time to detect CSF parasitosis at 1 mg/kg, po administered on day 7 post infection for 5 days measured after 14 to 21 days by microscopy2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555712Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 488 assessed as time to detect CSF parasitosis at 10 mg/kg, po administered on day 14 post infection for 5 days measured after 14 to 21 days by microscopy2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID562511Antitrypanosomal activity against wild-type Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as survival of mouse at 25 mg/kg, po for 4 days2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID1426419Antimalarial activity against hypnozoite-stage Plasmodium vivax in infected patient assessed as cure rate at 100 mg, po bid administered for 5 days measured every 12 hrs up to day 7, and on day 10, 14, 21, and 28 by Giemsa staining-based assay relative to2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID555721Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 520 assessed as time to detect CSF parasitosis at 10 mg/kg, po administered on day 28 post infection for 10 days measured after 14 to 21 days by microscopy2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID555726Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey assessed as body weight change at 10 mg/kg, po administered on day 28 post infection for 10 days measured on day 28 post treatment2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
AID252575In vivo effect on average days of survival was measured upon oral dose at 200 mg/kg in STIB900 mouse model2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
O-alkoxyamidine prodrugs of furamidine: in vitro transport and microsomal metabolism as indicators of in vivo efficacy in a mouse model of Trypanosoma brucei rhodesiense infection.
AID481847Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 in infected mouse model assessed as parasitemia cure in host at 25 mg/kg, po for 4 days2010Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10
Synthesis and antiprotozoal activity of 2,5-bis[amidinoaryl]thiazoles.
AID248592In vitro inhibitory activity against Trypanosoma brucei rhodesiense evaluated in acute mouse model of trypanosomiasis2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
O-alkoxyamidine prodrugs of furamidine: in vitro transport and microsomal metabolism as indicators of in vivo efficacy in a mouse model of Trypanosoma brucei rhodesiense infection.
AID555708Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in vervet monkey 471 assessed as time to detect CSF parasitosis at 10 mg/kg, po administered on day 14 post infection for 5 days measured after 14 to 21 days by microscopy2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (42)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's27 (64.29)29.6817
2010's15 (35.71)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.11

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index18.11 (24.57)
Research Supply Index3.85 (2.92)
Research Growth Index4.33 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.11)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (9.52%)5.53%
Reviews7 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other31 (73.81%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (5)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Phase II b Trial of DB289 for the Treatment of Stage I African Trypanosomiasis [NCT00803933]Phase 2111 participants (Actual)Interventional2003-02-28Completed
Randomized, Double-Blind Phase 1 Safety and Tolerability Study of Pafuramidine Maleate (DB289) in Healthy Subjects [NCT00619346]Phase 1100 participants (Actual)Interventional2007-11-30Terminated(stopped due to FDA Full Clinical Hold due to safety concerns, as of 12/21/07)
Phase II A Trial of DB289 for the Treatment of Stage I African Trypanosomiasis [NCT00802594]Phase 230 participants (Actual)Interventional2001-08-31Completed
International Randomized, Controlled Phase 3 Trial of DB289 Versus Trimethoprim-sulfamethoxazole for the Treatment of Acute Pneumocystis Jiroveci Pneumonia (PCP) in Patients With HIV/AIDS [NCT00302341]Phase 348 participants (Actual)Interventional2006-05-31Terminated(stopped due to FDA Clinical Hold as of 12/21/07 due to safety concerns)
Prophylactic Antimalarial Activity of DB289 in Volunteers Challenged With Plasmodium Falciparum [NCT00408369]Phase 1/Phase 219 participants (Anticipated)Interventional2006-11-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]