Compounds > fexinidazole
Page last updated: 2024-12-06

fexinidazole

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Description

Fexinidazole is a nitroimidazole drug that has shown promise in the treatment of African trypanosomiasis, also known as sleeping sickness. It is effective against both the bloodstream and the central nervous system stages of the disease, which is a significant advantage over older treatments. Fexinidazole is administered orally, which is more convenient and less invasive than the injections required for other drugs. The compound is being studied because it is well tolerated, has a long half-life, and exhibits good pharmacokinetic properties. It is important to note that fexinidazole is not yet widely available, and further research is ongoing to evaluate its long-term safety and efficacy.'

fexinidazole: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID68792
CHEMBL ID1631694
SCHEMBL ID1163575
MeSH IDM0115392

Synonyms (50)

Synonym
fexinidazole
hoe-239
1-methyl-2-[(4-methylsulfanylphenoxy)methyl]-5-nitroimidazole
59729-37-2
CHEMBL1631694
hoe 239
1-methyl-2-((4-(methylthio)phenoxy)methyl)-5-nitro-1h-imidazole
AKOS016010427
unii-306erl82ir
fexinidazolum [inn-latin]
who 4142
fexinidazolum
fexinidazol [inn-spanish]
fexinidazol
fexinidazole [usan:inn]
1-methyl-2-((p-(methylthio)phenoxy)methyl)-5-nitroimidazole
306erl82ir ,
S2600 ,
1h-imidazole, 1-methyl-2-((4-(methylthio)phenoxy)methyl)-5-nitro-
1-methyl-2-{[4-(methylthio)phenoxy]methyl}-5-nitro-1h-imidazole
fexinidazole [inn]
fexinidazole [orange book]
fexinidazole [who-dd]
fexinidazole [usan]
MLS006010234
smr004701311
SCHEMBL1163575
MIWWSGDADVMLTG-UHFFFAOYSA-N
1-methyl-2-(4-methylthiophenyloxymethyl)-5-nitro-imidazole
1-methyl-2-(4-methylthiophenyl-oxymethyl)-5-nitro-imidazole
DTXSID00208448 ,
CS-5535
HY-13801
mfcd00866607
1-methyl-2-((4-(methylthio)phenoxy)-methyl)-5-nitro-1h-imidazole
fexinidazole (hoe-239)
DB12265
BCP07460
Q5446115
fexinidazole (usan/inn)
D11252
SB16940
A869137
fexinidazolum (inn-latin)
dtxcid20130939
p01ca03
fexinidazol (inn-spanish)
1-methyl-2-{[4-(methylsulfanyl)phenoxy]methyl}-5-nitro-1h-imidazole
EN300-7359421
Z1741981510

Research Excerpts

Overview

Fexinidazole (FEX) is a heterocyclic compound and constitutes the first 100% oral treatment drug for African trypanosomiasis. The drug is a valuable first-line treatment option in the early stages of g-HAT.

ExcerptReferenceRelevance
"Oral fexinidazole is a safe and effective first-line treatment option across all gambiense human African trypanosomiasis disease stages in paediatric patients."( Safety and efficacy of oral fexinidazole in children with gambiense human African trypanosomiasis: a multicentre, single-arm, open-label, phase 2-3 trial.
Bardonneau, C; Bernhard, S; Blesson, S; Delhomme, S; Fina Lubaki, JP; Ilunga Wa Kyhi, M; Kande Betu Kumesu, V; Kaninda Badibabi, L; Kasongo Bonama, A; Kavunga Lukula, P; Kuziena Mindele, W; Lumbala, C; Lumeya Vuvu, S; Mahenzi Mbembo, H; Mandula Mokenge, G; Mutombo Kalonji, W; Nganzobo Ngima, P; Ngolo Tete, D; Scherrer, B; Simon, F; Strub-Wourgaft, N; Tarral, A; Valverde Mordt, O, 2022)		1.53
"Fexinidazole (FEX) is a heterocyclic compound and constitutes the first 100% oral treatment drug for African trypanosomiasis. "( Fexinidazole interferes with the growth and structural organization of Trypanosoma cruzi.
de Souza, W; Zuma, AA, 2022)		3.61
"Fexinidazole is a valuable first-line treatment option in the early stages of g-HAT."( Oral fexinidazole for stage 1 or early stage 2 African Trypanosoma brucei gambiense trypanosomiasis: a prospective, multicentre, open-label, cohort study.
Akwaso Masa, F; Bardonneau, C; Bernhard, S; Blesson, S; Botalema Bolengi, F; Delhomme, S; Kande Betu Ku Mesu, V; Kapongo Tshilumbwa, S; Lumbala, C; Lumeya Vuvu, S; Mahenzi Mbembo, H; Mayala Malu, T; Mpia Moke, C; Mpoyi Muamba Nzambi, D; Mudji E'kitiak, J; Mukendi Ilunga, M; Mutombo Kalonji, W; Ngolo Tete, D; Nkieri Matsho, M; Scherrer, B; Simon, F; Strub-Wourgaft, N; Tarral, A; Valverde Mordt, O, 2021)		2.58
"Fexinidazole is a 5-nitroimidazole recently included in a clinical efficacy trial as an oral drug for the treatment of human African trypanosomiasis (HAT). "( Determination of an optimal dosing regimen for fexinidazole, a novel oral drug for the treatment of human African trypanosomiasis: first-in-human studies.
Blesson, S; Bray, MA; Evène, E; Felices, M; Gualano, V; Hovsepian, L; Mordt, OV; Sassella, D; Strub-Wourgaft, N; Tarral, A; Torreele, E, 2014)		2.1
"Fexinidazole (FEX) is a nitroimidazole being developed as a new trypanocide treatment for human African trypanosomiasis/sleeping sickness. "( A DBS method for quantitation of the new oral trypanocidal drug fexinidazole and its active metabolites.
Abgrall, A; Augé, C; Blesson, S; Filali-Ansary, A; Mordt, OV; Pellissier, F; Sanderink, GJ; Souchaud, M, 2016)		2.12
"Fexinidazole is a 5-nitroimidazole drug currently in clinical development for the treatment of human sleeping sickness (human African trypanosomiasis [HAT]), caused by infection with species of the protozoan parasite Trypanosoma brucei. "( Antitrypanosomal activity of fexinidazole, a new oral nitroimidazole drug candidate for treatment of sleeping sickness.
Bourdin Trunz, B; Bray, MA; Brun, R; Cal, M; Kaiser, M; Torreele, E, 2011)		2.1
"Fexinidazole is an effective oral treatment of acute and chronic experimental CD caused by benznidazole-susceptible, partially resistant, and resistant T. "( Fexinidazole: a potential new drug candidate for Chagas disease.
Bahia, MT; Caldas, IS; de Andrade, IM; Diniz, Lde F; do Nascimento, ÁF; Martins, TA; Ribeiro, I; Talvani, A; Torreele, E; Trunz, BB, 2012)		3.26

Effects

ExcerptReferenceRelevance
"Fexinidazole has been reported as an effective oral monotherapy against non-severe gambiense human African trypanosomiasis in a recent trial in adults. "( Safety and efficacy of oral fexinidazole in children with gambiense human African trypanosomiasis: a multicentre, single-arm, open-label, phase 2-3 trial.
Bardonneau, C; Bernhard, S; Blesson, S; Delhomme, S; Fina Lubaki, JP; Ilunga Wa Kyhi, M; Kande Betu Kumesu, V; Kaninda Badibabi, L; Kasongo Bonama, A; Kavunga Lukula, P; Kuziena Mindele, W; Lumbala, C; Lumeya Vuvu, S; Mahenzi Mbembo, H; Mandula Mokenge, G; Mutombo Kalonji, W; Nganzobo Ngima, P; Ngolo Tete, D; Scherrer, B; Simon, F; Strub-Wourgaft, N; Tarral, A; Valverde Mordt, O, 2022)		2.46

Treatment

ExcerptReferenceRelevance
"Fexinidazole treatment was also shown to reduce myocarditis in all animals infected with VL-10 or Colombian resistant T."( Fexinidazole: a potential new drug candidate for Chagas disease.
Bahia, MT; Caldas, IS; de Andrade, IM; Diniz, Lde F; do Nascimento, ÁF; Martins, TA; Ribeiro, I; Talvani, A; Torreele, E; Trunz, BB, 2012)		2.54

Toxicity

Oral fexinidazole is a safe and effective first-line treatment option across all gambiense human African trypanosomiasis disease stages. It was rediscovered by the Drugs for Neglected Diseases initiative (DNDi) after extensive compound mining.

ExcerptReferenceRelevance
" Fexinidazole, a 2-substituted 5-nitroimidazole rediscovered by the Drugs for Neglected Diseases initiative (DNDi) after extensive compound mining of public and pharmaceutical company databases, has the potential to become a short-course, safe and effective oral treatment, curing both acute and chronic HAT."( Genotoxicity profile of fexinidazole--a drug candidate in clinical development for human African trypanomiasis (sleeping sickness).
Bourdin Trunz, B; Torreele, E; Tweats, D, 2012)		1.6
" Overall, 116 (93%) of 125 patients reported 586 treatment-emergent adverse events, mainly mild or moderate."( Safety and efficacy of oral fexinidazole in children with gambiense human African trypanosomiasis: a multicentre, single-arm, open-label, phase 2-3 trial.
Bardonneau, C; Bernhard, S; Blesson, S; Delhomme, S; Fina Lubaki, JP; Ilunga Wa Kyhi, M; Kande Betu Kumesu, V; Kaninda Badibabi, L; Kasongo Bonama, A; Kavunga Lukula, P; Kuziena Mindele, W; Lumbala, C; Lumeya Vuvu, S; Mahenzi Mbembo, H; Mandula Mokenge, G; Mutombo Kalonji, W; Nganzobo Ngima, P; Ngolo Tete, D; Scherrer, B; Simon, F; Strub-Wourgaft, N; Tarral, A; Valverde Mordt, O, 2022)		1.02
"Oral fexinidazole is a safe and effective first-line treatment option across all gambiense human African trypanosomiasis disease stages in paediatric patients."( Safety and efficacy of oral fexinidazole in children with gambiense human African trypanosomiasis: a multicentre, single-arm, open-label, phase 2-3 trial.
Bardonneau, C; Bernhard, S; Blesson, S; Delhomme, S; Fina Lubaki, JP; Ilunga Wa Kyhi, M; Kande Betu Kumesu, V; Kaninda Badibabi, L; Kasongo Bonama, A; Kavunga Lukula, P; Kuziena Mindele, W; Lumbala, C; Lumeya Vuvu, S; Mahenzi Mbembo, H; Mandula Mokenge, G; Mutombo Kalonji, W; Nganzobo Ngima, P; Ngolo Tete, D; Scherrer, B; Simon, F; Strub-Wourgaft, N; Tarral, A; Valverde Mordt, O, 2022)		1.53

Compound-Compound Interactions

ExcerptReferenceRelevance
" When these gels are used in combination with melarsoprol gel they are capable of curing experimental murine CNS-trypanosomiasis with a one-day treatment."( Topical chemotherapy for experimental murine African CNS-trypanosomiasis: the successful use of the arsenical, melarsoprol, combined with the 5-nitroimidazoles, fexinidazole or MK-436.
Atouguia, JM; Jennings, FW; Murray, M, 1996)		0.49

Bioavailability

ExcerptReferenceRelevance
" In laboratory animals, fexinidazole is well absorbed after oral administration and readily distributes throughout the body, including the brain."( Fexinidazole--a new oral nitroimidazole drug candidate entering clinical development for the treatment of sleeping sickness.
Bourdin Trunz, B; Bray, MA; Brun, R; Kaiser, M; Mazué, G; Pécoul, B; Torreele, E; Tweats, D, 2010)		2.11
" The 7-nitroquinoxalin-2-one and 5-nitroindazole scaffold derivatives 58 and 35, respectively, are particularly interesting because of their established oral bioavailability in mice."( Discovery of nitroheterocycles active against African trypanosomes. In vitro screening and preliminary SAR studies.
Arán, VJ; Dardonville, C; Kaiser, M, 2012)		0.38

Dosage Studied

Fezinidazole stands poised to replace the current treatment regimen for Trypanosoma brucei gambiense infections, following a positive Phase 2/3 clinical trial. Fourteen-day multiple ascending dosing administered up to 3,600 mg/day in fasted conditions showed that fexinidrazole was generally well-tolerated.

ExcerptRelevanceReference
" A combination chemotherapy, eflornithine alongside nifurtimox, has been introduced to decrease the time frame and overall dosing of eflornithine and reducing the risk of drug resistance emerging."( Potential new drugs for human African trypanosomiasis: some progress at last.
Barrett, MP, 2010)		0.36
" Fourteen-day multiple ascending dosing administered up to 3,600 mg/day in fasted conditions showed that fexinidazole was generally well-tolerated (mild to moderate, spontaneously reversible drug-related adverse events)."( Determination of an optimal dosing regimen for fexinidazole, a novel oral drug for the treatment of human African trypanosomiasis: first-in-human studies.
Blesson, S; Bray, MA; Evène, E; Felices, M; Gualano, V; Hovsepian, L; Mordt, OV; Sassella, D; Strub-Wourgaft, N; Tarral, A; Torreele, E, 2014)		0.87
" Pharmacokinetic data suggested that biological efficacy most likely resides with the sulfone metabolite (or subsequent reactive metabolites formed following reduction of the nitro group) following administration of either the sulfoxide or the sulfone and that prolonged plasma exposure over the 24-h dosing window is required to achieve high cure rates."( Antitrypanosomal activity of fexinidazole metabolites, potential new drug candidates for Chagas disease.
Bahia, MT; Caldas, IS; Charman, SA; Chatelain, E; Diniz, Lde F; Gonçalves, KR; Koltun, M; Marques, LF; Mazzeti, AL; Mota, LW; Nascimento, AF; Saunders, J; Scandale, I; Shackleford, DM; Talvani, A; White, KL, 2014)		0.69
"Decades after the last new chemical entity was added to the pharmacopeia for human African trypanosomiasis (or sleeping sickness), orally dosed fexinidazole stands poised to replace the current treatment regimen for Trypanosoma brucei gambiense infections, following a positive Phase 2/3 clinical trial."( Fexinidazole: A New Drug for African Sleeping Sickness on the Horizon.
Pollastri, MP, 2018)		2.12
" Following initial profiling, a first proof-of-concept in vivo study was undertaken, in which once daily oral dosing of a 7-substituted 2-nitroimidazooxazine analogue suppressed blood parasitemia to low or undetectable levels, although sterile cure was not achieved."( Re-evaluating pretomanid analogues for Chagas disease: Hit-to-lead studies reveal both in vitro and in vivo trypanocidal efficacy.
Avery, VM; Charman, SA; Chatelain, E; Cornwall, S; Denny, WA; Francisco, AF; Keenan, M; Kelly, JM; Marshall, AJ; O'Connor, PD; Perez, CJ; Read, KD; Riley, J; Sykes, ML; Thompson, AM; Thompson, RCA; White, KL; Zulfiqar, B, 2020)		0.56
" The pharmacokinetic profile required definition of a higher loading dosage for the first 4 days and administration of the daily dose together with a typical local meal to optimize product absorption and rapidly achieve drug steady state."( Development and Introduction of Fexinidazole into the Global Human African Trypanosomiasis Program.
Strub-Wourgaft, N; Tarral, A; Valverde Mordt, O, 2022)		1
"Further evaluation is needed to establish fexinidazole's minimum effective dosage and risk-benefit relationship."( A Phase 2, Randomized, Multicenter, Placebo-Controlled, Proof-of-Concept Trial of Oral Fexinidazole in Adults With Chronic Indeterminate Chagas Disease.
Barreira, F; Bilbe, G; Blum, B; Gascón, J; Ortiz, L; Palacios, A; Pinazo, MJ; Pinto, J; Ribeiro, I; Rojas, G; Schijman, AG; Strub-Wourgaft, N; Torrico, F; Vaillant, M, 2023)		1.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (79)

Assay IDTitleYearJournalArticle
AID1368587Antitrypanosomal activity against Trypanosoma brucei brucei TREU 667 infected in Swiss Webster mouse assessed as infection cure rate at 200 mg/kg, po qd for 5 days2018Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides.
AID780200Antimicrobial activity against Leishmania donovani amastigotes2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Targeting the human parasite Leishmania donovani: discovery of a new promising anti-infectious pharmacophore in 3-nitroimidazo[1,2-a]pyridine series.
AID548292Antimicrobial activity against Trypanosoma brucei NfxR1 infected in mouse assessed as decrease in parasitemia level at 200 mg/kg, ip QD for 3 days measured on day 60 by neubuaer hemocytometry2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID1368448Apparent permeability in MDCK2-MDR1 cells at 3 uM incubated over 150 mins at 37 degC by LC-MS/MS method2018Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides.
AID1406961Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay2018European journal of medicinal chemistry, Sep-05, Volume: 1578-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases.
AID1742369Antileishmanial activity against Leishmania infantum MHOM/MA/67/ITMAP-263 axenic amastigotes assessed as inhibition of parasitic metabolic activity incubated for 48 hrs by steady Glow reagent based luminescence assay
AID693076Redox potential of the compound assessed as one electron redox potential by pulse radiolysis method2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
1-Aryl-4-nitro-1H-imidazoles, a new promising series for the treatment of human African trypanosomiasis.
AID1586948Selectivity index, ratio of CC50 for human HepG2 cells to IC50 for promastigote stage of Leishmania donovani MHOM/IN/00/DEVI2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Nongenotoxic 3-Nitroimidazo[1,2-
AID548282Antimicrobial activity against Trypanosoma brucei NfxR22010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID1406964Selectivity index, ratio of CC50 for human HepG2 cells to IC50 for trypomastigote stage of Trypanosoma brucei brucei AnTat 1.92018European journal of medicinal chemistry, Sep-05, Volume: 1578-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases.
AID548281Antimicrobial activity against Trypanosoma brucei NfxR12010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID548301Antimicrobial activity against wild type Trypanosoma brucei infected in ip dosed NMRI administered QD for 3 days measured on day 6 by neubuaer hemocytometry2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID1528621Antitrypanosomal activity against Trypanosoma brucei gambiense infected in human assessed as cure rate administered orally for 10 days measured under phase 2/3 clinical trial studies2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Selectivity and Physicochemical Optimization of Repurposed Pyrazolo[1,5-
AID1740558Antileishmanial activity against Leishmania donovani MHOM/IN/00/DEVI promastigotes assessed as inhibition of metabolic activity measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 2028-Alkynyl-3-nitroimidazopyridines display potent antitrypanosomal activity against both T. b. brucei and cruzi.
AID568400Aqueous solubility of the compound at pH 7.5 at 25 degC2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Compounds containing 2-substituted imidazole ring for treatment against human African trypanosomiasis.
AID1586949Antileishmanial activity against intracellular amastigote stage of Leishmania donovani infected in human THP1 cells after 120 hrs by giemsa staining based microscopic analysis2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Nongenotoxic 3-Nitroimidazo[1,2-
AID1742367Antileishmanial activity against Leishmania donovani MHOM/IN/00/DEVI promastigotes assessed as inhibition of parasitic metabolic activity measured after 72 hrs by MTT assay
AID1406967Antileishmanial activity against intramacrophage amastigote stage of Leishmania donovani infected in human THP1 cells after 120 hrs by Giemsa staining based microscopy2018European journal of medicinal chemistry, Sep-05, Volume: 1578-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases.
AID548280Antimicrobial activity against Trypanosoma brucei2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID548294Cmax in NMRI mouse at 200 mg/kg, po after 15 mins2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID548290Antimicrobial activity against wild type Trypanosoma brucei infected NMRI assessed as cure rate at 50 mg/kg, ip QD for 3 days measured on day 6 by neubuaer hemocytometry2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID1548465Half life in NMRI mouse at 25 mg/Kg, ig measured up to 24 hrs by LCMS analysis
AID548283Selectivity ratio of EC50 for Trypanosoma brucei NfxR1 to EC50 for Trypanosoma brucei2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID1406977Electrochemical behavior of the compound assessed as redox potential corrected toward normal hydrogen electrode by cyclic voltammetry2018European journal of medicinal chemistry, Sep-05, Volume: 1578-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases.
AID568398Cytotoxicity against rat L6 cells after 72 hrs by SRB assay2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Compounds containing 2-substituted imidazole ring for treatment against human African trypanosomiasis.
AID1406960Antileishmanial activity against axenic amastigote stage of Leishmania infantum assessed as inhibition of parasite metabolic activity after 48 hrs by luciferase reporter gene based luminescence assay2018European journal of medicinal chemistry, Sep-05, Volume: 1578-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases.
AID548293Metabolic stability in blood of NMRI mouse assessed as accumulation of sulfoxide metabolite at 200 mg/kg, po measured after 2 hrs2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID692982Cytotoxicity against in rat L6 cells assessed as reduction in cell viability after 70 hrs by alamar blue assay2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
1-Aryl-4-nitro-1H-imidazoles, a new promising series for the treatment of human African trypanosomiasis.
AID1360419Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by MTT assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study.
AID1740563Cytotoxicity against human THP-1 cells assessed as reduction in cell viability after 72 hrs by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 2028-Alkynyl-3-nitroimidazopyridines display potent antitrypanosomal activity against both T. b. brucei and cruzi.
AID1480082Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 assessed as parasite growth inhibition after 72 hrs by Alamar blue assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design.
AID1740559Selectivity index, ratio of CC50 for cytotoxicity against human HepG2 cells to EC50 for antileishmanial activity against Leishmania donovani MHOM/IN/00/DEVI promastigotes2020European journal of medicinal chemistry, Sep-15, Volume: 2028-Alkynyl-3-nitroimidazopyridines display potent antitrypanosomal activity against both T. b. brucei and cruzi.
AID1586957Antitrypanosomal activity against trypomastigote stage of Trypanosoma brucei brucei AnTat 1.9 assessed as decrease in parasite viability after 69 hrs by Alamar Blue assay2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Nongenotoxic 3-Nitroimidazo[1,2-
AID1194921Antileishmanial activity against intracellular amastigote stage of Leishmania donovani MHOM/IN/00/DEVI infected in human THP1 cells assessed as decrease infected macrophages after 120 hrs by microscopy2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
Antileishmanial pharmacomodulation in 8-nitroquinolin-2(1H)-one series.
AID780199Antimicrobial activity against Leishmania donovani promastigotes2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Targeting the human parasite Leishmania donovani: discovery of a new promising anti-infectious pharmacophore in 3-nitroimidazo[1,2-a]pyridine series.
AID1548447Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
AID1740562Antitrypanosomal activity against Trypanosoma cruzi trypomastigotes infected in African green monkey Vero cells incubated for 120 hrs measured on day 6 cells followed by trypomastigotes release by haemocytometer-based light microscopy2020European journal of medicinal chemistry, Sep-15, Volume: 2028-Alkynyl-3-nitroimidazopyridines display potent antitrypanosomal activity against both T. b. brucei and cruzi.
AID1586945Antileishmanial activity against promastigote stage of Leishmania donovani MHOM/IN/00/DEVI after 72 hrs by MTT assay2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Nongenotoxic 3-Nitroimidazo[1,2-
AID548284Selectivity ratio of EC50 for Trypanosoma brucei NfxR2 to EC50 for Trypanosoma brucei2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID1740561Selectivity index, ratio of CC50 for human HepG2 cells to EC50 for Trypanosoma brucei brucei AnTat 1.92020European journal of medicinal chemistry, Sep-15, Volume: 2028-Alkynyl-3-nitroimidazopyridines display potent antitrypanosomal activity against both T. b. brucei and cruzi.
AID1586950Antileishmanial activity against Leishmania infantum axenic amastigotes after 48 hrs by steady-glo luciferase reporter gene assay2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Nongenotoxic 3-Nitroimidazo[1,2-
AID671049Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB9002012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Discovery of nitroheterocycles active against African trypanosomes. In vitro screening and preliminary SAR studies.
AID1406968Selectivity index, ratio of CC50 for human HepG2 cells to IC50 for intramacrophage amastigote stage of Leishmania donovani infected in human THP1 cells2018European journal of medicinal chemistry, Sep-05, Volume: 1578-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases.
AID1548448Selectivity index, ratio of CC50 for human HepG2 cells to EC50 for Trypanosoma brucei brucei trypomastigotes AnTat 1.9
AID1360417Antileishmanial activity against axenic amastigote stage of Leishmania infantum MHOM/MA/67/ITMAP-263 assessed as inhibition of parasite metabolic activity after 48 hrs by luciferase reporter assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study.
AID1742366Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
AID1360420Cytotoxicity against human THP1 cells assessed as decrease in cell viability after 72 hrs by MTT assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study.
AID1742370Selectivity index, ratio of CC50 for human HepG2 cells to EC50 for antileishmanial activity against Leishmania infantum MHOM/MA/67/ITMAP-263 axenic amastigotes
AID1706426Antitrypanosomal activity against bloodstream trypomastigotes form of Trypanosoma cruzi CL Brener infected in BALB/c mouse assessed as reduction in parasitemia at 100 mg/kg, po qd administered for 5 days starting from day 114 post infection followed by cy2020European journal of medicinal chemistry, Dec-01, Volume: 207Re-evaluating pretomanid analogues for Chagas disease: Hit-to-lead studies reveal both in vitro and in vivo trypanocidal efficacy.
AID1406963Antitrypanosomal activity against trypomastigote stage of Trypanosoma brucei brucei AnTat 1.9 assessed as decrease in parasite viability after 69 hrs by Alamar blue assay2018European journal of medicinal chemistry, Sep-05, Volume: 1578-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases.
AID568397Antimicrobial activity against Trypanosoma brucei rhodesiense after 48 hrs by proliferation assay2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Compounds containing 2-substituted imidazole ring for treatment against human African trypanosomiasis.
AID1548466Antitrypanosomal activity against Trypanosoma cruzi CL Brener amastigotes infected in African green monkey Vero cells assessed as reduction in parasite growth incubated for 120 hrs at 24 hrs post-infection and measured on day 6 post-infection by hemocytom
AID548296Fraction unbound in plasma of NMRI mouse at 200 mg/kg, po2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID1742368Selectivity index, ratio of CC50 for human HepG2 cells to EC50 for antileishmanial activity against Leishmania donovani MHOM/IN/00/DEVI promastigotes
AID1548446Antitrypanosomal activity against Trypanosoma brucei brucei AnTat 1.9 trypomastigotes assessed as reduction in parasite viability incubated for 69 hrs by Alamar Blue dye based assay
AID1360418Antitrypanosomal activity against trypomastigote stage of Trypanosoma brucei brucei AnTat 1.9 assessed as decrease in parasite viability after 69 hrs by Alamar Blue assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study.
AID1548445Antileishmanial activity against Leishmania infantum MHOM/MA/67/ITMAP-263 axenic amastigotes expressing luciferase plasmid assessed as reduction in parasite viability incubated for 48 hrs by Steady Glow reagent based luminescence assay
AID548297Antimicrobial activity against fexinidazole-resistant Trypanosoma brucei FxR12010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID548298Antimicrobial activity against fexinidazole-resistant Trypanosoma brucei FxR22010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID548289Antimicrobial activity against Trypanosoma brucei NfxR1 infected in ip dosed NMRI administered QD for 3 days measured on day 6 by neubuaer hemocytometry2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID1586959Cytotoxicity against human THP1 cells after 72 hrs by MTT assay2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Nongenotoxic 3-Nitroimidazo[1,2-
AID1406965Antileishmanial activity against promastigote stage of Leishmania donovani MHOM/IN/00/DEVI assessed as inhibition of parasite metabolic activity after 72 hrs by MTT assay2018European journal of medicinal chemistry, Sep-05, Volume: 1578-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases.
AID1586958Antitrypanosomal activity against Trypanosoma cruzi MHOM/BR/78/Silvio cloneX10/7A epimastigotes measured after 4 days by resazurin dye based fluorescence assay2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Nongenotoxic 3-Nitroimidazo[1,2-
AID671047Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 by Alamar blue growth inhibition assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Discovery of nitroheterocycles active against African trypanosomes. In vitro screening and preliminary SAR studies.
AID568399Aqueous solubility of the compound at pH 1.5 at 25 degC2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Compounds containing 2-substituted imidazole ring for treatment against human African trypanosomiasis.
AID1360421Antileishmanial activity against amastigote stage of Leishmania donovani MHOM/IN/00/DEVI infected in human THP1 cells assessed as inhibition of parasite infection after 120 hrs by Giemsa staining-based microscopic method2018European journal of medicinal chemistry, Jul-15, Volume: 155Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study.
AID1406969Cytotoxicity against human THP1 cells assessed as reduction in cell viability after 72 hrs by MTT assay2018European journal of medicinal chemistry, Sep-05, Volume: 1578-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases.
AID1740557Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 2028-Alkynyl-3-nitroimidazopyridines display potent antitrypanosomal activity against both T. b. brucei and cruzi.
AID1456710Antileishmanial activity against Leishmania donovani LV9 amastigotes infected in BALB/c mouse assessed as reduction in parasite burden at 200 mg/kg, po administered qd for 5 days2017Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
Nitroimidazoles: Molecular Fireworks That Combat a Broad Spectrum of Infectious Diseases.
AID1740560Antileishmanial activity against Trypanosoma brucei brucei AnTat 1.9 measured after 74 hrs by Alamar blue assay2020European journal of medicinal chemistry, Sep-15, Volume: 2028-Alkynyl-3-nitroimidazopyridines display potent antitrypanosomal activity against both T. b. brucei and cruzi.
AID1406966Selectivity index, ratio of CC50 for human HepG2 cells to IC50 for promastigote stage of Leishmania donovani MHOM/IN/00/DEVI2018European journal of medicinal chemistry, Sep-05, Volume: 1578-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases.
AID548291Selectivity ratio of ED50 for antitrypanosomal activity against Trypanosoma brucei NxfR1 infected in NMRI mouse to ED50 for antitrypanosomal activity against Trypanosoma brucei infected in NMRI mouse2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID1742395Electrochemical behavior of the compound assessed as redox potential corrected toward saturated calomel electrode by cyclic voltammetry
AID1406962Selectivity index, ratio of CC50 for human HepG2 cells to IC50 for axenic amastigote stage of Leishmania infantum2018European journal of medicinal chemistry, Sep-05, Volume: 1578-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases.
AID1594633Antitrypanosomal activity against Trypanosoma brucei 427 bloodstream forms assessed as inhibition of parasite growth incubated for 48 hrs by Alamar blue assay2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Synthesis of diphenoxyadamantane alkylamines with pharmacological interest.
AID1742371Antitrypanosomal activity against bloodstream form Trypanosoma brucei brucei AnTat 1.9 trypomastigotes assessed as reduction in parasite viability incubated for 69 hrs by Alamar Blue dye based assay
AID1742372Selectivity index, ratio of CC50 for human HepG2 cells to EC50 for Trypanosoma brucei brucei trypomastigotes AnTat 1.9
AID1586946Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Nongenotoxic 3-Nitroimidazo[1,2-
AID692981Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900 bloodstream forms assessed as reduction in cell viability after 70 hrs by alamar blue assay2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
1-Aryl-4-nitro-1H-imidazoles, a new promising series for the treatment of human African trypanosomiasis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (67)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902 (2.99)18.7374
1990's4 (5.97)18.2507
2000's0 (0.00)29.6817
2010's44 (65.67)24.3611
2020's17 (25.37)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 49.09

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index49.09 (24.57)
Research Supply Index4.28 (2.92)
Research Growth Index6.09 (4.65)
Search Engine Demand Index72.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (49.09)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (5.97%)5.53%
Reviews9 (13.43%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other54 (80.60%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
uracil
2,4-dihydroxypyrimidine: a urinary biomarker for bipolar disorder		1.9910pyrimidine nucleobase;
pyrimidone		allergen;
Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
prodrug;
Saccharomyces cerevisiae metabolite
amodiaquine
Amodiaquine: A 4-aminoquinoline compound with anti-inflammatory properties.. amodiaquine : A quinoline having a chloro group at the 7-position and an aryl amino group at the 4-position.		2.1310aminoquinoline;
organochlorine compound;
phenols;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
drug allergen;
EC 2.1.1.8 (histamine N-methyltransferase) inhibitor;
non-steroidal anti-inflammatory drug;
prodrug
diminazene
Diminazene: An effective trypanocidal agent.. diminazene : A triazene derivative that is triazene in which each of the terminal nitrogens is substituted by a 4-carbamimidoylphenyl group.		1.9610carboxamidine;
triazene derivative		antiparasitic agent;
trypanocidal drug
carbamazepine
Carbamazepine: A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties.. carbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant.		2.1710dibenzoazepine;
ureas		analgesic;
anticonvulsant;
antimanic drug;
drug allergen;
EC 3.5.1.98 (histone deacetylase) inhibitor;
environmental contaminant;
glutamate transporter activator;
mitogen;
non-narcotic analgesic;
sodium channel blocker;
xenobiotic
eflornithine
Eflornithine: An inhibitor of ORNITHINE DECARBOXYLASE, the rate limiting enzyme of the polyamine biosynthetic pathway.. eflornithine : A fluoroamino acid that is ornithine substituted by a difluoromethyl group at position 2.		4.5970alpha-amino acid;
fluoroamino acid		trypanocidal drug
diclofenac
Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.. diclofenac : A monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position.		2.1710amino acid;
aromatic amine;
dichlorobenzene;
monocarboxylic acid;
secondary amino compound		antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
miltefosine
miltefosine: hexadecyl phosphocholine derivative of cisplatin; did not substantially activate HIV long terminal repeat; less toxic than cisplatin. miltefosine : A phospholipid that is the hexadecyl monoester of phosphocholine.		4.6470phosphocholines;
phospholipid		anti-inflammatory agent;
anticoronaviral agent;
antifungal agent;
antineoplastic agent;
antiprotozoal drug;
apoptosis inducer;
immunomodulator;
protein kinase inhibitor
ketoconazole
1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.		1.9710dichlorobenzene;
dioxolane;
ether;
imidazoles;
N-acylpiperazine;
N-arylpiperazine
metronidazole
Metronidazole: A nitroimidazole used to treat AMEBIASIS; VAGINITIS; TRICHOMONAS INFECTIONS; GIARDIASIS; ANAEROBIC BACTERIA; and TREPONEMAL INFECTIONS.. metronidazole : A member of the class of imidazoles substituted at C-1, -2 and -5 with 2-hydroxyethyl, nitro and methyl groups respectively. It has activity against anaerobic bacteria and protozoa, and has a radiosensitising effect on hypoxic tumour cells. It may be given by mouth in tablets, or as the benzoate in an oral suspension. The hydrochloride salt can be used in intravenous infusions. Metronidazole is a prodrug and is selective for anaerobic bacteria due to their ability to intracellularly reduce the nitro group of metronidazole to give nitroso-containing intermediates. These can covalently bind to DNA, disrupting its helical structure, inducing DNA strand breaks and inhibiting bacterial nucleic acid synthesis, ultimately resulting in bacterial cell death.		4.960C-nitro compound;
imidazoles;
primary alcohol		antiamoebic agent;
antibacterial drug;
antimicrobial agent;
antiparasitic agent;
antitrichomonal drug;
environmental contaminant;
prodrug;
radiosensitizing agent;
xenobiotic
oxazepam
Oxazepam: A benzodiazepine used in the treatment of anxiety, alcohol withdrawal, and insomnia.. oxazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a hydroxy group at position 3 and phenyl group at position 5.		2.17101,4-benzodiazepinone;
organochlorine compound		anxiolytic drug;
environmental contaminant;
xenobiotic
pentamidine
Pentamidine: Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.. pentamidine : A diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease.		5.3290aromatic ether;
carboxamidine;
diether		anti-inflammatory agent;
antifungal agent;
calmodulin antagonist;
chemokine receptor 5 antagonist;
EC 2.3.1.48 (histone acetyltransferase) inhibitor;
NMDA receptor antagonist;
S100 calcium-binding protein B inhibitor;
trypanocidal drug;
xenobiotic
propranolol
Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3.		2.5820naphthalenes;
propanolamine;
secondary amine		anti-arrhythmia drug;
antihypertensive agent;
anxiolytic drug;
beta-adrenergic antagonist;
environmental contaminant;
human blood serum metabolite;
vasodilator agent;
xenobiotic
safrole
Safrole: A member of the BENZODIOXOLES that is a constituent of several VOLATILE OILS, notably SASSAFRAS oil. It is a precursor in the synthesis of the insecticide PIPERONYL BUTOXIDE and the drug N-methyl-3,4-methylenedioxyamphetamine (MDMA).. safrole : A member of the class of benzodioxoles that is 1,3-benzodioxole which is substituted by an allyl group at position 5. It is found in several plants, including black pepper, cinnamon and nutmeg, and is present in several essential oils, notably that of sassafras. It has insecticidal properties and has been used as a topical antiseptic. Although not thought to pose a significant carcinogenic risk to humans, findings of weak carcinogenicity in rats have resulted in the banning of its (previously widespread) use in perfumes and soaps, and as a food additive.		2.0610benzodioxolesflavouring agent;
insecticide;
metabolite;
plant metabolite
suramin
Suramin: A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties.. suramin : A member of the class of phenylureas that is urea in which each of the amino groups has been substituted by a 3-({2-methyl-5-[(4,6,8-trisulfo-1-naphthyl)carbamoyl]phenyl}carbamoyl)phenyl group. An activator of both the rabbit skeletal muscle RyR1 and sheep cardiac RyR2 isoform ryanodine receptor channels, it has been used for the treatment of human African trypanosomiasis for over 100 years.		2.6830naphthalenesulfonic acid;
phenylureas;
secondary carboxamide		angiogenesis inhibitor;
antinematodal drug;
antineoplastic agent;
apoptosis inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
GABA antagonist;
GABA-gated chloride channel antagonist;
purinergic receptor P2 antagonist;
ryanodine receptor agonist;
trypanocidal drug
tinidazole
Tinidazole: A nitroimidazole alkylating agent that is used as an antitrichomonal agent against TRICHOMONAS VAGINALIS; ENTAMOEBA HISTOLYTICA; and GIARDIA LAMBLIA infections. It also acts as an antibacterial agent for the treatment of BACTERIAL VAGINOSIS and anaerobic bacterial infections.. tinidazole : 1H-imidazole substituted at C-1 by a (2-ethylsulfonyl)ethyl group, at C-2 by a methyl group and at C-5 by a nitro group. It is used as an antiprotozoal, antibacterial agent.		3.2510imidazolesantiamoebic agent;
antibacterial drug;
antiparasitic agent;
antiprotozoal drug
mitomycin
Mitomycin: An antineoplastic antibiotic produced by Streptomyces caespitosus. It is one of the bi- or tri-functional ALKYLATING AGENTS causing cross-linking of DNA and inhibition of DNA synthesis.. mitomycin : A family of aziridine-containing natural products isolated from Streptomyces caespitosus or Streptomyces lavendulae.		2.0610mitomycinalkylating agent;
antineoplastic agent
4-nitroquinoline-1-oxide
4-nitroquinoline N-oxide : A quinoline N-oxide carrying a nitro substituent at position 4.		2.0610C-nitro compound;
quinoline N-oxide		carcinogenic agent
carbostyril
Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.. quinolin-2(1H)-one : A quinolone that is 1,2-dihydroquinoline substituted by an oxo group at position 2.		2.1710monohydroxyquinoline;
quinolone		bacterial xenobiotic metabolite
nitrobenzene
nitrobenzene : A nitroarene consisting of benzene carrying a single nitro substituent. An industrial chemical used widely in the production of aniline.		2.1710nitroarene;
nitrobenzenes
sulfoxide
sulfoxide: synergistic insecticide for use with pyrethrum, allethrin, rotenone, ryania, etc.; RN given refers to parent cpd; structure. sulfoxide : An organosulfur compound having the structure R2S=O or R2C=S=O (R =/= H).		2.0610benzodioxoles
benzoxazoles
1,3-benzoxazole : A benzoxazole in which the benzene ring is fused to a 1,3-oxazole ring across positions 4 and 5.. benzoxazole : Compounds based on a fused 1,2- or 1,3-oxazole and benzene bicyclic ring skeleton.		3.16101,3-benzoxazoles;
mancude organic heterobicyclic parent
melarsoprol
Melarsoprol: Arsenical used in trypanosomiases. It may cause fatal encephalopathy and other undesirable side effects.		9.4160triazines
podophyllotoxin
Podophyllum: A genus of poisonous American herbs, family BERBERIDACEAE. The roots yield PODOPHYLLOTOXIN and other pharmacologically important agents. The plant was formerly used as a cholagogue and cathartic. It is different from the European mandrake, MANDRAGORA.		2.0710furonaphthodioxole;
lignan;
organic heterotetracyclic compound		antimitotic;
antineoplastic agent;
keratolytic drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator
azomycin
azomycin: RN given refers to parent cpd with specified locant; structure		12.86484C-nitro compound;
imidazoles		antitubercular agent
ferrocin c
N-methyl-2-quinolone: structure in first source		2.1710
vinblastine
[no description available]		2.0610
ethambutol
Ethambutol: An antitubercular agent that inhibits the transfer of mycolic acids into the cell wall of the tubercle bacillus. It may also inhibit the synthesis of spermidine in mycobacteria. The action is usually bactericidal, and the drug can penetrate human cell membranes to exert its lethal effect. (From Smith and Reynard, Textbook of Pharmacology, 1992, p863). ethambutol : An ethylenediamine derivative that is ethane-1,2-diamine in which one hydrogen attached to each of the nitrogens is sutstituted by a 1-hydroxybutan-2-yl group (S,S-configuration). It is a bacteriostatic antimycobacterial drug, effective against Mycobacterium tuberculosis and some other mycobacteria. It is used (as the dihydrochloride salt) in combination with other antituberculous drugs in the treatment of pulmonary and extrapulmonary tuberculosis; resistant strains of M. tuberculosis are readily produced if ethambutol is used alone.		2.2110ethanolamines;
ethylenediamine derivative		antitubercular agent;
environmental contaminant;
xenobiotic
melarsonic acid
melarsonic acid: RN given refers to parent cpd		1.9710
tetradecanoylphorbol acetate
Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.. phorbol ester : Esters of phorbol, originally found in croton oil (from Croton tiglium, of the family Euphorbiaceae). A number of phorbol esters possess activity as tumour promoters and activate the mechanisms associated with cell growth. Some of these are used in experiments as activators of protein kinase C.. phorbol 13-acetate 12-myristate : A phorbol ester that is phorbol in which the hydroxy groups at the cyclopropane ring juction (position 13) and the adjacent carbon (position 12) have been converted into the corresponding acetate and myristate esters. It is a major active constituent of the seed oil of Croton tiglium. It has been used as a tumour promoting agent for skin carcinogenesis in rodents and is associated with increased cell proliferation of malignant cells. However its function is controversial since a decrease in cell proliferation has also been observed in several cancer cell types.		2.1510acetate ester;
diester;
phorbol ester;
tertiary alpha-hydroxy ketone;
tetradecanoate ester		antineoplastic agent;
apoptosis inducer;
carcinogenic agent;
mitogen;
plant metabolite;
protein kinase C agonist;
reactive oxygen species generator
ornidazole
Ornidazole: A nitroimidazole antiprotozoal agent used in ameba and trichomonas infections. It is partially plasma-bound and also has radiation-sensitizing action.. ornidazole : A C-nitro compound that is 5-nitroimidazole in which the hydrogens at positions 1 and 2 are replaced by 3-chloro-2-hydroxypropyl and methyl groups, respectively. It is used in the treatment of susceptible protozoal infections and for the treatment of anaerobic bacterial infections.		3.2510C-nitro compound;
imidazoles;
organochlorine compound;
secondary alcohol		antiamoebic agent;
antibacterial drug;
antiinfective agent;
antiprotozoal drug;
antitrichomonal drug;
epitope
cl 64855
[no description available]		3.830
benzonidazole
benzonidazole: used in treatment of Chagas' disease. benznidazole : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2-nitroimidazol-1-yl)acetic acid with the aromatic amino group of benzylamine. Used for treatment of Chagas disease.		5.92120C-nitro compound;
imidazoles;
monocarboxylic acid amide		antiprotozoal drug
satranidazole
satranidazole: anti-bacterial used to treat periodontitis; structure given in first source		1.9710
sitamaquine
[no description available]		2.1110
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		3.17101,2,3-triazole
artemisinin
(+)-artemisinin : A sesquiterpene lactone obtained from sweet wormwood, Artemisia annua, which is used as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.		2.1310organic peroxide;
sesquiterpene lactone		antimalarial;
plant metabolite
secnidazole
[no description available]		3.2510C-nitro compound;
imidazoles;
secondary alcohol		epitope
atovaquone
Atovaquone: A hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.. atovaquone : A naphthoquinone compound having a 4-(4-chlorophenyl)cyclohexyl group at the 2-position and a hydroxy substituent at the 3-position.		2.5320hydroxy-1,2-naphthoquinone
imidazo(1,2-a)pyridine
imidazo(1,2-a)pyridine: structure		2.0810
tretazicar
tretazicar: minor descriptor (75-84); on-line & Index Medicus search AZIRIDINES (75-84)		2.0510
n',n'-dibenzylbenzohydrazide
[no description available]		2.0710
mk 436
MK 436: structure		2.6830
ro 15-0216
[no description available]		3.110
pa 824
pretomanid: nitroimidazopyran derived from 5-nitroimidazoles; a prodrug that requires activation by a bacterial F420-depedent glucose-6-phosphate dehydrogenase (Fgd) and nitroreductase to activate components that then inhibit bacterial mycolic acid and protein synthesis; structure in first source		2.830
posaconazole
[no description available]		2.2510aromatic ether;
conazole antifungal drug;
N-arylpiperazine;
organofluorine compound;
oxolanes;
triazole antifungal drug;
triazoles		trypanocidal drug
amphotericin b
Amphotericin B: Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela.. amphotericin B : A macrolide antibiotic used to treat potentially life-threatening fungal infections.		4.6270antibiotic antifungal drug;
macrolide antibiotic;
polyene antibiotic		antiamoebic agent;
antiprotozoal drug;
bacterial metabolite
diminazene aceturate
diminazene diaceturate : An N-acetylglycinate salt resulting from the reaction of diminazene with 2 mol eq. of N-acetylglycine.		2.4120N-acetylglycinate saltantiparasitic agent;
trypanocidal drug
antimony
Antimony: A metallic element that has the atomic symbol Sb, atomic number 51, and atomic weight 121.75. It is used as a metal alloy and as medicinal and poisonous salts. It is toxic and an irritant to the skin and the mucous membranes.		2.1510metalloid atom;
pnictogen
arsenic
Arsenic: A shiny gray element with atomic symbol As, atomic number 33, and atomic weight 75. It occurs throughout the universe, mostly in the form of metallic arsenides. Most forms are toxic. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), arsenic and certain arsenic compounds have been listed as known carcinogens. (From Merck Index, 11th ed)		1.9710metalloid atom;
pnictogen		micronutrient
nitrofurazone
Nitrofurazone: A topical anti-infective agent effective against gram-negative and gram-positive bacteria. It is used for superficial WOUNDS AND INJURIES and skin infections. Nitrofurazone has also been administered orally in the treatment of TRYPANOSOMIASIS.. nitrofurazone : A semicarbazone resulting from the formal condensation of semicarbazide with 5-nitrofuraldehyde. A broad spectrum antibacterial drug, although with little activity against Pseudomonas species, it is used as a local application for burns, ulcers, wounds and skin infections.		2.0510
opc-67683
OPC-67683: an antitubercular agent		3.2510piperidines
nifurtimox
Nifurtimox: A nitrofuran thiazine that has been used against TRYPANOSOMIASIS.		8.14161nitrofuran antibiotic
scyx 7158
[no description available]		2.1710(trifluoromethyl)benzenes
warfarin
Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group.		2.1710benzenes;
hydroxycoumarin;
methyl ketone
rifampin
Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)		2.2110cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
African Sleeping Sickness
[description not available]		016.65343
Trypanosomiasis, African
A disease endemic among people and animals in Central Africa. It is caused by various species of trypanosomes, particularly T. gambiense and T. rhodesiense. Its second host is the TSETSE FLY. Involvement of the central nervous system produces African sleeping sickness. Nagana is a rapidly fatal trypanosomiasis of horses and other animals.		113.65343
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		06.64110
Bacterial Disease
[description not available]		03.0610
Infectious Diseases
[description not available]		03.0610
Parasite Infections
[description not available]		03.0610
Bacterial Infections
Infections by bacteria, general or unspecified.		03.0610
Communicable Diseases
An illness caused by an infectious agent or its toxins that occurs through the direct or indirect transmission of the infectious agent or its products from an infected individual or via an animal, vector or the inanimate environment to a susceptible animal or human host.		03.0610
American Trypanosomiasis
[description not available]		08.99201
Chagas Disease
Infection with the protozoan parasite TRYPANOSOMA CRUZI, a form of TRYPANOSOMIASIS endemic in Central and South America. It is named after the Brazilian physician Carlos Chagas, who discovered the parasite. Infection by the parasite (positive serologic result only) is distinguished from the clinical manifestations that develop years later, such as destruction of PARASYMPATHETIC GANGLIA; CHAGAS CARDIOMYOPATHY; and dysfunction of the ESOPHAGUS or COLON.		113.38402
Neutropenia
A decrease in the number of NEUTROPHILS found in the blood.		03.9911
Leishmania Infection
[description not available]		04.2530
Leishmaniasis
A disease caused by any of a number of species of protozoa in the genus LEISHMANIA. There are four major clinical types of this infection: cutaneous (Old and New World) (LEISHMANIASIS, CUTANEOUS), diffuse cutaneous (LEISHMANIASIS, DIFFUSE CUTANEOUS), mucocutaneous (LEISHMANIASIS, MUCOCUTANEOUS), and visceral (LEISHMANIASIS, VISCERAL).		16.2530
Neglected Diseases
Diseases that are underfunded and have low name recognition but are major burdens in less developed countries. The World Health Organization has designated six tropical infectious diseases as being neglected in industrialized countries that are endemic in many developing countries (HELMINTHIASIS; LEPROSY; LYMPHATIC FILARIASIS; ONCHOCERCIASIS; SCHISTOSOMIASIS; and TRACHOMA).		04.1750
Adverse Drug Event
[description not available]		02.2110
Drug-Related Side Effects and Adverse Reactions
Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.		02.2110
Black Fever
[description not available]		02.7730
Leishmaniasis, Visceral
A chronic disease caused by LEISHMANIA DONOVANI and transmitted by the bite of several sandflies of the genera Phlebotomus and Lutzomyia. It is commonly characterized by fever, chills, vomiting, anemia, hepatosplenomegaly, leukopenia, hypergammaglobulinemia, emaciation, and an earth-gray color of the skin. The disease is classified into three main types according to geographic distribution: Indian, Mediterranean (or infantile), and African.		14.7730
Parasitemia
The presence of parasites (especially malarial parasites) in the blood. (Dorland, 27th ed)		03.420
Trypanosomiasis
Infection with protozoa of the genus TRYPANOSOMA.		15.3520
Infections, Plasmodium
[description not available]		02.1310
Malaria
A protozoan disease caused in humans by four species of the PLASMODIUM genus: PLASMODIUM FALCIPARUM; PLASMODIUM VIVAX; PLASMODIUM OVALE; and PLASMODIUM MALARIAE; and transmitted by the bite of an infected female mosquito of the genus ANOPHELES. Malaria is endemic in parts of Asia, Africa, Central and South America, Oceania, and certain Caribbean islands. It is characterized by extreme exhaustion associated with paroxysms of high FEVER; SWEATING; shaking CHILLS; and ANEMIA. Malaria in ANIMALS is caused by other species of plasmodia.		02.1310
Extravascular Hemolysis
[description not available]		02.1310
Hemolysis
The destruction of ERYTHROCYTES by many different causal agents such as antibodies, bacteria, chemicals, temperature, and changes in tonicity.		02.1310
Entamoeba histolytica Infection
[description not available]		02.8810
Histomoniasis
[description not available]		02.8810
Infections, Trichomonas
[description not available]		02.8810
Trichomonas Infections
Infections in birds and mammals produced by various species of Trichomonas.		02.8810
Chronic Illness
[description not available]		01.9610
Chronic Disease
Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).		01.9610
Brain Disorders
[description not available]		01.9710
Brain Diseases
Pathologic conditions affecting the BRAIN, which is composed of the intracranial components of the CENTRAL NERVOUS SYSTEM. This includes (but is not limited to) the CEREBRAL CORTEX; intracranial white matter; BASAL GANGLIA; THALAMUS; HYPOTHALAMUS; BRAIN STEM; and CEREBELLUM.		01.9710