Synthesis and antiparasitic and antifungal evaluation of 2'-arylsubstituted-1H,1'H-[2,5']bisbenzimidazolyl-5-carboxamidines.
A series of 2'-arylsubstituted-1H,1'H-[2,5']-bisbenzimidazolyl-5-carboxamidines were prepared in a six-step process starting from 4-amino-3-nitrobenzonitrile. The antiparasitic activity against Trypanosoma brucei rhodesiense (T.b.r.), Plasmodium falciparum (P.f.), Leishmania donovani (L.d.) and Trypanosoma cruzi (T.c.) and antifungal activity against Candida albicans and Candida krusei were evaluated in vitro. Several compounds showed promising in vitro activity against T.b.r., P.f. and C. albicans and had superior activity against P.f. as compared to chloroquine.
Alp
Mehmet
M
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06100 Tandogan, Ankara, Turkey.
Göker
Hakan
H
Brun
Reto
R
Yildiz
Sulhiye
S
D000578:Amidines / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000977:Antiparasitic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D007893:Leishmania donovani / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship; D014346:Trypanosoma brucei brucei / Q000187:drug effects; D014349:Trypanosoma cruzi / Q000187:drug effects
D000578:Amidines; D000935:Antifungal Agents; D000977:Antiparasitic Agents