Effect of new diamidines against Leishmania donovani infection.
The impact of interamidine distance on antileishmanial activity of new aryldiamidines have been evaluated against amastigotes of L. donovani in hamster. Of the 20 compounds tested, only four (2,8-diamidino-9,10-dihydrodibenzoxepin; 2,7-diamidinoxanthone; 2,7-diamidinothioxanthone and 2,7-diamidinoxanthene) showed significant inhibition (more than 80%) of multiplication of amastigotes in spleen. The interamidine distance in the structure appears to have bearing on antileishmanial activity. The observations made are likely to evoke new understanding on the structure activity relationship of diarylamidines.
Chauhan
P M
PM
Medicinal Chemistry Division, Central Drug Research Institute, Lucknow, India.
Iyer
R N
RN
Shankhdhar
V
V
Guru
P Y
PY
Sen
A B
AB
D000578:Amidines / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000494:pharmacology*; D006224:Cricetinae; D004353:Drug Evaluation, Preclinical; D007898:Leishmaniasis, Visceral / Q000188:drug therapy*; D008297:Male; D008647:Mesocricetus; D013329:Structure-Activity Relationship
D000578:Amidines; D000981:Antiprotozoal Agents