Analogues of 8-[[6-(diethylamino) hexyl]amino]-6-methoxy-4-methylquinoline as candidate antileishmanial agents.
8-[[6-(Diethylamino)hexyl]amino]-6-methoxy-4-methylquinoline (I) has been shown to be highly effective against Leishmania donovani in hamsters, being approximately 475 times as active as the standard meglumine antimoniate. Several nuclear and side-chain analogues of I have been prepared in an attempt to further enhance the antileishmanial activity of this class of compounds. The compounds were tested against L. donovani in the golden hamster. Although several analogues had meglumine antimoniate indexes in excess of 300, none was superior to the model compound.
D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000627:therapeutic use; D006224:Cricetinae; D007898:Leishmaniasis, Visceral / Q000188:drug therapy*; D008647:Mesocricetus; D013329:Structure-Activity Relationship
D000634:Aminoquinolines; D000981:Antiprotozoal Agents; C080436:8-aminoquinoline