title: Antiparasitic structure-activity relationships of congocidine derivatives.
abstract: Several congocidine analogs were synthesized and tested for in vivo activity against Trypanosoma congolense and in vitro activity against amastigotes of Leishmania tropica. The tripyrrole derivative, beta-([N-methyl-4-[N-methyl-4-(guanidinoacetamido)pyrrole-2-carboxamido]pyrrole -2-carboxamido]pyrrole-2-carboxamido)butyroamidine dihydrochloride, was less toxic and more active than congocidine. The guanidinoacetyl moiety appears to be a structural requirement for antiparasitic activity in the congocidine series.
mesh_terms: D000818:Animals; D000977:Antiparasitic Agents; D000981:Antiprotozoal Agents; D006146:Guanidines / Q000494:pharmacology*; D007896:Leishmaniasis / Q000188:drug therapy; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D009429:Netropsin; D011758:Pyrroles / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013997:Time Factors; D014344:Trypanocidal Agents
chemical_list: D000977:Antiparasitic Agents; D000981:Antiprotozoal Agents; D006146:Guanidines; D011758:Pyrroles; D014344:Trypanocidal Agents; D009429:Netropsin