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, β‐{[N‐methyl‐4‐[N‐methyl‐4‐(guanidinoacetamido)pyrrole ‐2‐carboxa‐mido]pyrrole‐2‐carboxamido]pyrrole‐2‐carboxamidoibutyroamidine 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.
| Original language | English |
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| Pages (from-to) | 822-824 |
| Number of pages | 3 |
| Journal | Journal of Pharmaceutical Sciences |
| Volume | 70 |
| Issue number | 7 |
| DOIs |
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| State | Published - Jul 1981 |
Keywords
- Antiparasitic activity—tripyrrole derivatives of congocidine synthesized and evaluated for activity in mice, in vitro and in vivo studies
- Congocidine derivatives—tri‐ and monopyrrole analogs, synthesized and evaluated for antiparasitic activity in mice, in vivo and in vitro studies
- Structure‐activity relationships—tripyrrole derivatives of congocidine synthesized and evaluated for antiparasitic activity in mice, in vivo and in vitro studies