Evaluation of in-vitro leishmanicidal activity of hydrazones of thiophene carboxaldehydes against promastigotes of Leishmania infantum and Leishmania tropica.
The lack of leishmanicidal drugs has prompted the synthesis and testing of new hydrazones of thiophene carboxaldehydes against three Leishmania strains. The compounds were obtained by condensation of appropriate hydrazines with thiophene 2-carboxaldehyde (series 1), thiophene 3-carboxaldehyde (series 2), and 5-nitrothiophene-2-carboxaldehyde (series 3). Leishmanicidal activity was assessed against promastigotes of Leishmania strains, grown in-vitro in nutrient broth medium complemented with fresh rabbit blood. The minimal inhibitory concentrations were evaluated against pentamidine, as a reference drug. Several compounds exhibited significant leishmanicidal activity, the best being ten times more active than pentamidine.
Laboratory of Parasitology, Faculté de Pharmacie, Marseille, France.
B
B
Savornin
N E
NE
Madadi
F
F
Delmas
M
M
Gasquet
P
P
Timon-David
P
P
Vanelle
J
J
Maldonado
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D006835:Hydrazones / Q000138:chemical synthesis / Q000494:pharmacology*; D007893:Leishmania donovani / Q000187:drug effects*; D007895:Leishmania tropica / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D010419:Pentamidine / Q000494:pharmacology; D011817:Rabbits; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis / Q000494:pharmacology
D000981:Antiprotozoal Agents; D006835:Hydrazones; D013876:Thiophenes; D010419:Pentamidine