Savornin B, Madadi N E, Delmas F, Gasquet M, Timon-David P, Vanelle P, Maldonado J
Laboratory of Parasitology, Faculté de Pharmacie, Marseille, France.
J Pharm Pharmacol. 1991 Jan;43(1):58-9. doi: 10.1111/j.2042-7158.1991.tb05452.x.
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.
抗利什曼原虫药物的匮乏促使人们合成并测试新型噻吩甲醛腙对三种利什曼原虫菌株的效果。这些化合物是通过适当的肼与噻吩 -2-甲醛（系列1）、噻吩 -3-甲醛（系列2）和5-硝基噻吩 -2-甲醛（系列3）缩合得到的。针对在补充了新鲜兔血的营养肉汤培养基中体外培养的利什曼原虫菌株的前鞭毛体评估了抗利什曼原虫活性。以喷他脒作为参考药物评估了最小抑菌浓度。几种化合物表现出显著的抗利什曼原虫活性，其中效果最佳的比喷他脒活性高十倍。
