作者:Esteban Vargas、Fernando Echeverri、Yulieth Upegui、Sara Robledo、Wiston Quiñones
DOI:10.3390/molecules23010070
日期:——
acyl hydrazone derivatives of thiochroman-4-ones. Compounds were evaluated for their in vitro antileishmanial activity against the intracellular amastigote form of Leishmania panamensis and cytotoxic activity against human monocytes (U-937 ATCC CRL-1593.2). Our results show that derivatization of the thiochroman-4-ones with acyl hydrazones significantly enhances the antileishmanial activity. Among the
皮肤利什曼病(CL)是一种被忽视的热带病,可导致严重的皮肤损伤。由于缺乏有效的疫苗,并且除了复杂和长期的治疗外,还有可用药物的毒性或有效性降低,迫切需要开发具有不同作用机制的替代疗法来治疗CL。为了寻找对付利什曼原虫寄生虫的新方法,我们准备了18种thiochroman-4-ones酰基derivatives衍生物。评估了化合物对潘氏利什曼原虫(Leishmania panamensis)的胞内鞭毛体形式的体外抗螨虫活性和对人单核细胞的细胞毒性活性(U-937 ATCC CRL-1593.2)。我们的结果表明,使用硫代苯并二氢吡喃并用酰基进行衍生化可显着增强抗菌活性。