异恶唑衍生物对利什曼原虫的抗利什曼原虫评估 。 你提供的原文似乎不完整，“against”后面缺少具体内容。
Antileishmanial assessment of isoxazole derivatives against .
作者信息
Mukhopadhyay Sushobhan, Barak Dinesh S, Karthik R, Verma Sarvesh K, Bhatta Rabi S, Goyal Neena, Batra Sanjay
机构信息
Medicinal and Process Chemistry Division , CSIR-Central Drug Research Institute , Sector 10, Jankipuram Extension, Sitapur Road , Lucknow 226031 , India . Email:
Biochemistry Division , CSIR-Central Drug Research Institute , Sector 10, Jankipuram Extension, Sitapur Road , Lucknow 226031 , India . Email:
出版信息
RSC Med Chem. 2020 Jul 20;11(9):1053-1062. doi: 10.1039/d0md00083c. eCollection 2020 Sep 1.
A chemical library comprising substituted 3-nitroisoxazoles and 3-aminoisoxazoles was prepared and screened for their antileishmanial activity against . As compared to Miltefosine, the standard drug used in bioassays, several compounds displayed remarkably better inhibition of the promastigote and amastigote stages of parasites. The evaluation of a few compounds in a golden hamster model showed significant reduction of the parasite load post treatment the intraperitoneal route by several compounds. The preliminary pharmacokinetic evaluation of a representative compound the oral route, however, indicated high systemic clearance from the body.
制备了一个包含取代的3-硝基异恶唑和3-氨基异恶唑的化学文库，并对其针对……的抗利什曼原虫活性进行了筛选。与生物测定中使用的标准药物米替福新相比，几种化合物对寄生虫的前鞭毛体和无鞭毛体阶段表现出明显更好的抑制作用。在金黄仓鼠模型中对几种化合物的评估表明，通过腹腔注射途径给药后，几种化合物显著降低了寄生虫载量。然而，对一种代表性化合物经口服途径的初步药代动力学评估表明，该化合物从体内的全身清除率很高。
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