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Antileishmanial assessment of isoxazole derivatives against L. donovani
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2020-07-20 , DOI: 10.1039/d0md00083c Sushobhan Mukhopadhyay 1 , Dinesh S Barak 1 , R Karthik 2 , Sarvesh K Verma 3 , Rabi S Bhatta 3, 4 , Neena Goyal 2, 4 , Sanjay Batra 1, 4
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2020-07-20 , DOI: 10.1039/d0md00083c Sushobhan Mukhopadhyay 1 , Dinesh S Barak 1 , R Karthik 2 , Sarvesh K Verma 3 , Rabi S Bhatta 3, 4 , Neena Goyal 2, 4 , Sanjay Batra 1, 4
Affiliation
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A chemical library comprising substituted 3-nitroisoxazoles and 3-aminoisoxazoles was prepared and screened for their antileishmanial activity against L. donovani. 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 in vivo evaluation of a few compounds in a golden hamster model showed significant reduction of the parasite load post treatment via the intraperitoneal route by several compounds. The preliminary pharmacokinetic evaluation of a representative compound 4mfvia the oral route, however, indicated high systemic clearance from the body.
中文翻译：
异恶唑衍生物对 L. donovani 的 Antileishmanial 评估
制备了包含取代的 3-硝基异恶唑和 3-氨基异恶唑的化学文库，并筛选了它们对L. donovani的杀虫活性。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。金仓鼠模型中几种化合物的体内评估表明，几种化合物通过腹膜内途径治疗后的寄生虫负荷显着降低。然而，通过口服途径对代表性化合物4mf进行的初步药代动力学评估表明，其体内的全身清除率很高。
更新日期：2020-09-23
中文翻译：
异恶唑衍生物对 L. donovani 的 Antileishmanial 评估
制备了包含取代的 3-硝基异恶唑和 3-氨基异恶唑的化学文库，并筛选了它们对L. donovani的杀虫活性。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。金仓鼠模型中几种化合物的体内评估表明，几种化合物通过腹膜内途径治疗后的寄生虫负荷显着降低。然而，通过口服途径对代表性化合物4mf进行的初步药代动力学评估表明，其体内的全身清除率很高。
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