Synthesis and molecular docking studies of 1-phenyl-4-glycosyl-dihydropyridines as potent antileishmanial agents
详细信息 查看全文
- 作者：Vivek Parashar P ; ey ; Surendra Singh Bisht ; Mridul Mishra ; Ashutosh Kumar ; Mohammad Imran Siddiqi ; Aditya Verma ; Monika Mittal ; Shraddha A. Sane ; Suman Gupta ; Rama P. Tripathi
- 关键词：Leishmaniasis ; Luciferase assay ; Dihydropyridines ; 1-Phenyl-4-glycosyl-dihydropyridines ; Tetrabutylammonium hydrogensulphate
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2010
- 出版时间：June 2010
- 年：2010
- 卷：45
- 期：6
- 页码：2381-2388
- 全文大小：481 K
文摘
A series of 1-phenyl-4-glycosyl-dihydropyridines (4–17 and 19–21) were prepared by the one pot multicomponent reaction of glcosyl aldehyde, β-keto compounds and aniline or substituted aniline in the presence of TBAHS as catalyst. The compounds were screened in vitro and in vivo for their antileishmanial activities. Most of the compounds exhibited moderate to good activity against amastigotes and promastigotes of Leishmania donovani. The compounds 4, 11, 12, 13, and 17 exhibited potent in vivo activity with selectivity index (SI) values 7.43–18.93. Molecular docking studies with these compounds revealed L. donovani PTR1 as the possible target to show antileishmanial activities.