摘要
Keeping in view the recent success of molecular hybridization technique in drug design, 2,4-diarylpyrano[3,2-c]chromen-5(4H)-ones as conjugates of coumarins and chalcones have been designed and synthesized in the present study. The catalytic efficiency of various Lewis acids for the synthesis of designed conjugates under neat conditions was investigated, and SiO2 (200-400 mesh)-ZnCl2 was optimized as the best catalyst among the tested ones. The conjugates were evaluated for in-vitro xanthine oxidase activity. The results of the in-vitro assay were quite promising as some conjugates were endowed with remarkable inhibitory potential against the enzyme. HV-8, 11 and 12 were found to be high-potent inhibitors with HV-11 (the most potent inhibitor) possessing an IC50 value of 2.21 μM. The most active conjugate HV-11 was evaluated for the type of inhibition and was found to be a mixed type inhibitor. The compliance of some selected conjugates to the Lipinski rule was also calculated.
原文 | 英語 |
---|---|
頁(從 - 到) | 730-736 |
頁數 | 7 |
期刊 | Journal of Enzyme Inhibition and Medicinal Chemistry |
卷 | 30 |
發行號 | 5 |
DOIs | |
出版狀態 | 已發佈 - 9月 3 2015 |
對外發佈 | 是 |
ASJC Scopus subject areas
- 藥理
- 藥物發現
指紋
深入研究「Design, synthesis and evaluation of 2,4-diarylpyrano[3,2-c]chromen-5(4H)-one as a new class of non-purine xanthine oxidase inhibitors」主題。共同形成了獨特的指紋。資料集
-
Design, synthesis and evaluation of 2,4-diarylpyrano[3,2-c]chromen-5(4H)-one as a new class of non-purine xanthine oxidase inhibitors
Virdi, H. S. (Creator), Sharma, S. (Contributor), Mehndiratta, S. (Creator), Bedi, P. M. S. (Contributor) & Nepali, K. (Contributor), Figshare, 2015
DOI: 10.6084/m9.figshare.1568378.v1, https://figshare.com/articles/Design_synthesis_and_evaluation_of_2_4_diarylpyrano_3_2_c_chromen_5_4H_one_as_a_new_class_of_non_purine_xanthine_oxidase_inhibitors/1568378/1
資料集: Dataset