Submit Manuscript  

Article Details


Anti HIV-1 Agents 6. Synthesis and Anti-HIV-1 Activity of Indolyl Glyoxamides

[ Vol. 8 , Issue. 5 ]

Author(s):

Yi Wang, Ning Huang, Xiang Yu, Liu-Meng Yang, Xiao-Yan Zhi, Yong-Tang Zheng and Hui Xu   Pages 831 - 833 ( 3 )

Abstract:


In order to discover compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, 9 new indolyl glyoxamide derivatives (3a-i) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro. Among all the derivatives, especially compounds 3e and 3h showed the potent anti-HIV-1 activity with EC50 values of 6.83 and 4.35 μg/mL, and TI values of >27.15 and 49.45, respectively. It demonstrated that introduction of the substituent R3 as the halogen atom and the position of R3 were generally important to their activity.

Keywords:

Indolyl glyoxamide, Acquired immunodeficiency syndrome, Human immunodeficiency virus-1, Inhibitor, antifungal, atom, HIV, AIDS, oxalyl chloride, NMR

Affiliation:

Laboratory of Pharmaceutical Design & Synthesis, College of Sciences, Northwest A&F University, Yangling 712100, China.



Read Full-Text article