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

[ Vol. 8 , Issue. 5 ]


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


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.


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


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

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