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

Author(s): Yi Wang, Ning Huang, Xiang Yu, Liu-Meng Yang, Xiao-Yan Zhi, Yong-Tang Zheng, Hui Xu.

Journal Name: Medicinal Chemistry

Volume 8 , Issue 5 , 2012

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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

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Article Details

Year: 2012
Page: [831 - 833]
Pages: 3
DOI: 10.2174/157340612802084270
Price: $58

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