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- ISSN: 1573-4064
- E-ISSN: 1875-6638
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Anti HIV-1 Agents 6. Synthesis and Anti-HIV-1 Activity of Indolyl Glyoxamides
- Source: Medicinal Chemistry, Volume 8, Issue 5, Sep 2012, p. 831 - 833
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- 01 Sep 2012
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.
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