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Anti HIV-1 agents 6. Synthesis and anti-HIV-1 activity of indolyl glyoxamides.
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 EC(50) 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 R(3) as the halogen atom and the position of R(3) were generally important to their activity.
HIV Protease Inhibitors
Inhibitory Concentration 50
Magnetic Resonance Spectroscopy
Pub Type(s)Journal Article
Research Support, Non-U.S. Gov't