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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