Anti HIV-1 agents 6. Synthesis and anti-HIV-1 activity of indolyl glyoxamides

摘要

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.