Anti Human Immunodeficiency Virus-1 (HIV-1) Agents 3. Synthesis and in Vitro Anti-HIV-1 Activity of Some N-Arylsulfonylindoles

摘要

In order to find compounds with superior anti human immunodeficiency virus type 1 (HIV-1) activity, twelve simple N-arylsulfonylindoles (3a-1) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro for the first time. Several compounds demonstrated significant anti-HIV-1 activity, especially N-(3-ni_trobenzene)sulfonyl-6-methylindole (3h) and N-(3-nitrobenzene)sulfonylindole (3i) showed the highest anti-HIV-1 activity with EC_(50) values of 0.26 and 0.74 _g/ml, and TI values of 543.78 and >270.27, respectively.