Design, synthesis of new β-carboline derivatives and their selective anti-HIV-2 activity

In the present study, a new series of beta-carboline derivatives were synthesized and evaluated for inhibition activity against both HIV-1 and HIV-2 strains. Among these reported analogues, surprisingly (1-phenyl-9H-pyrido[3,4-b] indol-3-yl)(4-p-tolylpiperazin-1-yl) methanone (7b), (4-(2-methoxyphenyl) piperazin-1-yl)(1-phenyl-9H-pyrido[3,4-b] indol-3-yl) methanone (7f), (4-(4-fluorophenyl) piperazin-1-yl) (1-phenyl-9H-pyrido[3,4-b] indol-3-yl) methanone (7k), (4-(2-fluorophenyl) piperazin-1-yl)(1-phenyl-9H-pyrido[3,4-b] indol-3-yl) methanone (7l) displayed selective inhibition of HIV-2 strain with EC50 values of 3.3, 3.2, 2.6 and 5.4 mu M, respectively, which are comparable with nucleoside reverse transcriptase inhibitors lamivudine and dideoxyinosine. As these analogues have not shown in vitro HIV-2 reverse transcriptase inhibition, it could be excluded as potential target for their specific anti-HIV-2 activity. (C) 2015 Elsevier Ltd. All rights reserved.