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

作者：Ashok Penta; Chander Subhash; Balzarini Jan; Pannecouque Christophe; Murugesan Sankaranarayanan^*

来源：Bioorganic & Medicinal Chemistry Letters, 2015, 25(6): 1232-1235.

DOI：10.1016/j.bmcl.2015.01.058

• beta-Carboline
• HIV-1
• HIV-2
• Reverse transcriptase

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.

• 出版日期2015-3-15
• 单位河北医科大学