Indoles and pyridazinoindoles as nonnucleoside analog inhibitors of HIV-1 reverse transcriptase

Article abstract of DOI:10.1016/0223-5234(96)88316-4

The synthesis and the study of the activity of new indol-2-carboxamides and pyridazino<4,5-b>indoles as inhibitors of HIV-1 reverse transcriptase (RT) are presented.The activity of the compounds synthesized as inhibitors of different types of HIV-1 RT (wild type enzyme and mutant forms P236L, Y181C and P236L/Y181C) was evaluated.The activity of the most active compounds was investigated in the syncytia reduction in vitro assay, in HIV-1_IIIB-infected HT4lacZ-1 cells.Their potential cytotoxicity was determined in parallel.Two lead compounds,N-<1-<2-(3-isopropylamino)pyridyl>piperazin>-5,6-methylenedioxy indol-2-carboxamide 7q and N-<1-<2-(3-ethylamino)pyridyl>piperazin>-5,6-methylenedioxyindol-2-carboxamide 7s have been identified. - Keywords: indole; nonnucleoside RT inhibitor; syncytia assay; HIV-1_IIIBHT4lacZ-1 cells