Indoles and pyridazino[4,5-b]indoles as nonnucleoside analog inhibitors of HIV-1 reverse transcriptase

M. Font, A. Monge, A. Cuartero, A. Elorriaga, J. J. Martínez-Irujo, E. Alberdi, E. Santiago, I. Prieto, J. J. Lasarte, P. Sarobe, F. Borrás

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31 Citations (Scopus)

Abstract

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, Y 181C and P236L/Y181C) was evaluated. The activity of the most active compounds was investigated in the syncytia reduction in vitro assay, in HIV-1IIIB-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.

Original languageEnglish
Pages (from-to)963-971
Number of pages9
JournalEuropean Journal of Medicinal Chemistry
Volume30
Issue number12
DOIs
Publication statusPublished - 1995
Externally publishedYes

Keywords

  • indole
  • nonnucleoside RT inhibitor
  • syncytia assay/HIV-1 HT4lacZ-1 cells

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