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 Citas (Scopus)

Resumen

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.

Idioma originalInglés
Páginas (desde-hasta)963-971
Número de páginas9
PublicaciónEuropean Journal of Medicinal Chemistry
Volumen30
N.º12
DOI
EstadoPublicada - 1995
Publicado de forma externa

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