Merino, I. (Isidro)

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1997 - 19992

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    Synthesis and evaluation of new Reissert analogs as HIV-1 reverse transcriptase inhibitors. 1. Quinoline and quinoxaline derivatives
    (Gordon and Breach, 1997) Merino, I. (Isidro); Cuartero, A. (A); Alberdi, E. (Elena); Borras-Cuesta, F. (Francisco); Fidalgo, M.J. (M. J.); Alvarez, E. (E.); Sanmartin-Grijalba, C. (Carmen); Nadal, E. (Ernest); Font, M. (María); Prieto, I. (Inés); Losa, M.J. (M.J.); Monge, A. (Antonio); Martinez-Irujo, J.J. (Juan José); Sarobe, P. (Pablo); Santiago, E. (Esteban); Ruiz, I. (I); Lasarte, J.J. (Juan José)
    The synthesis and preliminary evaluation of new quinoline and quinoxaline derivatives (obtained by applying the original Reissert method, conveniently modified) as HIV-1 Reverse Transcriptase (RT) inhibitors are presented in this paper; likewise, the first structure-activity relationships are also proposed. Propyl 2-cyano-1(2H)-quinolin-carboxylate 2e, isopropyl 2-cyano-1 (2H)-quinolincarboxylate 2f, butyl 2-cyano-1 (2H)-quinolincarboxylate 2g and isobutyl 2-cyano-1 (2H)-quinolincarboxylate 2h have been selected as lead compounds. These compounds are active against the HIV-1 RT mutant type P236L (2f, IC50 = 1.2 microM) and present activity as anti-infective agents in HLT41acZ-1IIIB cells, showing no cytotoxicity at the active concentrations.
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    Synthesis and anti-HIV-1 activities of new pyrimido[5,4-b]indoles
    (Elsevier, 1999) Merino, I. (Isidro); Alberdi, E. (Elena); Borras-Cuesta, F. (Francisco); Font, M. (María); Monge, A. (Antonio); Prieto, I. (Isidro); Sarobe, P. (Pablo); Santiago, E. (Esteban); Martinez-de-Irujo, J.J. (Juan José); Lasarte, J.J. (Juan José)
    A set of new pyrimido[5,4-b]indole derivatives that are structurally related to some non-nucleside HIV-1 reverse transcriptase inhibitors were synthesized and biologically evaluated for their activity as inhibitors of wild and mutant HIV-1 RT types in an 'in vitro' recombinant HIV-1 RT screening assay, as well as anti-infectives in HLT4lacZ-1IIIB cells. Preliminary structure-activity relationships suggest that activity is promoted by simultaneous substitution in positions 2 and 4, especially when chains of alkyldiamine type are present, and by electron-releasing substituents (methoxy) in positions 7 and 8. The inactivity or the very low activity of title derivatives does not suggest interest in AIDS therapy.