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dc.creatorFont, M. (María)-
dc.creatorMonge, A. (Antonio)-
dc.creatorAlvarez, E. (E)-
dc.creatorCuartero, A. (A)-
dc.creatorLosa, M.J. (M.J.)-
dc.creatorFidalgo, M.J. (M. J.)-
dc.creatorSanmartin-Grijalba, C. (Carmen)-
dc.creatorNadal, E. (Ernest)-
dc.creatorRuiz, I. (I)-
dc.creatorMerino, I. (Isidro)-
dc.creatorMartinez-Irujo, J.J. (Juan José)-
dc.creatorAlberdi, E. (Elena)-
dc.creatorSantiago, E. (Esteban)-
dc.creatorPrieto, I. (Inés)-
dc.creatorLasarte, J.J. (Juan José)-
dc.creatorSarobe, P. (Pablo)-
dc.creatorBorras-Cuesta, F. (Francisco)-
dc.identifier.citationFont M, Monge A, Alvarez E, Cuartero A, Losa MJ, Fidalgo MJ, et al. Synthesis and evaluation of new Reissert analogs as HIV-1 reverse transcriptase inhibitors. 1. Quinoline and quinoxaline derivatives. Drug Des Discov 1997 Apr;14(4):305-332.es_ES
dc.description.abstractThe 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.es_ES
dc.publisherGordon and Breaches_ES
dc.subjectAnti-HIV Agents/chemical synthesises_ES
dc.subjectHIV Reverse Transcriptase/antagonists & inhibitorses_ES
dc.subjectQuinolines/chemical synthesises_ES
dc.subjectQuinoxalines/chemical synthesises_ES
dc.subjectReverse Transcriptase Inhibitors/chemical synthesises_ES
dc.titleSynthesis and evaluation of new Reissert analogs as HIV-1 reverse transcriptase inhibitors. 1. Quinoline and quinoxaline derivativeses_ES

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