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Synthesis and evaluation of new Reissert analogs as HIV-1 reverse transcriptase inhibitors. 1. Quinoline and quinoxaline derivatives
Authors: Font, M. (María)
Monge, A. (Antonio)
Alvarez, E. (E)
Cuartero, A. (A)
Losa, M.J. (MJ)
Fidalgo, M.J. (MJ)
Sanmartin-Grijalba, C. (Carmen)
Nadal, E. (Ernest)
Ruiz, I. (I)
Merino, I. (Isidro)
Martinez-Irujo, J.J. (Juan José)
Alberdi, E. (Elena)
Santiago, E. (Esteban)
Prieto, I. (Inés)
Lasarte, J.J. (Juan José)
Sarobe, P. (Pablo)
Borras-Cuesta, F. (Francisco)
Keywords: Anti-HIV Agents/chemical synthesis
HIV Reverse Transcriptase/antagonists & inhibitors
Quinolines/chemical synthesis
Quinoxalines/chemical synthesis
Reverse Transcriptase Inhibitors/chemical synthesis
Issue Date: 1997
Publisher: Gordon and Breach
Publisher version: http://cat.inist.fr/?aModele=afficheN&cpsidt=2673751
ISSN: 1029-2322
Citation: Font 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.
Abstract
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.
Permanent link: http://hdl.handle.net/10171/21594
Appears in Collections:DA - Medicina - Medicina Interna - Artículos de revista
DA - CIMA - Terapia génica y Hepatología - Inmunología hepatitis virales - Artículos de revista
DA - CIMA - Terapia génica y Hepatología - Inmunología experimental - Artículos de revista

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