Synthesis and evaluation of new Reissert analogs as HIV-1 reverse transcriptase inhibitors. 1. Quinoline and quinoxaline derivatives
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
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.

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