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.
Subject(s)
Anti-HIV Agents/chemical synthesis , HIV Reverse Transcriptase/antagonists & inhibitors , Quinolines/chemical synthesis , Quinoxalines/chemical synthesis , Reverse Transcriptase Inhibitors/chemical synthesis , Anti-HIV Agents/pharmacology , Cell Line , Humans , Quinolines/pharmacology , Quinoxalines/pharmacology , Reverse Transcriptase Inhibitors/pharmacology , Structure-Activity RelationshipABSTRACT
The Developmental Eye Movement (DEM) test is a clinical oculomotor test of a visual-verbal format which has been normalized and whose reliability and validity have been shown elsewhere in an English speaking population. In this paper, the authors provide normative data for a Spanish speaking population from ages 6 to 11 years. Also, a comparison of results for both languages is provided. The DEM test appears to be highly efficient and not linguistically related for all subjects involved in the study. Results in that age bracket are clinically the same. For age 6 years, although results are not similar (Spanish subjects are significantly slower), the ratio is similar in both groups. The DEM test appears to be reliable; its results could be used in any population regardless of the language.
