Search results for "NRTI"

A Multivariate Analysis on Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors and Resistance Induced by Mutation

2003

This paper describes the use of multivariate statistical procedure PCA as a tool to explore the inhibitory activity of classes of NNRTIs against HIV-1 viruses (wild type and more frequent mutants, Y181C, V106A, K103N, L100I) and against RT enzyme. The analysis of correlations between biological activity and molecular descriptors or similarity indexes allowed a reliable classification of the fifty five derivatives considered in this study. The best results were obtained in the case of L100I and K103N mutants for which the higher number of assignments was found when the principal components derived from the descriptors were used. On this basis this statistical approach is proposed as a reliab…

2-(2,6-Dihalophenyl)-3-(pyrimidin-2-yl)-1,3-thiazolidin-4-ones as non-nucleoside HIV-1 reverse transcriptase inhibitors.

2004

Several 1,3-thiazolidin-4-ones bearing a 2,6-dihalophenyl group at C-2 and a substituted pyrimidin-2-yl ring at the N-3 were synthesised and evaluated as anti-HIV agents. The results of the in vitro tests showed that some of them were highly effective inhibitors of human immunodeficiency virus type-1 (HIV-1) replication at 10–40 nM concentrations with minimal cytotoxicity. Structure–activity relationship studies revealed that the nature of the substituents at the 2 and 3 positions of the thiazolidinone nucleus had a significant impact on the in vitro anti-HIV activity of this class of potent antiretroviral agents. The compounds had significantly reduced activity against the characteristic N…

Synthesis of Azole-Heterocycles as Potential Antitumor and/or Antiviral Agents

2014

Efectos proinflamatorios de los fármacos antirretrovirales inhibidores de la transcriptasa inversa análogos de nucleósido in vitro e in vivo

2013

Los inhibidores de la transcriptasa inversa análogos de nucleós(t)ido (ITIAN) son una familia de fármacos empleados en el tratamiento de la infección por el virus de la inmunodeficiencia humana (VIH). Este grupo de antirretrovirales está presente en todas las opciones terapéuticas en combinación con fármacos antirretrovirales de otras familias. La administración de estos compuestos, en particular de abacavir (ABC) y didanosina (ddI), se ha asociado con la aparición de efectos adversos a nivel cardiovascular; sin embargo los mecanismos responsables permanecen sin esclarecer. Empleando modelos in vitro e in vivo, hemos evaluado los efectos de concentraciones clínicamente relevantes de estos a…