1,2,4-Triazole Derivatives Inhibiting the Human Immunodeficiency Virus Type 1 (HIV-1) in vitro

Irene M. Lagoja; Christophe Pannecouque; Laura Musumeci; Matheus Froeyen; Arthur Van Aerschot; Jan Balzarini; Piet Herdewijn; De Clercq Erik

doi:10.1002/1522-2675(200207)85:7<1883::aid-hlca1883>3.0.co;2-r

Abstract

1 min read

A novel series of selective 1,2,4-triazole nonnucleoside reverse transcriptase inhibitors (NNRTIs) is described. In MT-4 cells compound, 4f inhibited human immunodeficiency virus type 1 (HIV-1) induced cytopathology at an IC50 of 9.98 μM with a selectivity index of 18.6. The hypothetical docking model of RT/4f derived from X-ray crystallographic structure of capravirine complex with HIV-1 RT links the activity profile to the H-bonding network.

Discussion(0)

No comments yet. Be the first to comment.

Related publications

Article2012

Synthesis and Anti-HIV Evaluation of Novel 1,2,4-triazole Derivatives as Potential Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors

Zhenyu Li, Yuan Cao, Peng Zhan, Christophe Pannecouque, Jan Balzarini, De Clercq Erik, Xinyong Liu

Article2007

Synthesis of Novel Derivatives of 4-Amino-3-(2-Furyl)-5-Mercapto-1,2,4-Triazole as Potential HIV-1 NNRTIs

Jingde Wu, Xinyong Liu, Xian‐Chao Cheng, Yuan Cao, Defeng Wang, Zhong Li, Wenfang Xu, Christophe Pannecouque, Myriam Witvrouw, De Clercq Erik

Article2019

Targeting the hydrophobic channel of NNIBP: discovery of novel 1,2,3-triazole-derived diarylpyrimidines as novel HIV-1 NNRTIs with high potency against wild-type and K103N mutant virus

Zhongxia Zhou, Tao Liu, Gaochan Wu, Dongwei Kang, Zhipeng Fu, Zhao Wang, De Clercq Erik, Christophe Pannecouque, Peng Zhan, Xinyong Liu

Article2003

Inhibition of Human Immunodeficiency Virus by a New Class of Pyridine Oxide Derivatives

Miguel Stevens, Christophe Pannecouque, De Clercq Erik, Jan Balzarini

Article2014

Synthesis and Anti‐<scp>HIV</scp> Activity of 4‐(Naphthalen‐1‐yl)‐1,2,5‐thiadiazol‐3‐hydroxyl Derivatives

Diwakar Rai, Wen‐Ming Chen, Peng Zhan, Hong Liu, Ye Tian, Xin Liang, De Clercq Erik, Christophe Pannecouque, Jan Balzarini, Xinyong Liu