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1,2,4‐Triazole Derivatives Inhibiting the Human Immunodeficiency Virus Type 1 (HIV‐1) in vitro
Author(s) -
Lagoja Irene M.,
Pannecouque Christophe,
Musumeci Laura,
Froeyen Matheus,
Van Aerschot Arthur,
Balzarini Jan,
Herdewijn Piet,
De Clercq Erik
Publication year - 2002
Publication title -
helvetica chimica acta
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.74
H-Index - 82
eISSN - 1522-2675
pISSN - 0018-019X
DOI - 10.1002/1522-2675(200207)85:7<1883::aid-hlca1883>3.0.co;2-r
Subject(s) - chemistry , reverse transcriptase , in vitro , human immunodeficiency virus (hiv) , docking (animal) , ic50 , virology , triazole , virus , stereochemistry , gene , biochemistry , rna , biology , organic chemistry , medicine , nursing
Abstract 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 IC 50 of 9.98 μ M 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.