Picomolar inhibitor of reverse transcriptase featuring significantly improved metabolic stability

Considering the undesirable metabolic stability of our recently identified NNRTI 5 (t1/2 = 96 min) in human liver microsomes, we directed our efforts to improve its metabolic stability by introducing a new favorable hydroxymethyl side chain to the C-5 position of pyrimidine. This strategy provided a...

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Bibliographic Details
Main Authors: Ya-Li Sang, Christophe Pannecouque, Erik De Clercq, Shuai Wang, Fen-Er Chen
Format: Article
Language:English
Published: Elsevier 2023-07-01
Series:Acta Pharmaceutica Sinica B
Subjects:
Online Access:http://www.sciencedirect.com/science/article/pii/S2211383523001120