Picomolar inhibitor of reverse transcriptase featuring significantly improved metabolic stability

• Main Authors: Ya-Li Sang (Author), Christophe Pannecouque (Author), Erik De Clercq (Author), Shuai Wang (Author), Fen-Er Chen (Author)
• Format: Book
• Published: Elsevier, 2023-07-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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...