Exploring the hydrophobic channel of NNIBP leads to the discovery of novel piperidine-substituted thiophene[3,2-d]pyrimidine derivatives as potent HIV-1 NNRTIs

Exploring the hydrophobic channel of NNIBP leads to the discovery of novel piperidine-substituted thiophene[3,2-d]pyrimidine derivatives as potent HIV-1 NNRTIs

In this report, a series of novel piperidine-substituted thiophene[3,2-d]pyrimidine derivatives were designed to explore the hydrophobic channel of the non-nucleoside reverse transcriptase inhibitors binding pocket (NNIBP) by incorporating an aromatic moiety to the left wing of the lead K-5a2. The n...

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Bibliographic Details
Main Authors: Dongwei Kang, Da Feng, Tiziana Ginex, Jinmi Zou, Fenju Wei, Tong Zhao, Boshi Huang, Yanying Sun, Samuel Desta, Erik De Clercq, Christophe Pannecouque, Peng Zhan, Xinyong Liu
Format: Article
Language:English
Published: Elsevier 2020-05-01
Series:Acta Pharmaceutica Sinica B
Subjects:
HIV-1
NNRTIs
NNIBP
Thiophene[3,2-d]pyrimidine
Hydrophobic channel
Online Access:http://www.sciencedirect.com/science/article/pii/S2211383519306641

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http://www.sciencedirect.com/science/article/pii/S2211383519306641

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