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

• Main Authors: Dongwei Kang (Author), Da Feng (Author), Tiziana Ginex (Author), Jinmi Zou (Author), Fenju Wei (Author), Tong Zhao (Author), Boshi Huang (Author), Yanying Sun (Author), Samuel Desta (Author), Erik De Clercq (Author), Christophe Pannecouque (Author), Peng Zhan (Author), Xinyong Liu (Author)
• Format: Book
• Published: Elsevier, 2020-05-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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...