Synthesis and antiviral evaluation of novel heteroarylpyrimidines analogs as HBV capsid effectors. Issue 4 (15th February 2017)

• Record Type: Journal Article
• Authors: Boucle, Sebastien; Lu, Xiao; Bassit, Leda; Ozturk, Tugba; Russell, Olivia Ollinger; Amblard, Franck; Coats, Steven J.; Schinazi, Raymond F.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 4(2017)
• Page Start: 904
• Page End: 910
• Publication Date: 2017-02-15
• Subjects: HBV -- HAP -- Heteroarylpyrimidine -- Capsid assembly effectors; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.01.010
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: New modifications to the scaffold of previously reported HBV capsid assembly effectors such as BAY 41-4109, HAP-12 and GLS4 were explored. The anti-HBV activity in the HepAD38 system, and cytotoxicity profiles of each of the new compounds has been assessed. Among them, five new iodo- and bromo-heteroarylpyrimidines analogs displayed anti-HBV activity in the low micromolar range.