Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
Regular Article
Design, Synthesis, and Biological Evaluation of Novel 2-Heteroaryl-oxazolidine-4-one Derivatives as Novel HBV Capsid Assembly Modulators
Xuefen TaoYuan WangYunwen WangYinxiu JinYuxin WangJiansong LiRong Sheng
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2024 Volume 47 Issue 12 Pages 2003-2010

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Abstract

Using 2-pyrazole oxazolidine-4-one derivative 1 as the lead compound, a series of novel 2-heteroaryl-oxazolidine-4-one derivatives were designed and synthesized by replacing pyrazole moiety with other heterocycles, including methyl pyrazole, oxazole, thiazole, triazole, and reverse pyrazoles, based on the principle of bioisosterism. The structures of target compounds were established by 1H-NMR, 13C-NMR, and electrospray ionization (ESI)-MS. Majority of these compounds showed moderate to good inhibitory activities against hepatitis B virus (HBV) DNA proliferation with low cytotoxicities. Especially, compound 7g showed the most potent anti-HBV activity with EC50 value of 0.059 µM, accompanied with better selectivity index (SI) value than that of lead compound. Our research revealed the structure–activity relationship (SAR) of these newly designed compounds and compound 7g was identified as the potential HBV capsid assembly modulator.

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Published by The Pharmaceutical Society of Japan

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