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Oxadiazepinone HBV capsid assembly modulators
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2021-09-04 , DOI: 10.1016/j.bmcl.2021.128353
Scott D Kuduk 1 , Bart Stoops 2 , Angela M Lam 1 , Christine Espiritu 1 , Robert Vogel 1 , Vincent Lau 1 , Klaus Klumpp 1 , Osvaldo A Flores 1 , George D Hartman 1
Affiliation  

The HBV core protein serves multiple essential functions in the viral life cycle that enable chronic HBV infection to persist, and as such, represents a promising drug target. Modulation of the HBV capsid assembly has shown efficacy in early clinical trials through use of small molecule capsid assembly modulators (CAMs). Herein is described the evolution and SAR of a novel pyrazolo piperidine lead series into advanced oxadiazepinone HBV CAMs.



中文翻译:

Oxadiazepinone HBV衣壳组装调节剂

HBV 核心蛋白在病毒生命周期中发挥多种重要功能,使慢性 HBV 感染能够持续存在,因此,它代表了一个有前途的药物靶点。通过使用小分子衣壳组装调节剂 (CAM),HBV 衣壳组装的调节已在早期临床试验中显示出功效。本文描述了一种新型吡唑并哌啶先导系列在先进的恶二氮杂卓 HBV CAM 中的演变和 SAR。

更新日期:2021-10-06
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