Janssen Research and Development, 1400 McKean Road, Spring House, PA 19477, United States.
Janssen Research and Development, 1400 McKean Road, Spring House, PA 19477, United States.
Bioorg Med Chem Lett. 2022 Sep 15;72:128823. doi: 10.1016/j.bmcl.2022.128823. Epub 2022 May 27.
The HBV capsid core protein serves a number of important functions in the viral life cycle enabling chronic HBV infection to persist, and therefore is a promising drug target. Interfering with capsid assembly has shown efficacy in clinical trials with small molecule capsid assembly modulators (CAMs). Herein is described the further optimization of a progressive series of diazepinone HBV CAMs.
HBV 衣壳核心蛋白在病毒生命周期中发挥着许多重要功能，使慢性 HBV 感染得以持续存在，因此成为有前途的药物靶点。干扰衣壳组装已在小分子衣壳组装调节剂 (CAM) 的临床试验中显示出疗效。本文描述了对一系列逐步优化的二氮杂环酮 HBV CAM 的进一步优化。
