The SAR-based development of small molecular HBV capsid assembly modulators

The SAR-based development of small molecular HBV capsid assembly modulators
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基于 SAR 的小分子 HBV 衣壳组装调节剂的开发

DOI:
10.1007/s00044-022-02936-5
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发表时间:
2022-07
影响因子:
2.6
通讯作者:
Rong Sheng
Rong Sheng
中科院分区:
医学4区
文献类型:
--
作者:
Yunwen Wang;Shendan Wang;Xuefen Tao;Yuan Wang;Yuxuan Wu;Na Chen;Chenxian Hu;Hao Wang;Shuang Yu;Rong Sheng

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B型肝炎病毒(HBV)感染全球约2.96亿人,而临床上有效的治疗药物仍然有限。衣壳蛋白组装调节剂(CAM)是一种有效的抗HBV药物,具有实现功能性治疗的潜力,近年来受到广泛关注。目前已经开发出多种新型的支架药物,并且已经有十多种CAM候选药物进入临床试验,具有有效的抗HBV活性。本文综述了近年来基于SAR的各种骨架CAMs的研究进展,包括杂芳基二氢嘧啶(HAPs)、苯基丙烯酰胺(PPA)、氨磺酰苯甲酰胺(SBAs)、哒嗪酮、双杂环、芳基甲酰胺、氨基噻唑等,为CAMs的进一步开发提供了新的思路。
Hepatitis B virus (HBV) infected about 296 million people worldwidely, while clinical useful therapeutic agents were still limited. Capsid assembly modulators (CAM) have been validated as efficient anti-HBV virus agents with the potential to achieve functional cure, therefore piqued much attention in recent years. There are various novel scaffold agents been developed and more than ten CAM candidates have been progressed into clinical trials with efficient anti-HBV activities. Herein, we summarised the SAR-based development of CAMs with various scaffolds, including heteroaryldihydropyrimidines (HAPs), phenylacrylamides (PPAs), sulfamoylbenzamides (SBAs), pyridazinone, bis-heterocycle, arylformamides, aminothiazoles, and others, which may provide new suggestions for the further development of CAMs.
DOI: 10.1016/j.bmc.2016.12.017
发表时间: 2017-02-01
影响因子: 3.5
作者:
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