E-viri
Recenzirano
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Qiu, Zongxing; Lin, Xianfeng; Zhou, Mingwei; Liu, Yongfu; Zhu, Wei; Chen, Wenming; Zhang, Weixing; Guo, Lei; Liu, Haixia; Wu, Guolong; Huang, Mengwei; Jiang, Min; Xu, Zhiheng; Zhou, Zheng; Qin, Ning; Ren, Shuang; Qiu, Hongxia; Zhong, Sheng; Zhang, Yuxia; Zhang, Yi; Wu, Xiaoyue; Shi, Liping; Shen, Fang; Mao, Yi; Zhou, Xue; Yang, Wengang; Wu, Jim Z; Yang, Guang; Mayweg, Alexander V; Shen, Hong C; Tang, Guozhi
Journal of medicinal chemistry, 08/2016, Letnik: 59, Številka: 16Journal Article
Targeting the capsid protein of hepatitis B virus (HBV) and thus interrupting normal capsid formation have been an attractive approach to block the replication of HBV viruses. We carried out multidimensional structural optimizations based on the heteroaryldihydropyrimidine (HAP) analogue Bay41-4109 (1) and identified a novel series of HBV capsid inhibitors that demonstrated promising cellular selectivity indexes, metabolic stabilities, and in vitro safety profiles. Herein we disclose the design, synthesis, structure–activity relationship (SAR), cocrystal structure in complex with HBV capsid proteins and in vivo pharmacological study of the 4-methyl HAP analogues. In particular, the (2S,4S)-4,4-difluoroproline substituted analogue 34a demonstrated high oral bioavailability and liver exposure and achieved over 2 log viral load reduction in a hydrodynamic injected (HDI) HBV mouse model.
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Dostop do baze podatkov JCR je dovoljen samo uporabnikom iz Slovenije. Vaš trenutni IP-naslov ni na seznamu dovoljenih za dostop, zato je potrebna avtentikacija z ustreznim računom AAI.
Leto | Faktor vpliva | Izdaja | Kategorija | Razvrstitev | ||||
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
Baze podatkov, v katerih je revija indeksirana
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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Vir: Osebne bibliografije
in: SICRIS
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