Structure-activity relationships study of 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives as novel non-nucleoside anti-hepatitis B virus agents.

Guo RH; Zhang Q; Ma YB; Luo J; Geng CA; Wang LJ; Zhang XM; Zhou J; Jiang ZY; Chen JJ

首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Structure-activity relationships study of 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives as novel non-nucleoside anti-hepatitis B virus agents.

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Structure-activity relationships study of 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives as novel non-nucleoside anti-hepatitis B virus agents.

机译：作为新型非核苷类抗乙型肝炎病毒药物的6-氯-4-（2-氯苯基）-3-（2-羟乙基）喹啉-2（1H）-一衍生物的构效关系研究。

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A series of novel 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives were synthesized and evaluated for anti-hepatitis B virus (anti-HBV) activities in vitro to explore their structure-activity relationships (SARs). Most of the synthesized compounds possessed potent anti-HBV activity, of which the promising compound 44 exhibited significantly inhibitory potency against the secretion of hepatitis surface antigen (HBsAg) (IC(50) = 0.010 mM, SI > 135), hepatitis e antigen (HBeAg) (IC(50) = 0.026 mM, SI > 51) and the replication of HBV DNA (IC(50) = 0.045 mM). Preliminary mechanism study suggested compound 44 could mainly enhance the transcript activity of HBV ENI (enhancer I), EN-II (enhancer II).

机译：合成了一系列新型的6-氯-4-（2-氯苯基）-3-（2-羟乙基）喹啉-2（1H）-衍生物，并评估了其抗乙型肝炎病毒的体外活性。探索它们的构效关系（SAR）。大多数合成的化合物都具有有效的抗HBV活性，其中有希望的化合物44对肝炎表面抗原（HBsAg）（IC（50）= 0.010 mM，SI> 135），戊型肝炎抗原（ HBeAg）（IC（50）= 0.026 mM，SI> 51）和HBV DNA复制（IC（50）= 0.045 mM）。初步机理研究表明，化合物44可以主要增强HBV ENI（增强子I），EN-II（增强子II）的转录活性。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2011年第1期|共13页
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Guo RH; Zhang Q; Ma YB; Luo J; Geng CA; Wang LJ; Zhang XM; Zhou J; Jiang ZY; Chen JJ;
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机译：作为新型非核苷类抗乙型肝炎病毒药物的6-氯-4-（2-氯苯基）-3-（2-羟乙基）喹啉-2（1H）-一衍生物的构效关系研究。
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Structure-activity relationships study of 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives as novel non-nucleoside anti-hepatitis B virus agents.

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