Discovery of highly potent renin inhibitors potentially interacting with the S3鈥?subsite of renin

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Discovery of highly potent renin inhibitors potentially interacting with the S3鈥?subsite of renin

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作者：Xiaowei Sun^a ; ^b ; ¹ ; Xiaoan Wen^a ; ^b ; ¹ ; Yan-yan Chen^c ; Chen Shi^a ; ^b ; Chengzhe Gao^a ; ^b ; Yong Wu^a ; ^b ; Li-jun Wang^c ; Xiu-hong Yang^c ; ^{ljkyxhljn@163.com" class="auth_mail" title="E-mail the corresponding author} ; Hongbin Sun^a ; ^b ; ^{hbsun2000@yahoo.com" class="auth_mail" title="E-mail the corresponding author}
关键词：Renin inhibitors ; Structural modification ; Aliskiren ; Antihypertension
刊名：European Journal of Medicinal Chemistry
出版年：2015
出版时间：20 October 2015
年：2015
卷：103
期：Complete
页码：269-288
全文大小：2274 K

文摘

•: Several highly potent renin inhibitors have been identified by structural modification of aliskiren.
•: The most promising compound boldFont">39 was more potent than aliskiren.
•: Compound boldFont">39 had a good inhibitory selectivity for renin over cathepsins D and E.
•: Compound boldFont">39 displayed significant antihypertensive effect in double transgenic mouse hypertensive model.
•: The S3′ subsite of renin active site merits further exploration for renin inhibitor design.

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