A new series of HCV inhibitors based on a 2-(thieno[2,3b]pyridin-2-yl)-1,3,4-oxadiazole scaffold

Wei-Qiong Zuo; Ning-Yu Wang; Yong-xia Zhu; Li Liu; Kun-Jie Xiao; Li-Dan Zhang; Chao Gao; Zhi-Hao Liu; Xin-Yu You; Yao-Jie Shi; Cui-Ting Peng; Kai Ran; Hong Tang; Luo-Ting Yu

doi:10.1039/C6RA01179A

A new series of HCV inhibitors based on a 2-(thieno[2,3b]pyridin-2-yl)-1,3,4-oxadiazole scaffold

Wei-Qiong Zuo,†^a Ning-Yu Wang,†^a Yong-xia Zhu,^a Li Liu,^ab Kun-Jie Xiao,^a Li-Dan Zhang,^a Chao Gao,^a Zhi-Hao Liu,^a Xin-Yu You,^ab Yao-Jie Shi,^a Cui-Ting Peng,^ab Kai Ran,^a Hong Tang^a and Luo-Ting Yu*^a

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^a State Key Laboratory of Biotherapy, West China Hospital, West China MedicalSchool, Sichuan University, Chengdu 610041, China
E-mail: yuluot@scu.edu.cn
Fax: +86-28-85164060
Tel: +86-28-85164063

^b Department of Pharmaceutical and Bioengineering, School of Chemical Engineering, Sichuan University, Chengdu, Sichuan 610065, China

Abstract

A new series of HCV inhibitors based on a 2-(thieno[2,3-b]pyridin-2-yl)-1,3,4-oxadiazole scaffold was developed. Detailed SAR investigations revealed the HCV inhibitory activity was sensitive to the size of C5, the C6-fused ring, and the size and flexibility of C5′ cycloalkane, which led to the identification of several compounds with potent inhibitory activity against HCV genotype 1b replicon. The most potent compound 10d showed ∼100-fold improvement in potency compared with compound 1, with an EC₅₀ of 0.039 μM, but without obvious cytotoxicity in vitro.

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A new series of HCV inhibitors based on a 2-(thieno[2,3b]pyridin-2-yl)-1,3,4-oxadiazole scaffold

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A new series of HCV inhibitors based on a 2-(thieno[2,3b]pyridin-2-yl)-1,3,4-oxadiazole scaffold

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