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

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

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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

机译：基于2-（Thieno [2,3b]吡啶-2-基）-1,3,4-氧代唑支架的新系列HCV抑制剂

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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 similar to 100-fold improvement in potency compared with compound 1, with an EC50 of 0.039 mu M, but without obvious cytotoxicity in vitro.

机译：基于2-（Thieno [2,3-B] Pyridin-2-y1）-1,3,4-氧代唑支架的新系列HCV抑制剂。详细的SAR调查显示HCV抑制活性对C5，C6稠环和C5'环烷烃的尺寸和柔韧性敏感的，这导致了几种具有对HCV基因型1B复制子具有有效抑制活性的化合物的鉴定。与化合物1相比，最有效的化合物10d显示出类似于100倍的效力，EC50为0.039μm，但在体外没有明显的细胞毒性。

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《RSC Advances》 |2016年第46期|共10页
作者
Zuo Wei-Qiong; Wang Ning-Yu; Zhu Yong-xia; Liu Li; Xiao Kun-Jie; Zhang Li-Dan; Gao Chao; Liu Zhi-Hao; You Xin-Yu; Shi Yao-Jie; Peng Cui-Ting; Ran Kai; Tang Hong; Yu Luo-Ting;
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Sichuan Univ West China MedicalSch West China Hosp State Key Lab Biotherapy Chengdu 610041 Peoples R China;

Sichuan Univ West China MedicalSch West China Hosp State Key Lab Biotherapy Chengdu 610041 Peoples R China;

Sichuan Univ West China MedicalSch West China Hosp State Key Lab Biotherapy Chengdu 610041 Peoples R China;

Sichuan Univ West China MedicalSch West China Hosp State Key Lab Biotherapy Chengdu 610041 Peoples R China;

Sichuan Univ West China MedicalSch West China Hosp State Key Lab Biotherapy Chengdu 610041 Peoples R China;

Sichuan Univ West China MedicalSch West China Hosp State Key Lab Biotherapy Chengdu 610041 Peoples R China;

Sichuan Univ West China MedicalSch West China Hosp State Key Lab Biotherapy Chengdu 610041 Peoples R China;

Sichuan Univ West China MedicalSch West China Hosp State Key Lab Biotherapy Chengdu 610041 Peoples R China;

Sichuan Univ West China MedicalSch West China Hosp State Key Lab Biotherapy Chengdu 610041 Peoples R China;

Sichuan Univ West China MedicalSch West China Hosp State Key Lab Biotherapy Chengdu 610041 Peoples R China;

Sichuan Univ West China MedicalSch West China Hosp State Key Lab Biotherapy Chengdu 610041 Peoples R China;

Sichuan Univ West China MedicalSch West China Hosp State Key Lab Biotherapy Chengdu 610041 Peoples R China;

Sichuan Univ West China MedicalSch West China Hosp State Key Lab Biotherapy Chengdu 610041 Peoples R China;

Sichuan Univ West China MedicalSch West China Hosp State Key Lab Biotherapy Chengdu 610041 Peoples R China;

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1. A new series of HCV inhibitors based on a 2-(thieno[2,3b]pyridin-2-yl)-1,3,4-oxadiazole scaffold [J] . Zuo Wei-Qiong, Wang Ning-Yu, Zhu Yong-xia, RSC Advances . 2016,第46期

机译：基于2-（Thieno [2,3b]吡啶-2-基）-1,3,4-氧代唑支架的新系列HCV抑制剂
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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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