Discovery of thiophene‐containing biaryl amide derivatives as novel glucagon receptor antagonists,Chemical Biology & Drug Design

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Discovery of thiophene‐containing biaryl amide derivatives as novel glucagon receptor antagonists
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2018-04-10 , DOI: 10.1111/cbdd.13184
Jia Li _{1,

2,

3,

4} , Yang Feng ₅ , Huihui Li _{1,

2,

3} , Shuangjie Shu _{1,

2,

3} , Antao Dai ₅ , Xiaoqing Cai ₅ , Jiang Wang _{1,

2,

3} , Dehua Yang _{2,

3,

5} , Dakota Ma ₅ , Ming-Wei Wang _{2,

3,

5} , Hong Liu _{1,

2,

3,

4}

Affiliation

A novel series of thiophene‐containing biaryl amide glucagon receptor (GCGR) antagonists were designed and synthesized. Two compounds of this series, 14f and 14h, exhibited good GCGR binding (IC₅₀ = 6.1 and 4.4 μm, respectively) and cAMP functional activities (IC₅₀ = 4.4 and 14.4 μm, respectively). The possible binding modes of compounds 14f and 14h with GCGR were explored by molecular simulation.

中文翻译：

发现含有噻吩的联芳酰胺衍生物作为新型胰高血糖素受体拮抗剂

设计并合成了一系列新型的含有噻吩的联芳酰胺酰胺胰高血糖素受体（GCGR）拮抗剂。这一系列中，两种化合物14F和14H，显示出良好的结合GCGR（IC ₅₀ = 6.1和4.4μ米，分别地）和cAMP功能活性（IC ₅₀ = 4.4和14.4μ米，分别地）。通过分子模拟探索了化合物14f和14h与GCGR的可能结合方式。

更新日期：2018-04-10

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