Work

Design, synthesis and evaluation of 3-phenoxypyrazine-2-carboxamide derivatives as potent TGR5 agonists

Year: 2022

Type: article

Abstract: . The most potent compounds 18g and 18k exhibited excellent hTGR5 agonist activity, which was superior to those of the reference drug INT-777. In addition, compound 18k could significantly reduce blood glucose levels in C57 BL/6 mice and stimulate GLP-1 secretion in NCI-H716 cells and C57 BL/6 mice.

Source: RSC Advances

DOI: 10.1039/d1ra08867j

Authors: Shizhen Zhao, Le Wang, Jie Wang, Chenwei Wang, Shaowei Zheng, Yajie Fu, Yunfu Li, Wei-Dong Chen, Ruifang Hou, Dongbin Yang, Yan-Dong Wang

Institutions: Henan University, Inner Mongolia Medical University, State Key Laboratory of Chemical Resource Engineering, Beijing University of Chemical Technology

Language: English

Topic: Heterocyclic Compound Synthesis and Bioactivity

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

SDG: Good health and well-being

Open Access status: gold

Estimated APC paid: $1,042

Funders: National Natural Science Foundation of China, China Postdoctoral Science Foundation, Henan University, Natural Science Foundation of Henan Province, Henan Province Science and Technology Innovation Talent Program, China-Japan Friendship Hospital, Fundamental Research Funds for the Central Universities, National College Students Innovation and Entrepreneurship Training Program

Awards: G1916347013, G2255038605, G2745451053, G2926161692, G3014216404, G393740804, G4445088411, G5205474008, G5443538745, G5600847293, G5803023376, G6234502245, G6411766591

OpenAlex ID: W4210693790

FWCI: 0.371

Cites: 23

Cited by: 6

Related to: 10