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Design, Synthesis and SAR Studies of Novel and Potent Dipeptidyl Peptidase 4 Inhibitors
Author(s) -
Luo Na,
Fang Xiaoyu,
Su Mingbo,
Zhang Xinwen,
Li Dan,
Li Honglin,
Li Shiliang,
Zhao Zhenjiang
Publication year - 2021
Publication title -
chinese journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.28
H-Index - 41
eISSN - 1614-7065
pISSN - 1001-604X
DOI - 10.1002/cjoc.202000342
Subject(s) - chemistry , dipeptidyl peptidase 4 , enzyme , type 2 diabetes mellitus , dipeptidyl peptidase , amine gas treating , pharmacology , stereochemistry , combinatorial chemistry , diabetes mellitus , biochemistry , type 2 diabetes , endocrinology , organic chemistry , medicine
Main observation and conclusion Dipeptidyl peptidase 4 (DPP‐4) is a clinically validated target for the treatment of type 2 diabetes mellitus (T2DM). To discover novel and potent DPP‐4 inhibitors, three series of compounds were designed and synthesized in this study based on our previously identified novel scaffold of 2‐phenyl‐3,4‐dihydro‐2 H ‐benzo[ f ]chromen‐3‐amine. Among the designed compounds, 41d‐1 was the most potent one with an IC 50 value of 16.00 nM. Besides, 41d‐1 (5 mg/kg) displayed a moderate glucose tolerance capability in ICR mice. Structure‐activity‐relationship (SAR) studies were discussed in detail, which is constructive for our further optimization.

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