Synthesis and biological activity of substituted xanthines as DPP-IV inhibitors
10.16438/j.0513-4870.2015-1171
- VernacularTitle:黄嘌呤类DPP-IV抑制剂的化学合成和生物活性研究
- Author:
Yan-ping LI
1
;
Hong YI
1
;
Xin-bei JIANG
1
;
Zhuo-rong LI
1
Author Information
1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
dipeptidyl peptidase IV inhibitor;
linagliptin;
synthesis;
SAR
- From:
Acta Pharmaceutica Sinica
2016;51(6):947-
- CountryChina
- Language:Chinese
-
Abstract:
In order to find more potential DPP-IV inhibitor, a series of xanthine-scaffold analogs of linagliptin, an approved antidiabetes drug, were designed and synthesized for SAR study. All compounds with a concentration of 50 nmol·L-1 showed the inhibitory activity against DPP-IV enzyme in vitro, and the inhibition rate of compounds 1a, 1d and 1f was over 50%. Virtual docking was also performed to facilitate the SAR analysis of these substituted xanthines.
