Synthesis and evaluation of α-glucosidase inhibitory activity of sulfonylurea derivatives
Author:
Bui Thi Thoi1, Tran Van Loc2, Ngo Dai Quang3, Tran Van Chien2, Tran Van Sung2, Tran Thi Phuong Thao2
Affiliation:
1. Vietnam Institute of Industrial Chemistry , Nr. 2 Pham Ngu Lao street , Hoan Kiem distric , Ha Noi , Viet Nam 2. Institute of Chemistry, Vietnam Academy of Science and Technology (VAST), and Graduate University of Science and Technology (VAST) , Nr. 18 Hoang Quoc Viet Road , Cau Giay district , Hanoi , Viet Nam 3. Vietnam National Chemical Group , Nr. 1A Trang Tien street , Hoan Kiem district , Ha Noi , Viet Nam
Abstract
Abstract
Two series of sulfonylureas derivatives including 24 compounds (4, 7, 5a–5o, 8a–8h), among them 17 new derivatives, have been synthesized and evaluated for their α-glucosidase inhibitory activity. Compounds 5c, 5h and 8e showed significant in vitro α-glucosidase inhibition with IC50 values of 5.58, 79.85 and 213.36 µm, respectively, comparing with the standard compounds acarbose (IC50 = 268.29 µm) and glipizide (IC50 = 300.47 µm). The preliminary structure-activity relationships (SARs) of the synthesized compounds were also investigated.
Publisher
Walter de Gruyter GmbH
Subject
General Chemistry
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