Identification of potent α-amylase inhibitors via dynamic combinatorial chemistry

  • Bioorg Med Chem. 2022 Jan 6;55:116609. doi: 10.1016/j.bmc.2022.116609.
Yao Wu  1 ,  Shuang Zhao  1 ,  Lei Hu  2
Affiliations
  • 1. School of Pharmacy, Jiangsu University, 301 Xuefu Rd., Zhenjiang, China.
  • 2. School of Pharmacy, Jiangsu University, 301 Xuefu Rd., Zhenjiang, China. Electronic address: [email protected].
PMID: 35021143 DOI: 10.1016/j.bmc.2022.116609
Abstract

In this study, we report for the first time the discovery of potent α-amylase inhibitors using principle of dynamic combinatorial chemistry. The best compound identified exhibited not only high inhibitory efficiency but also low cytotoxicity. The binding mode and possible mechanism are determined in the subsequent kinetic and molecular docking studies.

Keywords
Dynamic combinatorial chemistry; Kinetic analysis; Molecular docking; Protein inhibition; α-amylase.
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