Department of Chemistry and Physics, La Trobe Institute for Molecular Science, La Trobe University, Melbourne, Victoria 3086, Australia.
Department of Biochemistry and Genetics, La Trobe Institute for Molecular Science, La Trobe University, Melbourne, Victoria 3086, Australia.
Bioorg Med Chem. 2021 Dec 15;52:116518. doi: 10.1016/j.bmc.2021.116518. Epub 2021 Nov 12.
Dihydrodipicolinate synthase (DHDPS), responsible for the first committed step of the diaminopimelate pathway for lysine biosynthesis, has become an attractive target for the development of new antibacterial and herbicidal agents. Herein, we report the discovery and exploration of the first inhibitors of E. coli DHDPS which have been identified from screening lead and are not based on substrates from the lysine biosynthesis pathway. Over 50 thiazolidinediones and related analogues have been prepared in order to thoroughly evaluate the structure-activity relationships against this enzyme of significant interest.
二氢二吡啶羧酸合酶（DHDPS）负责赖氨酸生物合成的二氨基庚二酸途径的第一步，已成为开发新型抗菌和除草剂的有吸引力的靶标。在此，我们报告了从筛选先导化合物中发现和探索大肠杆菌 DHDPS 的第一种抑制剂的情况，这些抑制剂不是基于赖氨酸生物合成途径的底物。为了彻底评估对这种具有重要意义的酶的活性关系，已经制备了 50 多个噻唑烷二酮及其相关类似物。
