2. Academic Validation
  3. Synthesis and structure-activity relationship studies of 2,4-thiazolidinediones and analogous heterocycles as inhibitors of dihydrodipicolinate synthase

Synthesis and structure-activity relationship studies of 2,4-thiazolidinediones and analogous heterocycles as inhibitors of dihydrodipicolinate synthase

  • Bioorg Med Chem. 2021 Dec 15;52:116518. doi: 10.1016/j.bmc.2021.116518.
Rebecca M Christoff 1,  Tatiana P Soares da Costa 2,  Saadi Bayat 1,  Jessica K Holien 3,  Matthew A Perugini 2,  Belinda M Abbott 4
Affiliations

Affiliations

  • 1 Department of Chemistry and Physics, La Trobe Institute for Molecular Science, La Trobe University, Melbourne, Victoria 3086, Australia.
  • 2 Department of Biochemistry and Genetics, La Trobe Institute for Molecular Science, La Trobe University, Melbourne, Victoria 3086, Australia.
  • 3 School of Science, STEM College, RMIT University, Melbourne, Victoria 3000, Australia.
  • 4 Department of Chemistry and Physics, La Trobe Institute for Molecular Science, La Trobe University, Melbourne, Victoria 3086, Australia. Electronic address: [email protected].
PMID: 34826680 DOI: 10.1016/j.bmc.2021.116518
Abstract

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.

Keywords

DHDPS inhibitors; Dihydrodipicolinate synthase; Enzyme inhibitors; Thiazolidinediones.

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