Synthesis and structure-activity relationship studies of 2,4-thiazolidinediones and analogous heterocycles as inhibitors of dihydrodipicolinate synthase
| Autor: | Rebecca M. Christoff, Jessica K Holien, Belinda M. Abbott, Tatiana P. Soares da Costa, Saadi Bayat, Matthew A. Perugini |
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| Rok vydání: | 2021 |
| Předmět: |
Dihydrodipicolinate synthase
Clinical Biochemistry Pharmaceutical Science Biochemistry Structure-Activity Relationship 03 medical and health sciences Diaminopimelate pathway Heterocyclic Compounds Drug Discovery Escherichia coli Structure–activity relationship Enzyme Inhibitors Molecular Biology Hydro-Lyases 030304 developmental biology chemistry.chemical_classification 0303 health sciences Dose-Response Relationship Drug Molecular Structure biology 030302 biochemistry & molecular biology Organic Chemistry Lysine Biosynthesis Pathway 3. Good health Enzyme chemistry Committed step biology.protein Molecular Medicine Thiazolidinediones Lysine biosynthesis |
| Zdroj: | Bioorganic & Medicinal Chemistry. 52:116518 |
| ISSN: | 0968-0896 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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