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Synthesis and antimycobacterial activity of thiazolidine-2,4-dione based derivatives with halogenbenzohydrazones and pyridinecarbohydrazones substituents.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2020 Mar 01; Vol. 189, pp. 112045. Date of Electronic Publication: 2020 Jan 10. - Publication Year :
- 2020
-
Abstract
- The two series of thiazolidine-2,4-dione (TZD) based hybrids with halogenbenzohydrazones and pyridinecarbohydrazones substituents were designed and synthesized. Target hydrazones were evaluated for their antimycobacterial activity by broth microdilution method with resazurin as an indicator of the metabolic activity of mycobacteria. Conducted studies revealed antimycobacterial activity in the concentration range of 1-512 μg/ml for 23 synthesized TZD-based derivatives. The highest antimycobacterial activity (MIC = 1 μg/ml) was demonstrated for the new group of compounds: TZD-based derivatives with pyridine-4-carbohydrazone substituent. Furthermore, all the tested compounds within this group were characterized by low cytotoxicity. On the basis of the results obtained, three compounds with the highest SI were selected. High effectiveness and safety of these synthesized derivatives makes them promising candidates as antimycobacterial agents.<br />Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.<br /> (Copyright © 2020 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Animals
Antitubercular Agents chemical synthesis
Chlorocebus aethiops
Drug Design
Hydrazones chemical synthesis
Microbial Sensitivity Tests
Molecular Structure
Mycobacterium tuberculosis drug effects
Thiazolidinediones chemical synthesis
Vero Cells
Antitubercular Agents pharmacology
Hydrazones pharmacology
Thiazolidinediones pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 189
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 31951961
- Full Text :
- https://doi.org/10.1016/j.ejmech.2020.112045