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- Title
Synthesis, Spectroscopic Characterization, and Biological Evaluation of Thiazolidin-4-one Derivatives of Sulfamethoxazole: Insights into ADMET Properties and Molecular Docking Studies.
- Authors
Hamdan, I. A. A.; Matloob, A. H.; Gatea, E. A.; Alfuraiji, N.
- Abstract
Antibiotic resistance has emerged as a formidable public health challenge, being recognized as a paramount priority demanding urgent resolution. Consequently, to augment the therapeutic armamentarium in combating recalcitrant microorganisms, the synthesis of novel molecules derived from pre-existing drugs has demonstrated substantial promise as an alternative approach. Herein, five novel thiazolidin-4-one derivatives based on sulfamethoxazole were successfully synthesized. The chemical structures were well characterized using FT-IR, 1H NMR, and 13C NMR and CHNS. Adjectives are predicted for ADMET properties and study the molecular docking for synthesis derivatives, percentage hemolysis ratio was within range (2.5–60%). Biological activity was also evaluated against two types of bacteria, Pseudomonas aeruginosa and Staphylococcus aureus, the results show that the synthesis compounds have good activity against Pseudomonas aeruginosa. Liver enzymes results show that synthesis compounds have a significant effect on raising liver enzymes compared with the reference and the healthy person.
- Subjects
MOLECULAR docking; SULFAMETHOXAZOLE; LIVER enzymes; PSEUDOMONAS aeruginosa; DRUG resistance in bacteria
- Publication
Russian Journal of General Chemistry, 2023, Vol 93, Issue 11, p2917
- ISSN
1070-3632
- Publication type
Article
- DOI
10.1134/S1070363223110233