Journal of Enzyme Inhibition and Medicinal Chemistry | |
Antioxidant activity and antibacterial evaluation of new thiazolin-4-one derivatives as potential tryptophanyl-tRNA synthetase inhibitors | |
Dan C. Vodnar1  Brînduşa Tiperciuc2  Ovidiu Oniga2  Gabriel Marc2  Anca Stana2  Daniela Benedec3  Radu Tamaian4  | |
[1] Department of Food Science and Technology, University of Agricultural Sciences and Veterinary Medicine, Cluj-Napoca, Romania;Department of Pharmaceutical Chemistry, “Iuliu Haţieganu” University of Medicine and Pharmacy, Cluj-Napoca, Romania;Department of Pharmacognosy, “Iuliu Haţieganu” University of Medicine and Pharmacy, Cluj-Napoca, Romania;ICSI Analytics Department, National Research and Development Institute for Cryogenics and Isotopic Technologies - ICSI Rm. Vâlcea, Râmnicu Vâlcea, Romania;SC Biotech Corp SRL, Râmnicu Vâlcea, Romani; | |
关键词: Thiazolin-4-one; antibacterial activity; antioxidant activity; tryptophanyl-tRNA synthetase; docking; | |
DOI : 10.1080/14756366.2019.1596086 | |
来源: publisher | |
【 摘 要 】
The rapid emergence of bacterial resistance to antibiotics currently available for treating infectious diseases requires effective antimicrobial agents with new structural profiles and mechanisms of action. Twenty-three thiazolin-4-one derivatives were evaluated for their antibacterial activity by determining the growth inhibition zone diameter, the minimum inhibitory concentration (MIC), and the minimum bactericidal concentration (MBC), against gram-positive and gram-negative bacteria. Compounds 3a–c, 3e–h, 6b–c and 9a–c expressed better MIC values than moxifloxacin, against Staphylococcus aureus. Compounds 3h and 9b displayed similar effect to indolmycin, a tryptophanyl-tRNA ligase inhibitor. Due to their structural analogy to indolmycin, all compounds were subjected to molecular docking on tryptophanyl-tRNA synthetase. Compounds 3a–e, 6a–e, 8 and 9a–e exhibited better binding affinities towards the target enzymes than indolmycin. The antioxidant potential of the compounds was evaluated by four spectrophotometric methods. Thiazolin-4-ones 3e, 6e and 9e presented better antiradical activity than ascorbic acid, trolox and BHT, used as references.
【 授权许可】
CC BY
【 预 览 】
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RO202004236366437ZK.pdf | 1218KB | download |