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2-Aryl-3-(6-trifluoromethoxy)benzo[d]thiazole-based thiazolidinone hybrids as potential anti-infective agents: Synthesis, biological evaluation and molecular docking studies
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-11-27 , DOI: 10.1016/j.bmcl.2020.127718
Michelyne Haroun 1 , Christophe Tratrat 1 , Anthi Petrou 2 , Athina Geronikaki 2 , Marina Ivanov 3 , Ana Ciric 3 , Marina Sokovic 3
Affiliation  

The search for new antimicrobial agents is greater than ever due to the perpetual threat of multidrug resistance in known pathogens and the relentless emergence of new infections. In this manuscript, ten thiazole-based thiazolidinone hybrids bearing a 6-trifluoromethoxy substituent on the benzothiazole core were synthesized and evaluated against a panel of four bacterial strains Salmonella typhimurium, Staphylococcus aureus, Escherichia coli and Listeria monocytogenes and three resistant strains Pseudomonas aeruginosa, E. coli and MRSA. The evaluation of minimum bactericidal and minimum inhibitory concentrations was accomplished by microdilution assay. As reference compounds ampicillin and streptomycin were employed. All compounds displayed antibacterial efficiencies with MBCs/MICs at 0.25–1 mg/mL and 0.12–1 mg/mL respectively while ampicillin displayed MBCs/MICs at 0.15–0.3 mg/mL and at 0.1–0.2 mg/mL respectively. MICs/MBC of streptomycin varied from 0.05 to 0.15 mg/mL and from 0.1 to 0.3 mg/mL respectively. The best overall effect was observed for compound h4, while compound h1 exhibited the highest effective action against E. coli (MIC/MBC 0.12/0.25 mg/ml) among all tested compounds.



中文翻译:

2-Aryl-3-(6-三氟甲氧基)苯并[d]噻唑基噻唑烷酮杂化物作为潜在的抗感染剂:合成、生物学评价和分子对接研究

由于已知病原体中多药耐药性的持续威胁和新感染的不断出现,对新抗菌药物的探索比以往任何时候都更加激烈。在该手稿,10噻唑系噻唑烷酮杂种支承在苯并噻唑核心的6-三氟甲氧基的取代基进行合成并评价针对四种细菌菌株面板鼠伤寒沙门氏菌,金黄色葡萄球菌,大肠杆菌李斯特菌和三个耐药菌株铜绿假单胞菌和大肠杆菌和 MRSA。最低杀菌浓度和最低抑菌浓度的评价通过微量稀释法进行。使用参考化合物氨苄青霉素和链霉素。所有化合物均显示出抗菌效率,MBCs/MICs 分别为 0.25–1 mg/mL 和 0.12–1 mg/mL,而氨苄西林显示 MBCs/MICs 分别为 0.15–0.3 mg/mL 和 0.1–0.2 mg/mL。链霉素的 MIC/MBC 分别在 0.05 至 0.15 mg/mL 和 0.1 至 0.3 mg/mL 之间变化。观察到化合物 h4 的总体效果最好,而化合物 h1在所有测试化合物中对大肠杆菌表现出最高的有效作用(MIC/MBC 0.12/0.25 mg/ml)。

更新日期:2020-12-02
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