Kartsev Victor, Geronikaki Athina, Zubenko Alexander, Petrou Anthi, Ivanov Marija, Glamočlija Jasmina, Sokovic Marina, Divaeva Lyudmila, Morkovnik Anatolii, Klimenko Alexander
InterBioScreen, 119019 Moscow, Russia.
School of Health, Faculty of Pharmacy, Aristotle University, 54124 Thessaloniki, Greece.
Antibiotics (Basel). 2022 Sep 30;11(10):1337. doi: 10.3390/antibiotics11101337.
Herein, we report the design, synthesis, and evaluation of the antimicrobial activity of new heteroaryl (aryl) thiazole derivatives. The design was based on a molecular hybridization approach. The in vitro evaluation revealed that these compounds demonstrated moderate antibacterial activity. The best activity was achieved for compound , with MIC and MBC in the range of 0.23-0.7 and 0.47-0.94 mg/mL, respectively. Three compounds (, , and ) were tested against three resistant strains, namely methicillin resistant , , and , which showed higher potential than the reference drug ampicillin. Antifungal activity of the compounds was better with MIC and MFC in the range of 0.06-0.47 and 0.11-0.94 mg/mL, respectively. The best activity was observed for compound , with MIC at 0.06-0.23 mg/mL and MFC at 0.11-0.47 mg/mL. According to docking studies, the predicted inhibition of the MurB enzyme is a putative mechanism of the antibacterial activity of the compounds, while inhibition of 14a-lanosterol demethylase is probably the mechanism of their antifungal activity.
在此，我们报告新型杂芳基（芳基）噻唑衍生物的抗菌活性的设计、合成及评估。该设计基于分子杂交方法。体外评估显示这些化合物表现出适度的抗菌活性。化合物 的活性最佳，其最低抑菌浓度（MIC）和最低杀菌浓度（MBC）分别在0.23 - 0.7和0.47 - 0.94 mg/mL范围内。三种化合物（ 、 和 ）针对三种耐药菌株进行了测试，即耐甲氧西林 、 和 ，它们显示出比参比药物氨苄西林更高的潜力。这些化合物的抗真菌活性较好，MIC和最低杀菌浓度（MFC）分别在0.06 - 0.47和0.11 - 0.94 mg/mL范围内。化合物 的活性最佳，MIC为0.06 - 0.23 mg/mL，MFC为0.11 - 0.47 mg/mL。根据对接研究，预测对MurB酶的抑制是这些化合物抗菌活性的一种假定机制，而对14α-羊毛甾醇脱甲基酶的抑制可能是其抗真菌活性的机制。
