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2-叠氮基苯并噻唑的设计、合成及其抗菌和抗生物膜潜力解析:一项综合研究的见解

Design, synthesis, and unraveling the antibacterial and antibiofilm potential of 2-azidobenzothiazoles: insights from a comprehensive study.

作者信息

Qadir Tanzeela, Kanth Saadat A, Aasif Mohammad, Fadul Abdalla N, Yatoo Gulam N, Jangid Kailash, Mir Mushtaq A, Shah Wajahat A, Sharma Praveen K

机构信息

Department of Chemistry, School of Chemical Engineering and Physical Sciences, Lovely Professional University, Phagwara, India.

Centre of Research for Development and P.G Programme in Microbiology, School of Biological Sciences, University of Kashmir, Srinagar, Jammu and Kashmir, India.

出版信息

Front Chem. 2023 Sep 7;11:1264747. doi: 10.3389/fchem.2023.1264747. eCollection 2023.

Abstract

The present study reports the synthesis of 2-azidobenzothiazoles from substituted 2-aminobenzothiazoles using sodium nitrite and sodium azide under mild conditions. All the synthesized compounds were examined for their antibacterial activity against Gram (+) bacteria, (ATCC 25923), (ATCC 51299), (ATCC 10876) and Gram (-) bacteria, (ATCC 10536), (ATCC 10145), (ATCC BAA-2146)and clinical isolates of Gram (+) Methicillin Resistant (MRSA) and Multi Drug Resistant . The Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) values by broth dilution method revealed that compound 2d exhibited significant antibacterial potential against and with MIC of 8 μg/mL, while other synthesized compounds had only moderate effects against all the tested species. The compound significantly inhibited the biofilm formation of the bacterial strains below its MIC. The selective cytotoxicity of Compound towards bacterial cells was evidenced on extended exposure of Human Embryonic Kidney-293 cell line to higher concentrations of the compound. Hence, the present study confirmed that compound can be a potential drug candidate for future development as an antibacterial drug.

摘要

本研究报道了在温和条件下,使用亚硝酸钠和叠氮化钠,由取代的2-氨基苯并噻唑合成2-叠氮基苯并噻唑。对所有合成的化合物针对革兰氏阳性菌(ATCC 25923、ATCC 51299、ATCC 10876)、革兰氏阴性菌(ATCC 10536、ATCC 10145、ATCC BAA - 2146)以及革兰氏阳性耐甲氧西林金黄色葡萄球菌(MRSA)和多重耐药菌的临床分离株进行了抗菌活性检测。通过肉汤稀释法测定的最低抑菌浓度(MIC)和最低杀菌浓度(MBC)值表明,化合物2d对[具体细菌名称1]和[具体细菌名称2]表现出显著的抗菌潜力,MIC为8μg/mL,而其他合成化合物对所有测试菌种仅具有中等效果。该化合物在低于其MIC时能显著抑制细菌菌株的生物膜形成。当人胚肾 - 293细胞系长时间暴露于较高浓度的该化合物时,证明了该化合物对细菌细胞具有选择性细胞毒性。因此,本研究证实该化合物可能是未来作为抗菌药物开发的潜在候选药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a56/10513370/e9fec4982499/FCHEM_fchem-2023-1264747_wc_sch1.jpg

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