Exploring the antimicrobial potential of novel 2-oxo-2-H-chromene conjugates with guanine, thiazole, and imidazole: Synthesis, characterization, and biological evaluation

Suman Lata , Ramandeep Kaur , Gurinder Singh , Divya Dhawal Bhandari , Vikrant Abbot
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Abstract

Five derived forms of 2-oxo-2-H-chromene clubbed guanine, thiazole and imidazoline derivatives 10 (iv), 11 (iv), and 12 (iv) were synthesized, characterized, and biologically tested for in vitro antimicrobial activity against two types of bacteria viz. Staphylococcus aureus (MTCC 87) and Escherichia coli (MTCC 40). The synthesized compounds demonstrated mild to moderate antibacterial activity against Escherichia coli and Staphylococcus aureus at all concentrations (100 μg/ml, 250 μg/ml, and 500 μg/ml) in comparison to standard drug ciprofloxacin. It was observed that the compounds 10i, 10v, 11i, 11v, 12i, 12ii, 12iv and 12v have noticeable activity at higher dose in comparison to standard drug. Zone of inhibition values indicated higher antimicrobial activity at 500 μg/ml against Escherichia coli and Staphylococcus aureus in case of imidazoline and thiazole clubbed coumarin derivatives in comparison to guanine derivatives. The guanine derivatives have been found to be potent at lower dose (100 μg/ml) in comparison to thiazole and imidazoline derivatives having negligible activity at 100 μg/ml. This suggests a differential efficacy profile among the synthesized compounds, with guanine derivatives showing promising activity at lower doses while thiazole and imidazole derivatives manifesting increased potency at higher concentrations. These findings underscore the potential of these novel compounds as antimicrobial agents, warranting further investigation into their mechanisms of action and therapeutic applications.

探索新型 2-氧代-2-H-色烯与鸟嘌呤、噻唑和咪唑共轭物的抗菌潜力:合成、表征和生物评估
合成了五种 2-氧代-2-H-色烯偶联鸟嘌呤、噻唑和咪唑啉衍生物 10 (i-v)、11 (i-v) 和 12 (i-v),并对其进行了表征和体外抗菌活性生物测试,测试对象为两种细菌,即金黄色葡萄球菌(MTCC 87)和大肠杆菌(MTCC 40)。与标准药物环丙沙星相比,合成的化合物在所有浓度(100 微克/毫升、250 微克/毫升和 500 微克/毫升)下对大肠杆菌和金黄色葡萄球菌都具有轻度到中度的抗菌活性。据观察,与标准药物相比,化合物 10i、10v、11i、11v、12i、12ii、12iv 和 12v 在较高剂量下具有明显的活性。与鸟嘌呤衍生物相比,咪唑啉和噻唑香豆素衍生物在 500 μg/ml 时对大肠杆菌和金黄色葡萄球菌具有更高的抗菌活性。与噻唑和咪唑类香豆素衍生物相比,鸟嘌呤衍生物在较低剂量(100 微克/毫升)时就具有较强的活性,而在 100 微克/毫升时活性微乎其微。这表明合成的化合物具有不同的药效特征,鸟嘌呤衍生物在低剂量时具有良好的活性,而噻唑和咪唑衍生物在高浓度时药效增强。这些发现强调了这些新型化合物作为抗菌剂的潜力,值得进一步研究其作用机制和治疗应用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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