新千年5-氧-咪唑类药物的有效抗菌谱

Roshan D. Nasare, M. Idrees, Satish S. Kola, Rajendra S. Dongre
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摘要

制药和治疗行业迫使化学家们寻找/发现具有特定生物活性和先天特征意义的新型抗菌杂环化合物。本章总结了新千年来5-氧咪唑类药物对革兰氏阳性和革兰氏阴性菌(苏云金芽胞杆菌、金黄色葡萄球菌、大肠杆菌和产气杆菌)的抗菌作用。5-(H/Br苯并呋喃-2-基)-1-苯基1h -吡唑-3碳酰肼与4-(芳基)-2苯基苯并唑-5(4H)- 1在醋酸中高温缩合得到产物5-(H/Br苯并呋喃-2-基)- n(4-芳基-5-氧-2-苯基-4,5-二氢咪唑-1-基)-1-苯基1h -吡唑-3羧酰胺。不同的底物,如4-(芳基)-2-苯氧氯唑-5(4H)- 1,允许与苯甲醛马尿酸反应生成5-氧基咪唑/ 5-氧基4,5-二氢咪唑。通过元素分析、FT-IR、H-NMR和质谱等技术对合成的5-氧-咪唑啉进行了表征。测定了所有5-氧基咪唑啉在不同浓度下对所述菌株的体外固有抗菌活性,并与标准氯霉素进行了比较。浓度为125 μg/mL的5-氧咪唑啉(3a和3c)对革兰氏阳性菌苏云金芽孢杆菌有良好的抑菌效果,而其他不同浓度的衍生物对革兰氏阳性菌金黄色葡萄球菌和苏云金芽孢杆菌均有中等抑菌活性。革兰氏阴性菌如大肠杆菌和产气大肠杆菌在较高浓度(1000、500和125 μg/mL)下测试,发现有良好至中等的抗菌活性。试验产物对125、61和31 μg/mL的产气荚膜无活性,对conc也无活性。31 μg/mL抗大肠杆菌。
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Potent Antibacterial Profile of 5-Oxo-Imidazolines in the New Millennium
Pharmaceutics and therapeutics industries enforced chemists to seek/discover antibacterial novel heterocycles owing specific bioactivity and innate characteristics significance. This chapter summarized potent antibacterial profile of 5-oxoimidazolines in the new millennium as an antibacterial against Gram-positive and Gram-negative bacteria viz. B. thuringiensis, S. aureus, E. coli, and E. aerogenes is presented in this chapter. 5-(H/Br benzofuran-2-yl)-1-phenyl 1H-pyrazole-3carbohydrazides are condensed with 4-(arylidene)-2 phenyloxazol-5(4H)-one in acetic acid at elevated temperature to yield product 5-(H/Br benzofuran-2-yl)-N(4-arylidene-5-oxo-2-phenyl-4,5-dihydroimidazol-1-yl)-1-phenyl-1H-pyrazole-3carboxamides. Different substrates like 4-(arylidene)-2-phenyloxazol-5(4H)-one allowed to react with benzaldehyde hippuric acid to yield 5-oxo-imidazolines/ 5-oxo-4,5-dihydroimidazole. All synthesized 5-oxo-imidazolines were characterized via elemental analysis and FT-IR, H-NMR and mass spectra techniques. All 5-oxo-imidazolines assayed in vitro for inherent antimicrobial activity at different concentration against stated bacterial strains and compared with standard chloramphenicol. 5-Oxo-imidazolines (3a and 3c) with 125 μg/mL concentration showed excellent antibacterial profile against Gram-positive bacteria, B. thuringiensis, while other derivatives at different concentrations showed moderate antibacterial activity against Gram-positive bacteria, S. aureus and B. thuringiensis. Gram-negative bacteria like E. coli and E. aerogenes are tested at higher concentration (1000, 500, and 125 μg/mL) and found good-to-moderate antibacterial activity. Tested products found non-active against E. aerogenes for 125, 61, and 31 μg/mL concentration also inactive at conc. 31 μg/mL against E. coli.
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