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合成含磺胺甲嘧啶/磺胺胍的新型磺胺类似物及其生物活性。

Synthesis of novel sulfonamide analogs containing sulfamerazine/sulfaguanidine and their biological activities.

机构信息

a Chemistry Department .

b Biology Department , and.

出版信息

J Enzyme Inhib Med Chem. 2016 Dec;31(6):1005-10. doi: 10.3109/14756366.2015.1079183. Epub 2015 Aug 31.

DOI:10.3109/14756366.2015.1079183
PMID:26327456
Abstract

Sulfamerazine and sulfaguanidine are clenched with p-nitrobenzoyl chloride and the products obtained are reduced to NaxS in ethanol-water. Novel sulfonamides (6a-g and 9a-g) were synthesized by the reaction of these reduced products (4 and 8) with various sulfonyl chlorides (5a-g). The structures of these compounds were characterized using spectroscopic analysis (IR, (1)H-NMR, (13)C-NMR and HRMS) technique. Antimicrobial activity of sulfonamides (3, 4, 7, 8, 6a-g and 9a-g) was evaluated by the agar diffusion method. These compounds showed antimicrobial activity against tested microorganism strains (Gram-positive bacteria, clinic isolate and yeast and mold). Compounds 9d, 9e, 9a, 6d and 6e showed particularly antimicrobial activity against tested Gram-positive (Bacillus cereus and B. subtilis) and Gram-negative (Enterobacter aerogenes) bacteria.

摘要

磺胺脒和磺胺胍与对硝基苯甲酰氯紧握,所得产物在乙醇-水中还原为 NaxS。通过还原产物(4 和 8)与各种磺酰氯(5a-g)的反应,合成了新型磺胺类化合物(6a-g 和 9a-g)。这些化合物的结构通过光谱分析(IR、(1)H-NMR、(13)C-NMR 和 HRMS)技术进行了表征。通过琼脂扩散法评估了磺胺类化合物(3、4、7、8、6a-g 和 9a-g)的抗菌活性。这些化合物对测试的微生物菌株(革兰氏阳性菌、临床分离株和酵母和霉菌)表现出抗菌活性。化合物 9d、9e、9a、6d 和 6e 对测试的革兰氏阳性(蜡样芽孢杆菌和枯草芽孢杆菌)和革兰氏阴性(产气肠杆菌)细菌表现出特别的抗菌活性。

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