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通过含氨基药物、氨基酸及其类似物缩合得到的新型磺胺类化合物的合成、表征及抗菌活性

Synthesis, characterization, and antibacterial activities of novel sulfonamides derived through condensation of amino group containing drugs, amino acids, and their analogs.

作者信息

Abdul Qadir Muhammad, Ahmed Mahmood, Iqbal Muhammad

机构信息

Institute of Chemistry, University of Punjab, Lahore 54590, Pakistan.

Department of Chemistry, Minhaj University, Lahore, Pakistan.

出版信息

Biomed Res Int. 2015;2015:938486. doi: 10.1155/2015/938486. Epub 2015 Feb 24.

DOI:10.1155/2015/938486
PMID:25802872
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4354722/
Abstract

Novel sulfonamides were developed and structures of the new products were confirmed by elemental and spectral analysis (FT-IR, ESI-MS, (1)HNMR, and (13)CNMR). In vitro, developed compounds were screened for their antibacterial activities against medically important gram (+) and gram (-) bacterial strains, namely, S. aureus, B. subtilis, E. coli, and K. pneumoniae. The antibacterial activities have been determined by measuring MIC values (μg/mL) and zone of inhibitions (mm). Among the tested compounds, it was found that compounds 5a and 9a have most potent activity against E. coli with zone of inhibition: 31 ± 0.12 mm (MIC: 7.81 μg/mL) and 30 ± 0.12 mm (MIC: 7.81 μg/mL), respectively, nearly as active as ciprofloxacin (zone of inhibition: 32 ± 0.12 mm). In contrast, all the compounds were totally inactive against the gram (+) B. subtilis.

摘要

开发了新型磺胺类药物,并通过元素分析和光谱分析(傅里叶变换红外光谱、电喷雾电离质谱、¹H核磁共振和¹³C核磁共振)确定了新产品的结构。在体外,对开发的化合物针对医学上重要的革兰氏阳性和革兰氏阴性细菌菌株,即金黄色葡萄球菌、枯草芽孢杆菌、大肠杆菌和肺炎克雷伯菌进行了抗菌活性筛选。通过测量最小抑菌浓度值(μg/mL)和抑菌圈(mm)来确定抗菌活性。在测试的化合物中,发现化合物5a和9a对大肠杆菌具有最强的活性,抑菌圈分别为:31±0.12 mm(最小抑菌浓度:7.81 μg/mL)和30±0.12 mm(最小抑菌浓度:7.81 μg/mL),几乎与环丙沙星活性相同(抑菌圈:32±0.12 mm)。相比之下,所有化合物对革兰氏阳性的枯草芽孢杆菌完全无活性。

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