Synthesized Phosphonium Compounds Demonstrate Resistant Modulatory and Antibiofilm Formation Activities against Some Pathogenic Bacteria

IF 16.4 1区 化学 Q1 CHEMISTRY, MULTIDISCIPLINARY
Cedric Dzidzor Kodjo Amengor, Cynthia Amaning Danquah, E. B. A. Adusei, F. K. Kekessie, Francis Ofosu-Koranteng, Paul Peprah, B. Harley, E. Orman, J. Adu, Yussif Saaka
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引用次数: 1

Abstract

A library of six compounds with new hybrids in a single molecule triazole ring attached to the phosphonium salts was synthesized. Click chemistry was, however, used to synthesize the 1-, 2-, and 3-triazole intermediates as a tether for the hybrid phosphonium salts. Their antibacterial activity against Gram-positive bacteria (Staphylococcus aureus and Enterococcus faecalis), Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa), and Mycobacterium smegmatis mc2155 was determined using the HT-SPOTi assay. Compound 2 showed the most effective antimicrobial activity as it inhibited the growth of Pseudomonas aeruginosa and Staphylococcus aureus at 0.0125 µg/mL and 31.25 µg/mL, respectively. From the FICI data, compounds 2ET-TOL (2) and RABYL-TOL (4) successfully modulated the activities of amoxicillin against Pseudomonas aeruginosa and Staphylococcus aureus. All the test compounds exhibited a concentration-dependent biofilm formation inhibition against S. aureus, except P-Z (compound 6). Compounds P-MEOXY (1) and 2ET-TOL (2) exhibited mild activity against P. aeruginosa with compound 4 showing antimycobacterial activity at 500 µg/mL.
合成的磷化合物对某些病原菌具有抗性调节和抗生物膜形成活性
合成了一个由六种新杂化化合物组成的库,这些化合物在单分子三唑环上与磷盐相连。然而,Click化学用于合成1-,2-和3-三唑中间体作为杂化磷盐的系链。采用HT-SPOTi法测定其对革兰氏阳性菌(金黄色葡萄球菌和粪肠球菌)、革兰氏阴性菌(大肠杆菌和铜绿假单胞菌)和耻垢分枝杆菌mc2155的抑菌活性。化合物2对铜绿假单胞菌和金黄色葡萄球菌的抑菌活性分别为0.0125µg/mL和31.25µg/mL,抑菌活性最强。根据FICI数据,化合物2ET-TOL(2)和RABYL-TOL(4)成功地调节了阿莫西林对铜绿假单胞菌和金黄色葡萄球菌的活性。除P-Z(化合物6)外,所有化合物对金黄色葡萄球菌均表现出浓度依赖性的生物膜形成抑制作用。化合物P-MEOXY(1)和2ET-TOL(2)对铜绿假单胞菌(P. aeruginosa)表现出轻微的抑制作用,化合物4在500µg/mL时表现出抑菌活性。
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来源期刊
Accounts of Chemical Research
Accounts of Chemical Research 化学-化学综合
CiteScore
31.40
自引率
1.10%
发文量
312
审稿时长
2 months
期刊介绍: Accounts of Chemical Research presents short, concise and critical articles offering easy-to-read overviews of basic research and applications in all areas of chemistry and biochemistry. These short reviews focus on research from the author’s own laboratory and are designed to teach the reader about a research project. In addition, Accounts of Chemical Research publishes commentaries that give an informed opinion on a current research problem. Special Issues online are devoted to a single topic of unusual activity and significance. Accounts of Chemical Research replaces the traditional article abstract with an article "Conspectus." These entries synopsize the research affording the reader a closer look at the content and significance of an article. Through this provision of a more detailed description of the article contents, the Conspectus enhances the article's discoverability by search engines and the exposure for the research.
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