2-{[(2R,4R)-4-羧基-2-羟基吡咯烷-1-基]羰基}苯-1,5-二羧酸和2-氨基苯基苯-1,5-二羧酸类似物的合成及抗生素评价

A. Tukur, I. Bello, N. Koorbanally, J. Habila
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引用次数: 0

摘要

我们对新型抗生素的研究导致了新型二羧酸类似物的合成和生物学评价。该合成涉及不同取代的苯胺、苯胺、烷基胺和4-羟基- l-脯氨酸与氨基甲酰苯甲酸的亲核加成。抑菌区(ZOI)结果表明,z10对铜绿假单胞菌(32 mm)的抑菌活性最高,对星状假丝酵母(27 mm)和耐万古霉素肠球菌(27 mm)的抑菌活性最低,z7对耐甲氧西林金黄色葡萄球菌(MRSA)的抑菌活性最低(22 mm)。最小抑制浓度(MIC)测定表明,z10在低浓度为6.25 μg/mL时抑制被试微生物的生长,而z9和z12在12.5 μg/mL时抑制大部分微生物的生长,MIC最小。最小杀菌/杀真菌浓度(MBC/MFC)结果显示,除念珠菌和耐万古霉素肠球菌(VRE)的MBC/MFC为25 μg/mL外,z10对试验微生物的杀菌/杀真菌效果最高,浓度为12.5 μg/mL。这项研究的结果揭示了目标化合物(z1 - 3,5,7 - 12)在寻找新的抗菌药物方面的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Syntheses and Antibiotic Evaluation of 2-{[(2R,4R)-4-Carboxy-2-hydroxypyrrolidin-1-yl]carbonyl}benzene-1,5-dicarboxylic Acids and 2-Carbamoylbenzene-1,5-dicarboxylic Acid Analogues
Our search for new antibiotics led to the syntheses and biological evaluation of new classes of dicarboxylic acid analogues. The syntheses involve nucleophilic addition of different substituted benzylamine, aniline, alkylamine, and 4-hydroxyl-L-proline with carbamoylbenzoic acid. The results of the antimicrobial activity as indicated by the zone of inhibition (ZOI) showed that Z 10 is the most active against Pseudomonas aeruginosa (32 mm) and least active against Candida stellatoidea (27 mm) and Vancomycin Resistant Enterococci (VRE) (27 mm), while Z 7 shows the least zone of inhibition (22 mm) against Methicillin Resistant Staphylococcus aureus (MRSA). The minimum inhibition concentration (MIC) determination reveals that Z 10 inhibits the growth of tested microbes at a low concentration of 6.25 μg/mL, while Z 9 and Z 12 inhibits the growth of most microbes at a concentration of 12.5 μg/mL, recording the least MIC. The Minimum Bactericidal/Fungicidal Concentration (MBC/MFC) results revealed that Z 10 has the highest bactericidal/fungicidal effect on the test microbes, at a concentration of 12.5 μg/mL, with the exception of Candida stellatoidea and Vancomycin Resistant Enterococci (VRE) with MBC/MFC of 25 μg/mL. The result of this investigation reveals the potential of the target compounds (Z 1–3,5,7–12) in the search for new antimicrobial agents.
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期刊介绍: International Journal of Medicinal Chemistry is a peer-reviewed, Open Access journal that publishes original research articles as well as review articles in all areas of chemistry associated with drug discovery, design, and synthesis. International Journal of Medicinal Chemistry is a peer-reviewed, Open Access journal that publishes original research articles as well as review articles in all areas of chemistry associated with drug discovery, design, and synthesis.
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