新合成烟酰胺的合成与抗菌活性。

IF 4.9 3区 医学 Q1 PHARMACOLOGY & PHARMACY
Bojana Anić Marković, Aleksandar Marinković, Jelena Antić Stanković, Stefan Mijatović, Ilija Cvijetić, Milena Simić, Irena Arandjelović
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引用次数: 0

摘要

抗氧化剂是一种很有前景的化合物,对耐药性病原体具有抗菌活性,尤其是与传统抗菌剂结合使用时。我们的研究旨在确定由烟酸和硫代酰肼合成的烟酰胺的结构特征,并评估其抗菌和抗真菌活性。研究人员利用带有羟基取代基的单硫代羧基肼以及具有抗菌活性的喹诺酮环、酚环和吡啶环合成了七种烟酸酰肼(NC 1-7)。根据 EUCAST 2024 准则,采用肉汤微稀释法测试了浓度为 0.001 至 1 mM 的 NC 1-7 对金黄色葡萄球菌(ATCC 6538)、粪肠球菌(ATCC 29212)、铜绿假单胞菌(ATCC 27853)、肺炎克雷伯菌(NCIMB 9111)和白色念珠菌(ATCC 24433)的体外抗菌活性。根据光密度计算微生物存活率,并使用 PharmMapper 数据库确定潜在的分子靶标。结果表明,铜绿假单胞菌对化合物的敏感性最高,而白僵菌的敏感性最低。NC 3 在 0.016 mM 的浓度下能明显抑制铜绿假单胞菌和肺炎双球菌的生长,而对金黄色葡萄球菌、粪大肠杆菌和白僵菌则需要更高的浓度。NC 5 在 0.03 毫摩尔时对革兰氏阳性菌最有效。只有 NC 4 能在 1 毫摩尔以下完全抑制白僵菌。NC 3 是抑制 50% 生长的最低浓度(0.016-0.064 mM),它对特定的 AMR 相关蛋白(博来霉素抗性蛋白、HTH 型转录调节因子 QacR 和链霉毒素 A 乙酰转移酶)显示出良好的抗菌潜力,表明这类化合物可以增强或恢复已有抗生素的活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis and Antimicrobial Activity of Newly Synthesized Nicotinamides.

Antioxidants are promising compounds with antimicrobial activity against drug-resistant pathogens, especially when combined with conventional antimicrobials. Our study aimed to characterize the structure of nicotinamides synthesized from nicotinic acid and thiocarbohydrazones and to evaluate their antibacterial and antifungal activity. Seven nicotinic acid hydrazides (NC 1-7) were synthesized using mono-thiocarbohydrazones with hydroxyl group substituents, along with quinolone, phenolic, and pyridine rings known for their antimicrobial activity. The in vitro antimicrobial activity of NC 1-7, at concentrations ranging from 0.001 to 1 mM, was tested against Staphylococcus aureus (ATCC 6538), Enterococcus faecalis (ATCC 29212), Pseudomonas aeruginosa (ATCC 27853), Klebsiella pneumoniae (NCIMB 9111), and Candida albicans (ATCC 24433) using the broth microdilution method per EUCAST 2024 guidelines. Microorganism survival percentages were calculated based on optical density, and target fishing using the PharmMapper database identified potential molecular targets. The results showed that P. aeruginosa was most susceptible to the compounds, while C. albicans was the least susceptible. NC 3 significantly inhibited P. aeruginosa and K. pneumoniae growth at 0.016 mM, while higher concentrations were required for S. aureus, E. faecalis, and C. albicans. NC 5 was most effective against gram-positive bacteria at 0.03 mM. Only NC 4 completely inhibited C. albicans below 1 mM. NC 3, with the lowest concentration for 50% growth inhibition (0.016-0.064 mM), showed promising antibacterial potential against specific AMR-related proteins (bleomycin resistance protein, HTH-type transcriptional regulator QacR, and streptogramin A acetyltransferase), suggesting that this class of compounds could enhance or restore the activity of established antibiotics.

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来源期刊
Pharmaceutics
Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
7.90
自引率
11.10%
发文量
2379
审稿时长
16.41 days
期刊介绍: Pharmaceutics (ISSN 1999-4923) is an open access journal which provides an advanced forum for the science and technology of pharmaceutics and biopharmaceutics. It publishes reviews, regular research papers, communications,  and short notes. Covered topics include pharmacokinetics, toxicokinetics, pharmacodynamics, pharmacogenetics and pharmacogenomics, and pharmaceutical formulation. Our aim is to encourage scientists to publish their experimental and theoretical details in as much detail as possible. There is no restriction on the length of the papers. The full experimental details must be provided so that the results can be reproduced.
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