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4,4'-(4-甲酰基-1-吡唑-1,3-二基)二苯甲酸衍生物的合成作为用于潜在治疗感染的窄谱抗生素

Synthesis of 4,4'-(4-Formyl-1-pyrazole-1,3-diyl)dibenzoic Acid Derivatives as Narrow Spectrum Antibiotics for the Potential Treatment of Infections.

作者信息

Delancey Evan, Allison Devin, Kc Hansa Raj, Gilmore David F, Fite Todd, Basnakian Alexei G, Alam Mohammad A

机构信息

Department of Chemistry and Physics, College of Science and Mathematics, Arkansas State University, Jonesboro, AR 72467, USA.

Department of Biological Sciences, College of Science and Mathematics, Arkansas State University, Jonesboro, AR 72467, USA.

出版信息

Antibiotics (Basel). 2020 Sep 28;9(10):650. doi: 10.3390/antibiotics9100650.

DOI:10.3390/antibiotics9100650
PMID:32998384
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7601628/
Abstract

has emerged as one of the most lethal drug-resistant bacteria in recent years. We report the synthesis and antimicrobial studies of 25 new pyrazole-derived hydrazones. Some of these molecules are potent and specific inhibitors of strains with a minimum inhibitory concentration (MIC) value as low as 0.78 µg/mL. These compounds are non-toxic to mammalian cell lines in in vitro studies. Furthermore, one of the potent molecules has been studied for possible in vivo toxicity in the mouse model and found to be non-toxic based on the effect on 14 physiological blood markers of organ injury.

摘要

近年来已成为最致命的耐药菌之一。我们报告了25种新型吡唑衍生腙的合成及抗菌研究。其中一些分子是菌株的强效特异性抑制剂,最低抑菌浓度(MIC)值低至0.78 µg/mL。在体外研究中,这些化合物对哺乳动物细胞系无毒。此外,已对其中一种强效分子在小鼠模型中进行了体内毒性研究,基于对14种器官损伤生理血液标志物的影响,发现其无毒。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5470/7601628/b1cbca62f237/antibiotics-09-00650-g002a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5470/7601628/c02b106c1de8/antibiotics-09-00650-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5470/7601628/85bab23e8616/antibiotics-09-00650-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5470/7601628/b1cbca62f237/antibiotics-09-00650-g002a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5470/7601628/c02b106c1de8/antibiotics-09-00650-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5470/7601628/85bab23e8616/antibiotics-09-00650-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5470/7601628/b1cbca62f237/antibiotics-09-00650-g002a.jpg

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