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4-(4-甲酰基-3-苯基-1H-吡唑-1-基)苯甲酸新型衍生物作为强效抗鲍曼不动杆菌药物的合成及抗菌研究

Synthesis and antimicrobial studies of novel derivatives of 4-(4-formyl-3-phenyl-1H-pyrazol-1-yl)benzoic acid as potent anti-Acinetobacter baumannii agents.

作者信息

Allison Devin, Delancey Evan, Ramey Hunter, Williams Conrad, Alsharif Zakeyah Ali, Al-Khattabi Hessa, Ontko Allyn, Gilmore David, Alam Mohammad A

机构信息

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

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

出版信息

Bioorg Med Chem Lett. 2017 Feb 1;27(3):387-392. doi: 10.1016/j.bmcl.2016.12.068. Epub 2016 Dec 29.

Abstract

Microbial resistance to antibiotics is a global concern. The World Health Organization (WHO) has identified antimicrobial resistance as one the three greatest threats for human beings in the 21st century. Without urgent and coordinated action, the world is moving toward a post-antibiotic era, in which normal infections or minor injuries may become fatal. In an effort to find new agents, we report the synthesis and antimicrobial activities of 40 novel 1,3-diphenyl pyrazole derivatives. These compounds have shown zones of growth inhibition up to 85mm against Acinetobacter baumannii. We tested the active compounds against this Gram-negative bacterium in minimum inhibitory concentration (MIC) tests and found activity with concentration as low as 4μg/mL.

摘要

微生物对抗生素的耐药性是一个全球关注的问题。世界卫生组织(WHO)已将抗菌药物耐药性确定为21世纪对人类的三大最大威胁之一。如果不采取紧急和协调一致的行动,世界正在走向一个后抗生素时代,在这个时代,正常感染或轻伤可能会致命。为了寻找新的药物,我们报告了40种新型1,3-二苯基吡唑衍生物的合成及其抗菌活性。这些化合物对鲍曼不动杆菌显示出高达85毫米的生长抑制圈。我们在最低抑菌浓度(MIC)试验中测试了这些活性化合物对这种革兰氏阴性菌的效果,发现浓度低至4μg/mL时仍有活性。

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