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2
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3
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Molecules. 2019 May 29;24(11):2051. doi: 10.3390/molecules24112051.
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Novel pyrazoles as potent growth inhibitors of staphylococci, enterococci and bacteria.新型吡唑类化合物可强效抑制葡萄球菌、肠球菌和其他细菌的生长。
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Update on antimicrobial susceptibility rates among gram-negative and gram-positive organisms in the United States: results from the Tigecycline Evaluation and Surveillance Trial (TEST) 2005 to 2007.美国革兰氏阴性菌和革兰氏阳性菌的抗菌药敏率最新情况:2005年至2007年替加环素评估与监测试验(TEST)结果
Clin Ther. 2008 Nov;30(11):2040-50. doi: 10.1016/j.clinthera.2008.11.006.
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Novel naphthalimide nitroimidazoles as multitargeting antibacterial agents against resistant Acinetobacter baumannii.新型萘酰亚胺硝咪唑类化合物作为抗耐药鲍曼不动杆菌的多靶抗菌剂。
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Synthesis, antitubercular and antimicrobial evaluation of 3-(4-chlorophenyl)-4-substituted pyrazole derivatives.合成、抗结核和抗菌评估 3-(4-氯苯基)-4-取代吡唑衍生物。
Bioorg Med Chem Lett. 2012 Aug 1;22(15):5129-33. doi: 10.1016/j.bmcl.2012.05.063. Epub 2012 May 24.
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Thiophene and benzodioxole appended thiazolyl-pyrazoline compounds: Microwave assisted synthesis, antimicrobial and molecular docking studies.噻吩和苯并二恶唑连接的噻唑基吡唑啉化合物:微波辅助合成、抗菌及分子对接研究
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Development of naphthalimide hydrazide derivatives as potent antibacterial agents against carbapenem-resistant .萘二甲酰亚胺酰肼衍生物作为抗碳青霉烯耐药菌的强效抗菌剂的研发
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Enhancement by pyrazolones of colistin efficacy against mcr-1-expressing E. coli: an in silico and in vitro investigation.吡唑酮类化合物增强多黏菌素对表达 mcr-1 的大肠杆菌的疗效:体外和体内研究。
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Development of 4-[4-(Anilinomethyl)-3-phenyl-pyrazol-1-yl] Benzoic Acid Derivatives as Potent Anti-Staphylococci and Anti-Enterococci Agents.4-[4-(苯胺甲基)-3-苯基-吡唑-1-基]苯甲酸衍生物作为强效抗葡萄球菌和抗肠球菌药物的研发
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Novel pyrazoles as potent growth inhibitors of staphylococci, enterococci and bacteria.新型吡唑类化合物可强效抑制葡萄球菌、肠球菌和其他细菌的生长。
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本文引用的文献

1
Metronidazole containing pyrazole derivatives potently inhibit tyrosyl-tRNA synthetase: design, synthesis, and biological evaluation.含吡唑衍生物的甲硝唑可有效抑制酪氨酰 - tRNA合成酶:设计、合成及生物学评价
Chem Biol Drug Des. 2016 Oct;88(4):592-8. doi: 10.1111/cbdd.12793. Epub 2016 Jun 24.
2
The therapeutic voyage of pyrazole and its analogs: A review.吡唑及其类似物的治疗之旅:综述
Eur J Med Chem. 2016 Sep 14;120:170-201. doi: 10.1016/j.ejmech.2016.04.077. Epub 2016 May 10.
3
Discovery of IWP-051, a Novel Orally Bioavailable sGC Stimulator with Once-Daily Dosing Potential in Humans.IWP-051的发现,一种新型口服生物可利用的可溶性鸟苷酸环化酶(sGC)刺激剂,具有在人类中每日一次给药的潜力。
ACS Med Chem Lett. 2016 Feb 24;7(5):465-9. doi: 10.1021/acsmedchemlett.5b00479. eCollection 2016 May 12.
4
Novel pyrazole derivatives with oxa/thiadiazolyl, pyrazolyl moieties and pyrazolo[4,3-d]-pyrimidine derivatives as potential antimicrobial and anticancer agents.具有恶二唑基/噻二唑基、吡唑基部分的新型吡唑衍生物以及吡唑并[4,3-d]嘧啶衍生物作为潜在的抗菌和抗癌药物。
Bioorg Med Chem Lett. 2016 May 15;26(10):2428-2433. doi: 10.1016/j.bmcl.2016.03.117. Epub 2016 Apr 2.
5
Pyrazole antagonists of the CB1 receptor with reduced brain penetration.脑渗透性降低的CB1受体吡唑拮抗剂。
Bioorg Med Chem. 2016 Mar 1;24(5):1063-70. doi: 10.1016/j.bmc.2016.01.033. Epub 2016 Jan 18.
6
Structure-activity relationship of indoloquinoline analogs anti-MRSA.吲哚喹啉类似物抗耐甲氧西林金黄色葡萄球菌的构效关系
Bioorg Med Chem Lett. 2015 Dec 1;25(23):5551-4. doi: 10.1016/j.bmcl.2015.10.058. Epub 2015 Oct 21.
7
New INH-pyrazole analogs: Design, synthesis and evaluation of antitubercular and antibacterial activity.新型异烟肼-吡唑类似物:抗结核和抗菌活性的设计、合成与评价
Bioorg Med Chem Lett. 2015 Dec 1;25(23):5540-5. doi: 10.1016/j.bmcl.2015.10.057. Epub 2015 Oct 21.
8
ESKAPEing the labyrinth of antibacterial discovery.逃出抗菌药物发现的迷宫。
Nat Rev Drug Discov. 2015 Aug;14(8):529-42. doi: 10.1038/nrd4572. Epub 2015 Jul 3.
9
Recent progress on pyrazole scaffold-based antimycobacterial agents.基于吡唑骨架的抗分枝杆菌剂的最新进展。
Arch Pharm (Weinheim). 2015 May;348(5):299-314. doi: 10.1002/ardp.201400452. Epub 2015 Mar 27.
10
Recent advances in bioactive pyrazoles.生物活性吡唑的最新进展
Eur J Med Chem. 2015 Jun 5;97:786-815. doi: 10.1016/j.ejmech.2014.11.059. Epub 2014 Dec 5.

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.

DOI:10.1016/j.bmcl.2016.12.068
PMID:28065568
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5486227/
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。