4-[3-(3-氟苯基)-4-甲酰基-1-吡唑-1-基]苯甲酸和4-[3-(4-氟苯基)-4-甲酰基-1-吡唑-1-基]苯甲酸作为耐药细菌有效生长抑制剂的合成及抗菌研究
Synthesis and Antimicrobial Studies of 4-[3-(3-Fluorophenyl)-4-formyl-1-pyrazol-1-yl]benzoic Acid and 4-[3-(4-Fluorophenyl)-4-formyl-1-pyrazol-1-yl]benzoic Acid as Potent Growth Inhibitors of Drug-Resistant Bacteria.
作者信息
Whitt Jedidiah, Duke Cameron, Ali Mohamad Akbar, Chambers Steven A, Khan Md Mahbub Kabir, Gilmore David, Alam Mohammad A
机构信息
Department of Chemistry and Physics, College of Science and Mathematics and Department of Biological Sciences, College of Science and Mathematics, Arkansas State University, Jonesboro, Arkansas 72467, United States.
Department of Chemistry, College of Science, King Faisal University, Al-Ahsa 31982, Saudi Arabia.
出版信息
ACS Omega. 2019 Aug 21;4(10):14284-14293. doi: 10.1021/acsomega.9b01967. eCollection 2019 Sep 3.
Microbial resistance to antibiotics is an urgent and worldwide concern. Several pyrazole-derived hydrazones were synthesized by using benign reaction conditions. Several of these molecules are potent growth inhibitors of drug-resistant strains of and with minimum inhibitory concentration values as low as 0.39 μg/mL. Furthermore, these molecules are nontoxic to human cells at high concentrations. Some of these molecules were tested for their ability to disrupt the bacterial membrane by using the SYTO-9/propidium iodide (BacLight) assay.
微生物对抗生素的耐药性是一个紧迫且全球关注的问题。通过使用温和的反应条件合成了几种吡唑衍生的腙。其中几种分子是耐药菌株的强效生长抑制剂，最低抑菌浓度值低至0.39μg/mL。此外，这些分子在高浓度下对人类细胞无毒。其中一些分子通过使用SYTO-9/碘化丙啶（BacLight）检测法测试了它们破坏细菌膜的能力。
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