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并评估苯甲酰肼类化合物的抗活性。

and Evaluations of Anti- Activity of Benzohydrazones Compounds.

机构信息

Postgraduate Program in Health Sciences, State University of Maringá, Maringá, Brazil.

Postgraduate Program in Bioscience and Physiopathology, and State University of Maringá, Maringá, Brazil.

出版信息

Microb Drug Resist. 2021 Nov;27(11):1564-1577. doi: 10.1089/mdr.2020.0392. Epub 2021 Apr 28.

DOI:10.1089/mdr.2020.0392
PMID:33913749
Abstract

Tuberculosis is a disease caused by , with high mortality rates and an extended treatment that causes severe adverse effects, besides the emergence of resistant bacteria. Therefore, the search for new compounds with anti- activity has considerably increased in recent years. In this context, benzohydrazones are significant compounds that have antifungal and antibacterial action. This study aimed at evaluating the activity of 18 benzohydrazones against . Compounds' cytotoxicity, inhibition of efflux pumps, and absorption, distribution, metabolism, excretion, and toxicity (ADMET) assays were also performed. In general, the minimum inhibitory concentration values for the standard HRv strain ranged from 7.8 to 250 μg/mL, and some compounds were not toxic to any of the cells tested (IC ranged from 18.0 to 302.5 μg/mL). In addition, compounds () and () showed to be possible efflux pump inhibitors. In ADMET assays, all benzohydrazones had high gastrointestinal absorption. Most of the compounds were able to overcome the blood-brain barrier, and no compounds had irritant or tumorigenic effects. Compounds (), (), (), (), and () stood out for showing good activities, both and assays.

摘要

结核病是由引起的疾病,死亡率高,治疗时间长,会产生严重的不良反应,此外还出现了耐药细菌。因此,近年来人们对寻找具有抗活性的新化合物的兴趣大大增加。在这方面,苯并腙类化合物是具有抗真菌和抗菌作用的重要化合物。本研究旨在评估 18 种苯并腙类化合物对的活性。还进行了化合物的细胞毒性、外排泵抑制作用以及吸收、分布、代谢、排泄和毒性(ADMET)测定。一般来说,标准 HRv 菌株的最小抑菌浓度值范围为 7.8 至 250μg/mL,并且有些化合物对测试的任何细胞均无毒(IC 范围为 18.0 至 302.5μg/mL)。此外,化合物()和()显示出可能是外排泵抑制剂。在 ADMET 测定中,所有苯并腙类化合物都具有很高的胃肠道吸收性。大多数化合物能够克服血脑屏障,并且没有化合物具有刺激性或致癌作用。化合物()、()、()、()和()因其在和测定中均表现出良好的活性而脱颖而出。

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