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取代的 4-氯-3-硝基苯基硫脲衍生物:抗菌和细胞毒性研究。

Disubstituted 4-Chloro-3-nitrophenylthiourea Derivatives: Antimicrobial and Cytotoxic Studies.

机构信息

Department of Biochemistry, Medical University, 02-097 Warszawa, Poland.

Department of Biomedical Sciences, Section of Microbiology and Virology, University of Cagliary, Cittadella Universitaria, 09042 Monserrato, Italy.

出版信息

Molecules. 2018 Sep 21;23(10):2428. doi: 10.3390/molecules23102428.

DOI:10.3390/molecules23102428
PMID:30248936
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6222614/
Abstract

4-Chloro-3-nitrophenylthioureas ⁻ were synthesized and tested for their antimicrobial and cytotoxic activities. Compounds exhibited high to moderate antistaphylococcal activity against both standard and clinical strains (MIC values 2⁻64 μg/mL). Among them derivatives with electron-donating alkyl substituents at the phenyl ring were the most promising. Moreover, compounds ⁻ and ⁻ were cytotoxic against MT-4 cells and various other cell lines derived from human hematological tumors (CC ≤ 10 μM). The influence of derivatives , and on viability, mortality and the growth rate of immortalized human keratinocytes (HaCaT) was observed.

摘要

4-氯-3-硝基苯基硫脲被合成并测试了其抗菌和细胞毒性活性。化合物对标准和临床分离株均表现出高至中度的抗葡萄球菌活性(MIC 值为 2⁻64 μg/mL)。其中,苯环上带有供电子烷基取代基的衍生物最有前景。此外,化合物 ⁻ 和 ⁻ 对 MT-4 细胞和源自人血液肿瘤的各种其他细胞系具有细胞毒性(CC ≤ 10 μM)。观察了衍生物 ⁻、 ⁻ 和 ⁻ 对永生化人角质形成细胞(HaCaT)活力、死亡率和增长率的影响。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/23ab/6222614/1a9a31b7bcb3/molecules-23-02428-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/23ab/6222614/d324b80e89aa/molecules-23-02428-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/23ab/6222614/0efa3f3577bf/molecules-23-02428-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/23ab/6222614/1604845d1900/molecules-23-02428-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/23ab/6222614/979561e34a90/molecules-23-02428-g003a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/23ab/6222614/1a9a31b7bcb3/molecules-23-02428-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/23ab/6222614/d324b80e89aa/molecules-23-02428-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/23ab/6222614/0efa3f3577bf/molecules-23-02428-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/23ab/6222614/1604845d1900/molecules-23-02428-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/23ab/6222614/979561e34a90/molecules-23-02428-g003a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/23ab/6222614/1a9a31b7bcb3/molecules-23-02428-g004.jpg

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