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螺-4H-吡喃衍生物对某些革兰氏阳性菌和革兰氏阴性菌的抗菌活性的合成与评价

Synthesis and Evaluation of the Antimicrobial Activity of Spiro-4H-pyran Derivatives on Some Gram Positive and Gram Negative Bacteria.

作者信息

Nazari Pardis, Bazi Aliyeh, Ayatollahi Seyed AbdulMajid, Dolati Hadi, Mahdavi Seyedeh Mahbobeh, Rafighdoost Laleh, Amirmostofian Marzieh

机构信息

Depatment of Pharmaceutical Biotechnology, School of Pharmacy, Zabol University of Medical Sciences, Zabol, Iran.

Phytochemistry Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.

出版信息

Iran J Pharm Res. 2017 Summer;16(3):943-952.

Abstract

Infections are one of the most important causes of death, disability and inappropriate conditions for millions of people around the world. Therefore, the development in prognosis, prevention and treatment of infectious diseases made a considerable progress in designing and synthesis of new antimicrobial drugs. Nowadays, due to the increase in microbial resistance, discovery of new compounds with broad spectrum effects is granted. 4H-pyran derivatives and spiro compounds are the most important fragments in some effective drugs with antimicrobial activity. Therefore, in this study, 6 compounds with spiro-4H-pyran core were synthesized and evaluated for their antimicrobial activity against four different bacterial species using microbroth dilution and disk diffusion methods. Minimum inhibitory concentration (MIC) has been measured for each compound and also for the standard antibiotic, gentamicin, and they were all compared together. According to our result, one of the spiropyran derivative (5d) containing both the indole and the cytosine ring, has been shown good antibacterial effects against standard and clinical isolates of and .

摘要

感染是全球数百万人死亡、残疾及身体不适的最重要原因之一。因此,在设计和合成新型抗菌药物方面,传染病预后、预防和治疗的发展取得了显著进展。如今,由于微生物耐药性增加,开发具有广谱效应的新化合物成为必然。4H-吡喃衍生物和螺环化合物是一些具有抗菌活性的有效药物中最重要的片段。因此,在本研究中,合成了6种具有螺-4H-吡喃核心的化合物,并采用微量肉汤稀释法和纸片扩散法评估了它们对四种不同细菌的抗菌活性。测定了每种化合物以及标准抗生素庆大霉素的最低抑菌浓度(MIC),并将它们进行了比较。根据我们的结果,一种同时含有吲哚环和胞嘧啶环的螺吡喃衍生物(5d)对标准菌株和临床分离株均显示出良好的抗菌效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d547/5610750/3df756c62500/ijpr-16-0943-g001.jpg

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