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季铵化稠合-β-咔啉作为抗耐甲氧西林金黄色葡萄球菌(MRSA)药物的合成及生物评价

Synthesis and Bio-Evaluation of Quaternized Fused-β-Carbolines as Anti-MRSA Agents.

作者信息

Vutla Adilakshmi, Saxena Deepanshi, Maitra Rahul, Chopra Sidharth, Batra Sanjay

机构信息

Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Sector 10, Jankipuram Extension, Lucknow, 226031, Uttar Pradesh, India.

Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, India.

出版信息

ChemMedChem. 2025 May 5;20(9):e202400955. doi: 10.1002/cmdc.202400955. Epub 2025 Feb 25.

DOI:10.1002/cmdc.202400955
PMID:39948749
Abstract

The drastic increase in the emergence of methicillin and vancomycin resistant S. aureus has resulted in almost negligible treatment options available to tackle these drug-resistant strains and therefore, search for newer antibiotics is essential. In this context, a new series of quaternized fused β-carbolines was synthesized and evaluated for its anti-bacterial potential. Several compounds from the series displayed potent anti-bacterial activity against Gram-positive bacteria including the drug-resistant strains with minimal cytotoxicity and promising bactericidal action.

摘要

耐甲氧西林和万古霉素金黄色葡萄球菌的出现急剧增加,导致应对这些耐药菌株的治疗选择几乎微乎其微,因此,寻找新型抗生素至关重要。在此背景下,合成了一系列新型季铵化稠合β-咔啉,并对其抗菌潜力进行了评估。该系列中的几种化合物对革兰氏阳性菌,包括耐药菌株,显示出强效抗菌活性,细胞毒性极小且具有良好的杀菌作用。

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