Antibacterial Potential of Tetrahydrocarbazoles (THCZ): A Review

Q2 Pharmacology, Toxicology and Pharmaceutics

Current Bioactive Compounds Pub Date : 2024-02-06 DOI:10.2174/0115734072275884240125100455

Nitin Kumar, Shalini Sharma, Saurabh Agrawal, Vishesh Verma

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引用次数: 0

Abstract

Antibiotic resistance has become a major public threat across the globe associated with human health. Some bacterial and fungal infections produce bacterial resistance, such as methicillin- resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecium (VRE) and multidrug-resistant (MDR) species Acinetobacter baumannii etc. Tetrahydrocarbazoles (THCz) are a sub-class of indole alkaloids profoundly present in natural products and biologically active compounds and have displayed potential biological activities in literature. THCz exhibit potential antibacterial activities through major bacterial pathways like cell wall synthesis inhibition and DNA gyrase enzyme inhibition with DNA sliding clamp inhibitors and MreB inhibitors. These THCZ also showed significant in vitro antibacterial activities against bacterial-resistant species, such as MRSA, VRE and Acinetobacter baumannii (MDR) in literature. MTDL (Multi Target Direct ligand) approach has been significantly used for the design of THC motif-based antibacterial agents. In this review article, we collected literature on THCz as a potential antibacterial agent from 2014 to date. The review study of THC core-based derivatives found excellent in vitro antibacterial profiles and revealed that they can play a significant role in drug discovery and the development of new antibiotics against various infectious diseases.

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四氢咔唑（THCZ）的抗菌潜力：综述

抗生素耐药性已成为全球与人类健康相关的主要公共威胁。一些细菌和真菌感染会产生细菌耐药性，如耐甲氧西林金黄色葡萄球菌（MRSA）、耐万古霉素粪肠球菌（VRE）和耐多药（MDR）鲍曼不动杆菌（Acinetobacter baumannii）等。四氢咔唑（THCz）是吲哚生物碱的一个亚类，广泛存在于天然产物和生物活性化合物中，并在文献中显示出潜在的生物活性。THCz 通过细胞壁合成抑制和 DNA 回旋酶抑制（DNA 滑动钳抑制剂和 MreB 抑制剂）等主要细菌途径显示出潜在的抗菌活性。MTDL（多靶点直接配体）方法已被大量用于设计基于 THC 主题的抗菌剂。在这篇综述文章中，我们收集了 2014 年至今有关 THCz 作为潜在抗菌剂的文献。对基于 THC 核心的衍生物进行的综述研究发现，这些衍生物具有极佳的体外抗菌谱，并揭示了它们在药物发现和开发新型抗生素以防治各种感染性疾病方面可发挥重要作用。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Current Bioactive Compounds Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)

CiteScore

1.90

自引率

0.00%

发文量

112

期刊介绍： The journal aims to provide comprehensive review articles on new bioactive compounds with proven activities in various biological screenings and pharmacological models with a special emphasis on stereoeselective synthesis. The aim is to provide a valuable information source of bioactive compounds synthesized or isolated, which can be used for further development of pharmaceuticals by industry and academia. The journal should prove to be essential reading for pharmacologists, natural product chemists and medicinal chemists who wish to be kept informed and up-to-date with the most important developments on new bioactive compounds of natural or synthetic origin, including their stereoeselective synthesis.