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喹啉骨架的抗菌和抗真菌活性的最新进展。

Recent update on antibacterial and antifungal activity of quinoline scaffolds.

作者信息

Dorababu Atukuri

机构信息

Department of Chemistry, SRMPP Govt. First Grade College, Huvinahadagali, Karnataka, India.

出版信息

Arch Pharm (Weinheim). 2021 Mar;354(3):e2000232. doi: 10.1002/ardp.202000232. Epub 2020 Nov 19.

Abstract

Although most of the heterocycles have been reported to possess a significant pharmacological activity, only a few of them, namely quinoline derivatives, have exhibited the finest biological activities. Despite the few medicinal properties of the plain quinoline molecule, its derivatives exhibit diverse pharmacological properties such as anticancer, anti-inflammatory, antibacterial, antiviral, antifungal, antiprotozoal activities, and so on. The potential antimicrobial properties of the quinoline derivatives are evident from the decades of research on these derivatives. Owing to limitations like drug resistance, high cost, severe side effects, and less bioavailability of previously synthesized antimicrobial agents, these drugs have become obsolete in recent years. Hence, the design of more efficient antimicrobial drugs must be given topmost priority. A breakthrough in drug discovery is a must to prevent malevolent microbial diseases. Addressing all these issues, researchers have been continuously contributing to antimicrobial drug discovery. Herein, a short description of the pharmacology of antimicrobial agents such as antibacterials and antifungals synthesized recently is provided. The versatile derivatization of the quinoline moiety leading to significant antimicrobial potencies is discussed, considering the structure-activity relationship.

摘要

尽管据报道大多数杂环化合物都具有显著的药理活性,但其中只有少数,即喹啉衍生物,展现出了最佳的生物活性。尽管普通喹啉分子的药用特性较少,但其衍生物却表现出多种药理特性,如抗癌、抗炎、抗菌、抗病毒、抗真菌、抗原虫活性等等。喹啉衍生物潜在的抗菌特性从对这些衍生物数十年的研究中便可明显看出。由于诸如耐药性、高成本、严重副作用以及先前合成的抗菌剂生物利用度较低等限制,这些药物近年来已过时。因此,必须将设计更高效的抗菌药物置于最优先地位。药物发现方面的突破对于预防恶性微生物疾病而言必不可少。为解决所有这些问题,研究人员一直在为抗菌药物发现不断做出贡献。在此,提供了对近期合成的抗菌剂(如抗菌药和抗真菌药)药理学的简短描述。考虑到构效关系,讨论了导致显著抗菌效力的喹啉部分的多功能衍生化。

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