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β-咔啉:一种具有潜在抗疟活性的天然优势骨架。

β-Carboline: a privileged scaffold from nature for potential antimalarial activity.

作者信息

Punmiya Amisha, Pandey Alka Raj, Vora Amisha

机构信息

Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's Narsee Monjee Institute of Management Studies (NMIMS) Deemed-to-be University V. L. Mehta Road, Vile Parle (West) Mumbai-400056 Maharashtra India

出版信息

RSC Med Chem. 2025 Aug 27. doi: 10.1039/d5md00299k.

Abstract

Malaria is one of the most prevalent infectious diseases in the world. Despite the implementation of malaria prophylaxis by the WHO, the mortality rate has been rising. Owing to the development of resistance to presently prescribed antimalarial medication regimes in humans and insecticides in malaria vectors, the prevention and treatment of these illnesses are severely hindered. β-Carbolines are a class of naturally occurring alkaloids that have garnered attention because of their unique structures and diverse biological activities. This review consolidates various methods for synthesizing diverse β-carbolines and highlights their potential as antimalarial agents, emphasizing the molecular targets of . Based on various research findings, we underscore the potential of β-carbolines to overcome therapeutic challenges and develop effective antimalarials. This review also highlights the structure-activity relationships (SARs) of various β-carboline derivatives to enhance their antimalarial efficacy. With thorough compilation of recent advancements, this review aims to inform and inspire further research and innovation in the quest to combat malaria.

摘要

疟疾是世界上最普遍的传染病之一。尽管世界卫生组织实施了疟疾预防措施,但死亡率仍在上升。由于人类对目前规定的抗疟药物治疗方案以及疟疾病媒对杀虫剂产生了耐药性,这些疾病的预防和治疗受到严重阻碍。β-咔啉是一类天然存在的生物碱,因其独特的结构和多样的生物活性而受到关注。本综述综合了合成各种β-咔啉的多种方法,并强调了它们作为抗疟剂的潜力,重点介绍了其分子靶点。基于各种研究结果,我们强调β-咔啉克服治疗挑战和开发有效抗疟药物的潜力。本综述还突出了各种β-咔啉衍生物的构效关系,以提高其抗疟疗效。通过全面汇编近期进展,本综述旨在为抗击疟疾的进一步研究和创新提供信息并激发灵感。

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