Synthetic account on indoles and their analogues as potential anti-plasmodial agents.

IF 3.9 2区 化学 Q2 CHEMISTRY, APPLIED
Molecular Diversity Pub Date : 2025-02-01 Epub Date: 2024-05-06 DOI:10.1007/s11030-024-10842-8
Tejas M Dhameliya, Drashtiben D Vekariya, Pooja R Bhatt, Tarun Kachroo, Kumkum D Virani, Khushi R Patel, Shelly Bhatt, Sandip P Dholakia
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Abstract

Malaria caused by P. falciparum, has been recognized as one of the major infectious diseases causing the death of several patients as per the reports from the World Health Organization. In search of effective therapeutic agents against malaria, several research groups have started working on the design and development of novel heterocycles as anti-malarial agents. Heterocycles have been recognized as the pharmacophoric features for the different types of medicinally important activities. Among all these heterocycles, nitrogen containing aza-heterocycles should not be underestimated owing to their wide therapeutic window. Amongst the aza-heterocycles, indoles and fused indoles such as marinoquinolines, isocryptolepines and their regioisomers, manzamines, neocryptolenines, and indolones have been recognized as anti-malarial agents active against P. falciparum. The present work unleashes the synthetic attempts of anti-malarial indoles and fused indoles through cyclocondensation, Fischer-indole synthesis, etc. along with the brief discussions on structure-activity relationships, in vitro or in vivo studies for the broader interest of these medicinal chemists, working on their design and development as potential anti-malarial agents.

Abstract Image

关于吲哚及其类似物作为潜在抗疟药物的合成研究。
根据世界卫生组织的报告,由恶性疟原虫引起的疟疾已被认为是导致数名患者死亡的主要传染病之一。为了寻找有效的疟疾治疗药物,一些研究小组开始致力于设计和开发新型杂环作为抗疟疾药物。人们已经认识到,杂环具有不同类型的重要药用活性的药效特征。在所有这些杂环中,含氮杂环因其广泛的治疗窗口而不容小觑。在偶氮杂环中,吲哚和融合吲哚,如 marinoquinolines、isocryptolepines 及其 Regioisomers、manzamines、neocryptolenines 和 indolones 已被认为是对恶性疟原虫有活性的抗疟药物。本研究通过环缩合、费舍尔-吲哚合成等方法,对抗疟吲哚和融合吲哚进行了合成尝试,并简要讨论了它们的结构-活性关系、体外或体内研究,以引起这些药物化学家的广泛兴趣,并将它们设计和开发为潜在的抗疟药物。
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来源期刊
Molecular Diversity
Molecular Diversity 化学-化学综合
CiteScore
7.30
自引率
7.90%
发文量
219
审稿时长
2.7 months
期刊介绍: Molecular Diversity is a new publication forum for the rapid publication of refereed papers dedicated to describing the development, application and theory of molecular diversity and combinatorial chemistry in basic and applied research and drug discovery. The journal publishes both short and full papers, perspectives, news and reviews dealing with all aspects of the generation of molecular diversity, application of diversity for screening against alternative targets of all types (biological, biophysical, technological), analysis of results obtained and their application in various scientific disciplines/approaches including: combinatorial chemistry and parallel synthesis; small molecule libraries; microwave synthesis; flow synthesis; fluorous synthesis; diversity oriented synthesis (DOS); nanoreactors; click chemistry; multiplex technologies; fragment- and ligand-based design; structure/function/SAR; computational chemistry and molecular design; chemoinformatics; screening techniques and screening interfaces; analytical and purification methods; robotics, automation and miniaturization; targeted libraries; display libraries; peptides and peptoids; proteins; oligonucleotides; carbohydrates; natural diversity; new methods of library formulation and deconvolution; directed evolution, origin of life and recombination; search techniques, landscapes, random chemistry and more;
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