Dhameliya Tejas M, Vekariya Drashtiben D, Bhatt Pooja R, Kachroo Tarun, Virani Kumkum D, Patel Khushi R, Bhatt Shelly, Dholakia Sandip P
Department of Pharmaceutical Chemistry and Quality Assurance, L. M. College of Pharmacy, Navrangpura, Ahmedabad, 380 009, Gujarat, India.
Present Address: Department of Pharmaceutical Chemistry, Institute of Pharmacy, Nirma University, Ahmedabad, 382481, Gujarat, India.
Mol Divers. 2025 Feb;29(1):871-897. doi: 10.1007/s11030-024-10842-8. Epub 2024 May 6.
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.
根据世界卫生组织的报告，由恶性疟原虫引起的疟疾已被确认为导致多名患者死亡的主要传染病之一。为了寻找有效的抗疟疾治疗药物，几个研究小组已开始致力于设计和开发新型杂环化合物作为抗疟剂。杂环已被公认为具有不同类型重要药用活性的药效基团特征。在所有这些杂环化合物中，含氮氮杂环因其广泛的治疗窗而不容小觑。在氮杂环中，吲哚和稠合吲哚，如马里诺喹啉、异隐色胺及其区域异构体、蔓生胺、新隐色林和吲哚酮，已被确认为对恶性疟原虫有活性的抗疟剂。目前的工作展示了通过环缩合、费歇尔吲哚合成等方法合成抗疟吲哚和稠合吲哚的尝试，并简要讨论了构效关系、体外或体内研究，以满足这些药物化学家对将其设计和开发为潜在抗疟剂的更广泛兴趣。
