N11修饰的四氢β-卡罗啉类似物的合成及其抗疟活性研究

IF 2.6 4区医学 Q3 CHEMISTRY, MEDICINAL

Medicinal Chemistry Research Pub Date : 2024-10-28 DOI:10.1007/s00044-024-03324-x

Deepak Kumar, Cherish Prashar, Vandana Vandana, Kailash C. Pandey, Dipti Vaya, Tejpal Singh Chundawat

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引用次数: 0

摘要

四氢β-羰基化合物是吲哚家族中重要的一类药用化合物。四氢β-卡泊啉在吲哚上的n -苄基化变化需要探索其药理活性。以2-（5-甲氧基- 1h -吲哚-3-酰基）-2-氧乙醛和2-（5-甲氧基- 1h -吲哚-3-酰基）乙二胺（n-烷基化）为原料，经Pictet-Spengler反应和LiCl/NaBH4酮还原，合成了17个n- 11-苄基- β-羰基衍生物，包括11个n-取代的和6个酮还原的β-羰基衍生物。研究了这些类似物对寄生虫3D7和C580Y菌株的抗疟活性。

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Synthesis of tetrahydro-β-carboline analogs with N11 modifications and study of their antimalarial activities

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Synthesis of tetrahydro-β-carboline analogs with N11 modifications and study of their antimalarial activities

Tetrahydro-β-carbolines are medicinal important class of compounds have their place in indole family. N-benzylation variations at indole of Tetrahydro-β-Carboline’s needs to explored of its pharmacological activities. Seventeen N-11-benzylic- β-carboline derivatives were synthesized from 2-(5-methoxy-1H-indol-3-yl)-2-oxoacetaldehyde and 2-(5-methoxy-1H-indol-3-yl)ethan-1-amine (N-alkylated) via Pictet–Spengler reaction and Keto reduction using LiCl/NaBH₄, including eleven N-substituted and six Keto reduced β-carboline derivatives. Antimalarial activities of these analogs were studied on 3D7 and C580Y parasite strains.

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来源期刊

Medicinal Chemistry Research 医学-医药化学

CiteScore

4.70

自引率

3.80%

发文量

162

审稿时长

5.0 months

期刊介绍： Medicinal Chemistry Research (MCRE) publishes papers on a wide range of topics, favoring research with significant, new, and up-to-date information. Although the journal has a demanding peer review process, MCRE still boasts rapid publication, due in part, to the length of the submissions. The journal publishes significant research on various topics, many of which emphasize the structure-activity relationships of molecular biology.