2-(2-氰基吡咯烷-1-基)-N-3-羟基金刚烷-1-基)乙酰胺(格列吡嗪)的合成和药理应用的当前趋势和未来方向

IF 2.6 4区 医学 Q3 CHEMISTRY, MEDICINAL Medicinal Chemistry Research Pub Date : 2024-06-11 DOI:10.1007/s00044-024-03218-y
Shaikh Yahya, Mohammad Usman Shaikh, Prathmesh Pramod Deshpande, Sangshetti Jaiprakash Navnath, Akram Choudhary, Nisha Sharma, Mohd Shafeeque, M. Shahar Yar
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引用次数: 0

摘要

二肽基肽酶 4(DPP-4)被称为 T 细胞抗原 CD26 酶,于 1966 年由 Hopsu-Havu 和 Glenner 发现。这种酶因其重要的功能而备受关注,例如:(1)导致胰岛素分解的增量素激素失活;(2)水解参与疼痛调节的阿片肽等。此外,DPP-4 还是多种细胞外和细胞内底物的载体蛋白和配体。寻找 DPP-4 抑制剂是治疗冠心病、心力衰竭、中风和糖尿病(DM)等多种疾病的新方法。过去几十年的研究结果表明,格列汀类药物(DPP-4 抑制剂)比传统降糖药物更有前途,因为前者可以每周单药治疗一次,也可以与其他降糖药物联合使用。考虑到 DPP-4 抑制剂的所有有利特性,本节选主要针对已获临床批准的口服格列汀类药物,重点介绍其传统、现代以及专利的中间体和最终产品开发方法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Current trends and future directions for the synthesis and pharmacological applications of 2-(2-cyanopyrrolidin-1-yl)-N-3-hydroxyadamantan-1-yl) acetamide (Gliptins)

Dipeptidyl peptidase 4 (DPP-4), well known as the T-cell antigen CD26 enzyme which, was discovered in the year of 1966 by Hopsu-Havu and Glenner. The enzyme gained considerable attention due to its vital functions, such as (1) deactivation of the incretin hormone, which is responsible for insulin catabolism, (2) hydrolyzes of opioid peptides engaged in pain modulation, etc. Moreover, DPP-4 also acts as a carrier protein and ligand for a variety of extracellular and intracellular substrates. The Finding of DPP-4 inhibitors is the newer approach to treating numerous disorders/ diseases, for example, coronary heart disease, heart failure, stroke, and Diabetes mellitus (DM). The outcomes of studies carried out in the past few decades revealed that Gliptins (DPP-4 inhibitors) is a more promising candidate than conventional hypoglycaemic agents, as the former can be taken in monotherapy once a week or conjointly with another hypoglycaemic agent. By considering all favorable properties of DPP-4 inhibitors, this excerpt was written with the primary focused on the clinically approved, orally acting Gliptin class of drugs, with an emphasizing on their conventional, modern as well as patented methods of intermediates and final product development.

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来源期刊
Medicinal Chemistry Research
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.
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