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作为抗糖尿病药物的吡咯烷和哌啶磺酰胺衍生物的设计与合成

Design and synthesis of sulfonamide derivatives of pyrrolidine and piperidine as anti-diabetic agents.

作者信息

Sharma Radhika, Soman Shubhangi S

机构信息

Department of Chemistry, Faculty of Science, The M. S. University of Baroda, Vadodara, Gujarat 390 002, India.

Department of Chemistry, Faculty of Science, The M. S. University of Baroda, Vadodara, Gujarat 390 002, India.

出版信息

Eur J Med Chem. 2015 Jan 27;90:342-50. doi: 10.1016/j.ejmech.2014.11.041. Epub 2014 Nov 22.

Abstract

Type 2 diabetes (T2D) is a lifestyle disease affecting millions of people worldwide. Various therapies are available for the management of T2D and dipeptidyl peptidase-IV (DPP-IV) inhibition has emerged as a promising therapy for the treatment of type 2 diabetes (T2D). Here we report design, synthesis and in vitro efficacy of sulfonamide derivatives of pyrrolidine and piperidine as anti-diabetic agents. Amongst all the compounds synthesized in this series, 9a, is the most potent (IC50 = 41.17 nM).

摘要

2型糖尿病(T2D)是一种影响全球数百万人的生活方式疾病。有多种疗法可用于管理T2D,而二肽基肽酶-IV(DPP-IV)抑制已成为治疗2型糖尿病(T2D)的一种有前景的疗法。在此,我们报告吡咯烷和哌啶的磺酰胺衍生物作为抗糖尿病药物的设计、合成及体外疗效。在该系列合成的所有化合物中,9a最为有效(IC50 = 41.17 nM)。

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