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Recent advances and structure-activity relationship studies of DPP-4 inhibitors as anti-diabetic agents
Bioorganic Chemistry ( IF 5.1 ) Pub Date : 2024-03-12 , DOI: 10.1016/j.bioorg.2024.107277
Shipra Singhal , Vaishali Manikrao Patil , Saroj Verma , Neeraj Masand

Diabetes mellitus (DM) is one of the largest public health problems worldwide and in the last decades various therapeutic targets have been investigated. For the treatment of type-2 DM (T2DM), dipeptidyl peptidase-4 (DPP-4) is one of the well reported target and has established safety in terms of cardiovascular complexicity. Preclinical and clinical studies using DPP-4 inhibitors have demonstrated its safety and effectiveness and have lesser risk of associated hypoglycaemic effect making it suitable for elderly patients. FDA has approved a number of structurally diverse DPP-4 inhibitors for clinical use. The present manuscript aims to focus on the well reported hybrid and non-hybrid analogues and their structural activity relationship (SAR) studies. It aims to provide structural insights for this class of compounds pertaining to favourable applicability of selective DPP-4 inhibitors in the treatment of T2DM.

中文翻译:

DPP-4抑制剂抗糖尿病的最新进展及构效关系研究

糖尿病(DM)是全球最大的公共卫生问题之一,在过去的几十年里,人们对各种治疗目标进行了研究。对于 2 型糖尿病 (T2DM) 的治疗,二肽基肽酶 4 (DPP-4) 是报道较多的靶标之一,并且在心血管复杂性方面已确立安全性。使用DPP-4抑制剂的临床前和临床研究已证明其安全性和有效性,并且相关降血糖作用的风险较小,适合老年患者。 FDA 已批准多种结构多样的 DPP-4 抑制剂用于临床。本手稿旨在重点关注已报道的混合和非混合类似物及其结构活性关系(SAR)研究。它旨在为此类化合物提供与选择性 DPP-4 抑制剂在 T2DM 治疗中的良好适用性相关的结构见解。
更新日期:2024-03-12
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