Singhal Shipra, Manikrao Patil Vaishali, Verma Saroj, Masand Neeraj
Department of Pharmaceutical Chemistry, KIET School of Pharmacy, KIET Group of Institutions, Delhi NCR, Ghaziabad, Uttar Pradesh, India.
Charak School of Pharmacy, Chaudhary Charan Singh (CCS) University, Meerut, Uttar Pradesh, India; Faculty of Pharmaceutical Sciences, UCSI University, Kuala Lumpur, Malaysia.
Bioorg Chem. 2024 May;146:107277. doi: 10.1016/j.bioorg.2024.107277. Epub 2024 Mar 12.
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.
糖尿病(DM)是全球最大的公共卫生问题之一,在过去几十年中,人们对各种治疗靶点进行了研究。对于2型糖尿病(T2DM)的治疗,二肽基肽酶-4(DPP-4)是一个报道较多的靶点,并且在心血管复杂性方面已确立了安全性。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,且低血糖相关效应的风险较小,使其适用于老年患者。美国食品药品监督管理局(FDA)已批准多种结构各异的DPP-4抑制剂用于临床。本手稿旨在聚焦于报道较多的杂合和非杂合类似物及其构效关系(SAR)研究。其目的是为这类化合物提供结构见解,以利于选择性DPP-4抑制剂在T2DM治疗中的应用。