In the past decade, developments of computational technology around density functional
theory (DFT) calculations have considerably increased the system sizes which can be …

Many diseases have been regarded to correlate with the in vivo oxidative damages, which
are caused by overproduced free radicals from metabolic process or reactive oxygen …

Abstract Type 2 Diabetes Mellitus (T2DM) is one of the highly prevalence disorder and
increasing day by day worldwidely. T2DM is a metabolic disorder, which is characterized by …

Background: Dipeptidyl peptidase-4 (DPP-4) inhibitors have emerged as anti-hyperglycemic
agents that improve glycemic control in type 2 diabetic patients, either as monotherapy or in …

In the present work, a novel series of trifluoromethyl-substituted tetrahydropyran derivatives
were rationally designed and synthesized as potent DPP-4 inhibitors with significantly …

A novel Michael/alkylation cascade reaction of N-unprotected 3-bromooxindoles with α, β-
unsaturated acyl phosphonates using DABCO as a robust catalyst followed by the …

Structure–activity relationships (SARs) and structure–property relationships (SPRs) have
been considered the most important factors during the drug optimization process. For …

Poor medication adherence in patients with type 2 diabetes mellitus has become one of the
main causes of suboptimal glycemic control. Once-weekly drugs can markedly improve the …

Our previous discovery of pyrazolo [1, 5-a] pyrimidin-7 (4H)-one scaffold-based DPP-4
inhibitors yielded two potent compounds b2 (IC 50= 79 nM) and d1 (IC 50= 49 nM) but …

Considerable effort has been made to achieve less frequent dosing in the development of
DPP-4 inhibitors. Enthusiasm for long-acting DPP-4 inhibitors is based on the promise that …