Results 101 to 110 of about 3,073 (139)

Sitagliptin phosphate: A DPP-4 inhibitor for the treatment of type 2 diabetes mellitus

Clinical Therapeutics, 2007
Sitagliptin phosphate, the first dipeptidyl peptidase 4 (DPP-4) inhibitor, provides a new treatment option for patients with type 2 diabetes.The purpose of this article is to review the pharmacology, pharmacokinetics, pharmacodynamics, clinical efficacy, adverse effects, and cost of sitagliptin in adults with type 2 diabetes.A literature search of ...
Tina Zerilli
exaly   +3 more sources

Efficient stereocontrolled synthesis of sitagliptin phosphate

Tetrahedron: Asymmetry, 2014
Abstract The synthesis of sitagliptin phosphate 1 , a novel DPP-IV inhibitor for the treatment of type 2 diabetes mellitus has been accomplished starting from the chiral synthon (1,4-bis[( R )-1-phenylethyl]piperazine-2,5-dione) 2 , involving highly stereocontrolled (>98%) alkylation as a key step, in a good overall yield of 50% over six steps.
Wahajul Haq
exaly   +2 more sources

Promoter engineering‐mediated Tuning of esterase and transaminase expression for the chemoenzymatic synthesis of sitagliptin phosphate at the kilogram‐scale

Biotechnology and Bioengineering, 2021
AbstractHere, we report a bienzymatic cascade to produce β‐amino acids as an intermediate for the synthesis of the leading oral antidiabetic drug, sitagliptin. A whole‐cell biotransformation using recombinant Escherichia coli coexpressing a esterase and transaminase were developed, wherein the desired expression level of each enzyme was achieved by ...
Taresh P Khobragade   +2 more
exaly   +3 more sources

Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: Close analogs of JANUVIA™ (sitagliptin phosphate)

Bioorganic and Medicinal Chemistry Letters, 2007
A series of beta-aminoamides bearing triazolopiperazines has been prepared and evaluated as potent, selective, orally active dipeptidyl peptidase IV (DPP-4) inhibitors. Efforts at optimization of the beta-aminoamide series, which ultimately led to the discovery of JANUVIA (sitagliptin phosphate, compound 1), are described.
Dooseop Kim   +2 more
exaly   +3 more sources

A comparative study of smart spectrophotometric methods for simultaneous determination of sitagliptin phosphate and metformin hydrochloride in their binary mixture

Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy, 2015
Simple, specific, accurate and precise spectrophotometric methods were developed and validated for the simultaneous determination of the oral antidiabetic drugs; sitagliptin phosphate (STG) and metformin hydrochloride (MET) in combined pharmaceutical formulations.
Hayam M Lotfy, Shereen Mowaka
exaly   +3 more sources

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