Dipeptidyl peptidase-4 inhibitor with β-amino amide scaffold: Synthesis, SAR and biological evaluation

The SAR studies and evaluation of β-amino amide DPP4 inhibitor 5m are reported. Inhibitors of dipeptidyl peptidase-4 (DPP4) have been shown to be effective treatments for type 2 diabetes. Several series of β-amino amide containing piperazine derivatives have been prepared and evaluated as a inhibito...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-09, Vol.22 (17), p.5545-5549
Hauptverfasser:	Kim, Heung Jae, Kwak, Woo Young, Min, Jong Pil, Sung, Si Young, Kim, Ha Dong, Kim, Mi Kyung, Kim, Hae Sun, Park, Kyung Jin, Son, Moon Ho, Kim, Soon Hoe, Lee, Bong Jin
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemical synthesis Amides - chemistry Amides - pharmacology Animals Biological and medical sciences Blood Glucose - metabolism Diabetes Diabetes Mellitus, Type 2 - drug therapy Diabetes Mellitus, Type 2 - enzymology Dipeptidyl Peptidase 4 - metabolism Dipeptidyl-Peptidase IV Inhibitors - chemical synthesis Dipeptidyl-Peptidase IV Inhibitors - chemistry Dipeptidyl-Peptidase IV Inhibitors - pharmacology Dogs DPP4 GLP-1 Glucose Tolerance Test Humans Medical sciences Mice Mice, Inbred C57BL Models, Molecular Pharmacology. Drug treatments Piperazines - chemical synthesis Piperazines - chemistry Piperazines - pharmacology Rats Rats, Sprague-Dawley β-Amino amide
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Zusammenfassung:	The SAR studies and evaluation of β-amino amide DPP4 inhibitor 5m are reported. Inhibitors of dipeptidyl peptidase-4 (DPP4) have been shown to be effective treatments for type 2 diabetes. Several series of β-amino amide containing piperazine derivatives have been prepared and evaluated as a inhibitor of DPP4. Finally compound 5m was selected for further evaluation.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2012.07.019