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

Heung Jae Kim; Woo Young Kwak; Jong Pil Min; Si Young Sung; Ha Dong Kim; Mi Kyung Kim; Hae Sun Kim; Kyung Jin Park; Moon Ho Son; Soon Hoe Kim; Bong Jin Lee

doi:10.1016/j.bmcl.2012.07.019

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

Bioorg Med Chem Lett. 2012 Sep 1;22(17):5545-9. doi: 10.1016/j.bmcl.2012.07.019. Epub 2012 Jul 14.

Authors

Heung Jae Kim¹, Woo Young Kwak, Jong Pil Min, Si Young Sung, Ha Dong Kim, Mi Kyung Kim, Hae Sun Kim, Kyung Jin Park, Moon Ho Son, Soon Hoe Kim, Bong Jin Lee

Affiliation

¹ Dong-A Pharm. Co., Ltd, 47-5, Sanggal-dong, Giheung-gu, Yongin-si, Gyeonggi-do 446-905, Republic of Korea.

PMID: 22850208
DOI: 10.1016/j.bmcl.2012.07.019

Abstract

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.

MeSH terms

Amides / chemical synthesis
Amides / chemistry*
Amides / pharmacology*
Animals
Blood Glucose / metabolism
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
Glucose Tolerance Test
Humans
Mice
Mice, Inbred C57BL
Models, Molecular
Piperazines / chemical synthesis
Piperazines / chemistry
Piperazines / pharmacology
Rats
Rats, Sprague-Dawley

Substances

Amides
Blood Glucose
Dipeptidyl-Peptidase IV Inhibitors
Piperazines
Dipeptidyl Peptidase 4