Long-acting peptidomimetics based DPP-IV inhibitors

Pradip Jadav; Rajesh Bahekar; Shailesh R Shah; Dipam Patel; Amit Joharapurkar; Samadhan Kshirsagar; Mukul Jain; Mubeen Shaikh; Kalapatapu V V M Sairam

doi:10.1016/j.bmcl.2012.03.078

Long-acting peptidomimetics based DPP-IV inhibitors

Bioorg Med Chem Lett. 2012 May 15;22(10):3516-21. doi: 10.1016/j.bmcl.2012.03.078. Epub 2012 Mar 28.

Authors

Pradip Jadav¹, Rajesh Bahekar, Shailesh R Shah, Dipam Patel, Amit Joharapurkar, Samadhan Kshirsagar, Mukul Jain, Mubeen Shaikh, Kalapatapu V V M Sairam

Affiliation

¹ Zydus Research Centre, Sarkhej-Bavla NH 8A Moraiya, Ahmedabad, India.

PMID: 22503246
DOI: 10.1016/j.bmcl.2012.03.078

Abstract

Pyrrolidine based peptidomimetics are reported as potent and selective DPP-IV inhibitors for the treatment of T2DM. Compounds 16c and 16d showed excellent in vitro potency and selectivity towards DPP-IV and the lead compound 16c showed sustained antihyperglycemic effects, along with improved pharmacokinetic profile.

MeSH terms

Animals
Dipeptidyl-Peptidase IV Inhibitors / pharmacokinetics
Dipeptidyl-Peptidase IV Inhibitors / pharmacology*
Hypoglycemic Agents / pharmacology*
Mice
Mice, Inbred C57BL
Peptidomimetics / pharmacokinetics
Peptidomimetics / pharmacology*

Substances

Dipeptidyl-Peptidase IV Inhibitors
Hypoglycemic Agents
Peptidomimetics