A potent dipeptide inhibitor of dipeptidyl peptidase IV

M Yamada; C Okagaki; T Higashijima; S Tanaka; T Ohnuki; T Sugita

doi:10.1016/s0960-894x(98)00259-5

A potent dipeptide inhibitor of dipeptidyl peptidase IV

Bioorg Med Chem Lett. 1998 Jun 16;8(12):1537-40. doi: 10.1016/s0960-894x(98)00259-5.

Authors

M Yamada¹, C Okagaki, T Higashijima, S Tanaka, T Ohnuki, T Sugita

Affiliation

¹ Lead Generation Research Laboratory, Tanabe Seiyaku Co., Ltd., Osaka, Japan.

PMID: 9873385
DOI: 10.1016/s0960-894x(98)00259-5

Abstract

A series of novel potent inhibitors of dipeptidyl peptidase IV (DPP-IV) has been developed. A brief structure-activity relationship of the inhibitors was investigated. The dipeptide TSL-225, tryptophyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, was identified with the critical structure for the inhibitory activity.

MeSH terms

Dipeptidyl Peptidase 4 / drug effects*
Isoquinolines / chemical synthesis*
Isoquinolines / pharmacology*
Serine Proteinase Inhibitors / chemistry*
Serine Proteinase Inhibitors / pharmacology*
Structure-Activity Relationship
Tetrahydroisoquinolines*

Substances

Isoquinolines
Serine Proteinase Inhibitors
TSL 225
Tetrahydroisoquinolines
Dipeptidyl Peptidase 4