1.
Bioorg Med Chem Lett
; 17(15): 4167-72, 2007 Aug 01.
Article
in English
| MEDLINE
| ID: mdl-17544668
ABSTRACT
Synthesis of a novel series of DPPIV inhibitors with 1,2,4- and 1,3,4-oxadiazolyl ketone derivatives and its structure-activity relationships are discussed. Compound 18h showed good inhibitory activity against DPPIV and favorable pharmacokinetic properties. In vivo pharmacodynamic efficacy and co-crystal structure of compound 18h with DPPIV is also described.
Subject(s)
Dipeptidyl-Peptidase IV Inhibitors , Ketones/chemistry , Ketones/chemical synthesis , Protease Inhibitors/chemistry , Protease Inhibitors/chemical synthesis , Animals , Crystallography, X-Ray , Dipeptidyl Peptidase 4/metabolism , Dogs , Haplorhini , Ketones/pharmacology , Kinetics , Models, Molecular , Molecular Structure , Protease Inhibitors/pharmacology , Rats , Structure-Activity Relationship
2.
Angew Chem Int Ed Engl
; 41(1): 176-8, 2002 Jan 04.
Article
in English
| MEDLINE
| ID: mdl-12491478
