1.
Bioorg Med Chem Lett
; 20(12): 3565-8, 2010 Jun 15.
Article
in English
| MEDLINE
| ID: mdl-20488702
ABSTRACT
A series of novel azobicyclo[3.3.0]octane derivatives were synthesized and evaluated as dipeptidyl peptidase 4 (DPP-4) inhibitors. The effort resulted in the discovery of inhibitor 2a, which exhibited excellent efficacies in an oral glucose tolerance test. Introduction of methyl group (2j) could prolong the inhibition of serum DPP-4 activity.
Subject(s)
Diabetes Mellitus, Type 2/drug therapy , Dipeptidyl-Peptidase IV Inhibitors/chemical synthesis , Hypoglycemic Agents/chemical synthesis , Octanes/chemical synthesis , Octanes/therapeutic use , Animals , Azo Compounds/chemical synthesis , Bridged Bicyclo Compounds/chemical synthesis , Dipeptidyl Peptidase 4/blood , Dipeptidyl Peptidase 4/metabolism , Dipeptidyl-Peptidase IV Inhibitors/pharmacology , Dipeptidyl-Peptidase IV Inhibitors/therapeutic use , Glucose Tolerance Test , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/therapeutic use , Mice , Mice, Inbred ICR , Octanes/pharmacology , Pharmacokinetics , Rats , Rats, Sprague-Dawley , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 20(12): 3521-5, 2010 Jun 15.
Article
in English
| MEDLINE
| ID: mdl-20488704
ABSTRACT
A series of novel bicyclo[3.3.0]octane derivatives have been synthesized and found to be dipeptidyl peptidase 4 (DPP-4) inhibitors. Compounds 10a and 10b demonstrate good efficacies in oral glucose tolerance tests.
