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New fluorinated pyrrolidine and azetidine amides as dipeptidyl peptidase IV inhibitors.

Hulin, Bernard; Cabral, Shawn; Lopaze, Michael G; Van Volkenburg, Maria A; Andrews, Kim M; Parker, Janice C.

Bioorg Med Chem Lett ; 15(21): 4770-3, 2005 Nov 01.

Article in English | MEDLINE | ID: mdl-16115768

ABSTRACT

Cyclohexylglycine amides of various fluorinated pyrrolidines and azetidines were prepared and tested for activity against dipeptidyl peptidase IV and in vivo in the KK mouse model of type 2 diabetes. The tetrafluoropyrrolidide, cis-3,4-difluoropyrrolidide and the fluorinated azetidides displayed unexpectedly strong activity.

Subject(s)

Adenosine Deaminase Inhibitors , Amides/chemical synthesis , Glycoproteins/antagonists & inhibitors , Pyrrolidines/chemical synthesis , Serine Proteinase Inhibitors/chemical synthesis , Amides/pharmacology , Animals , Azetidines , Diabetes Mellitus, Type 2/drug therapy , Dipeptidyl Peptidase 4 , Disease Models, Animal , Fluorine , Glucose Tolerance Test , Inhibitory Concentration 50 , Mice , Pyrrolidines/pharmacology , Serine Proteinase Inhibitors/pharmacology , Structure-Activity Relationship

ABSTRACT

Subject(s)

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