Author/Authors :
Ravi Kurukulasuriya، نويسنده , , Jeffrey J. Rohde، نويسنده , , Bruce G. Szczepankiewicz، نويسنده , , Fatima Basha، نويسنده , , Chunqui Lai، نويسنده , , Hwan-Soo Jae، نويسنده , , Martin Winn، نويسنده , , Kent D. Stewart، نويسنده , , Kenton L. Longenecker، نويسنده , , Thomas W. Lubben، نويسنده , , Stephen J. Ballaron، نويسنده , , Hing L. Sham، نويسنده , , Thomas W. von Geldern، نويسنده ,
Abstract :
A series of xanthine mimetics containing 5,5 and 5,6 heterocycle fused imidazoles were synthesized as dipeptidyl peptidase IV inhibitors. Compound 7 is potent (h-DPPIV Ki = 2 nM) and exhibits excellent selectivity and no species specificity against rat and human enzymes. The X-ray structure confirms that the binding mode of 7 to rat DPPIV is similar to the parent xanthines.
Keywords :
Dipeptidyl peptidase IV (DPPIV) , SAR , X-ray structure , type 2 diabetes , xanthines
