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 K(i)=2nM) 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.
Representative scheme of DPP4N_Peptidase_S9 structure and an image from PDBsum server
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2I3ZFold classification based on Structure-Structure alignment of Proteins - FSSP server
