| Title : Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors - Kurukulasuriya_2006_Bioorg.Med.Chem.Lett_16_6226 |
| Author(s) : Kurukulasuriya R , Rohde JJ , Szczepankiewicz BG , Basha F , Lai C , Jae HS , Winn M , Stewart KD , Longenecker KL , Lubben TW , Ballaron SJ , Sham HL , von Geldern TW |
| Ref : Bioorganic & Medicinal Chemistry Lett , 16 :6226 , 2006 |
|
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 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. |
| PubMedSearch : Kurukulasuriya_2006_Bioorg.Med.Chem.Lett_16_6226 |
| PubMedID: 17010607 |
| Gene_locus related to this paper: ratno-dpp4 |
| Inhibitor | LIR |
| Gene_locus | ratno-dpp4 |
| Structure | 2I3Z |
Kurukulasuriya R, Rohde JJ, Szczepankiewicz BG, Basha F, Lai C, Jae HS, Winn M, Stewart KD, Longenecker KL, Lubben TW, Ballaron SJ, Sham HL, von Geldern TW (2006)
Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors
Bioorganic & Medicinal Chemistry Lett
16 :6226
Kurukulasuriya R, Rohde JJ, Szczepankiewicz BG, Basha F, Lai C, Jae HS, Winn M, Stewart KD, Longenecker KL, Lubben TW, Ballaron SJ, Sham HL, von Geldern TW (2006)
Bioorganic & Medicinal Chemistry Lett
16 :6226