| Name | DPP IV |
|---|---|
| Synonyms | ADABP; ADCP 2; ADCP2; Adenosine deaminase complexing protein 2; CD26; DPP IV; DPP 4; DPP4… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 17317162 | Yoshida T, Sakashita H, Akahoshi F, Hayashi Y: [(S)-gamma-(4-Aryl-1-piperazinyl)-l-prolyl] thiazolidines as a novel series of highly potent and long-lasting DPP-IV inhibitors. Bioorg Med Chem Lett. 2007 May 1;17(9):2618-21. Epub 2007 Feb 8. Of these compounds, the 4-(5-nitro-2-pyridyl) piperazine analog 21e showed a sub-nanomolar (IC (50)=0.92 nmol/L) DPP-IV inhibitory activity and a long-lasting in vivo DPP-IV inhibition profile. |
83(1,1,1,3) | Details |
| 17220239 | Vincent SH, Reed JR, Bergman AJ, Elmore CS, Zhu B, Xu S, Ebel D, Larson P, Zeng W, Chen L, Dilzer S, Lasseter K, Gottesdiener K, Wagner JA, Herman GA: Metabolism and excretion of the dipeptidyl peptidase 4 inhibitor [14C] sitagliptin in humans. Drug Metab Dispos. 2007 Apr;35(4):533-8. Epub 2007 Jan 12. These metabolites were the N- and N-carbamoyl conjugates of parent drug, a mixture of hydroxylated derivatives, an ether of a hydroxylated metabolite, and two metabolites formed by oxidative desaturation of the piperazine ring followed by cyclization. |
2(0,0,0,2) | Details |
| 16330047 | Engel M, Hoffmann T, Manhart S, Heiser U, Chambre S, Huber R, Demuth HU, Bode W: Rigidity and flexibility of dipeptidyl peptidase IV: crystal structures of and docking experiments with DPIV. J Mol Biol. 2006 Jan 27;355(4):768-83. Epub 2005 Nov 22. Here, we analyse DPIV complexes with a t-butyl-- tripeptide, Pro-boroPro, a piperazine compound, and aminoethyl phenyl sulfonylfluoride. |
2(0,0,0,2) | Details |
| 17220241 | Beconi MG, Reed JR, Teffera Y, Xia YQ, Kochansky CJ, Liu DQ, Xu S, Elmore CS, Ciccotto S, Hora DF, Stearns RA, Vincent SH: Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs. Drug Metab Dispos. 2007 Apr;35(4):525-32. Epub 2007 Jan 12. Approximately 10 to 16% of the radiolabeled dose was recovered in the rat and dog excreta as phase I and II metabolites, which were formed by N-sulfation, N-carbamoyl glucuronidation, hydroxylation of the triazolopiperazine ring, and oxidative desaturation of the piperazine ring followed by cyclization via the primary amine. |
2(0,0,0,2) | Details |
| 18039579 | Kondo T, Nekado T, Sugimoto I, Ochi K, Takai S, Kinoshita A, Hatayama A, Yamamoto S, Kishikawa K, Nakai H, Toda M: Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group. Bioorg Med Chem. 2008 Feb 15;16(4):1613-31. Epub 2007 Nov 17. Structural optimization of a N-(3-phenyl-1,2,4-thiadiazol-5-yl) piperazine analog 8, which was found by high-speed analog synthesis, was carried out to improve the potency and duration of action. |
2(0,0,0,2) | Details |
| 17352677 | Thornberry NA, Weber AE: Discovery of JANUVIA (Sitagliptin), a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Curr Top Med Chem. 2007;7(6):557-68. Initial work in an alpha-amino acid series related to isoleucyl thiazolidide was discontinued due to lack of selectivity; however, SAR studies on two screening leads led to the identification of a highly selective beta-amino acid piperazine series. |
2(0,0,0,2) | Details |
| 18996694 | Ahn JH, Park WS, Jun MA, Shin MS, Kang SK, Kim KY, Rhee SD, Bae MA, Kim KR, Kim SG, Kim SY, Sohn SK, Kang NS, Lee JO, Lee DH, Cheon HG, Kim SS: Synthesis and biological evaluation of homopiperazine derivatives with beta-aminoacyl group as dipeptidyl peptidase IV inhibitors. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6525-9. Epub 2008 Oct 21. |
1(0,0,0,1) | Details |
| 15324904 | Brockunier LL, He J, Colwell LF Jr, Habulihaz B, He H, Leiting B, Lyons KA, Marsilio F, Patel RA, Teffera Y, Wu JK, Thornberry NA, Weber AE, Parmee ER: Substituted piperazines as novel dipeptidyl peptidase IV inhibitors. . Bioorg Med Chem Lett. 2004 Sep 20;14(18):4763-6. Incorporation of a fluorophenyl beta-amino amide moiety into piperazine screening lead 2 has resulted in the discovery of a structurally novel series of potent and selective DP-IV inhibitors. |
1(0,0,0,1) | Details |