Results 241 to 250 of about 22,239 (295)

Applications of dipeptidyl peptidase IV inhibitors in diabetes mellitus

The International Journal of Biochemistry & Cell Biology, 2006
A number of alternative therapies for type 2 diabetes are currently under development that take advantage of the actions of the incretin hormones glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide on the pancreatic beta-cell.
Christopher H S, McIntosh, Hans-Ulrich, Demuth, Su-Jin, Kim, J Andrew, Pospisilik, Raymond A, Pederson   +4 more
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Sitagliptin, a Dipeptidyl Peptidase-IV Inhibitor, Improves Psoriasis

Dermatology, 2011
A patient with a 17-year history of plaque psoriasis accompanied by type 2 diabetes mellitus discontinued cyclosporine and steroid ointment given for treatment of psoriasis because she was dissatisfied with the effects of the drugs. After sitagliptin, a dipeptidyl peptidase-IV (DPP-IV) inhibitor, was administered for control of blood glucose, psoriatic
Tatsuya, Nishioka, Masayuki, Shinohara, Noriyasu, Tanimoto, Chizuru, Kumagai, Kozo, Hashimoto   +4 more
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Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors

Bioorganic & Medicinal Chemistry Letters, 2009
A new series of DPP-4 inhibitors derived from piperidine-fused benzimidazoles and imidazopyridines is described. Optimization of this class of DPP-4 inhibitors led to the discovery of imidazopyridine 34. The potency, selectivity, cross-species DMPK profiles, and in vivo efficacy of 34 is reported.
Scott D, Edmondson, Anthony, Mastracchio, Jason M, Cox, George J, Eiermann, Huaibing, He, Kathryn A, Lyons, Reshma A, Patel, Sangita B, Patel, Aleksandr, Petrov, Giovanna, Scapin, Joseph K, Wu, Shiyao, Xu, Bing, Zhu, Nancy A, Thornberry, Ranabir Sinha, Roy, Ann E, Weber   +15 more
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Substituted piperazines as novel dipeptidyl peptidase IV inhibitors

Bioorganic & Medicinal Chemistry Letters, 2004
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. Simplification of the molecule and incorporation of multiple fluorine atoms on the phenyl ring has provided low molecular weight analogs such as compound 32 ...
Linda L, Brockunier, Jiafang, He, Lawrence F, Colwell, Bahanu, Habulihaz, Huaibing, He, Barbara, Leiting, Kathryn A, Lyons, Frank, Marsilio, Reshma A, Patel, Yohannes, Teffera, Joseph K, Wu, Nancy A, Thornberry, Ann E, Weber, Emma R, Parmee   +13 more
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Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors

Bioorganic & Medicinal Chemistry Letters, 2005
Dipeptidyl peptidase IV (DPP4) is a multifunctional type II transmembrane serine peptidase which regulates various physiological processes, most notably plasma glucose homeostasis by cleaving peptide hormones glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide.
Guohua, Zhao, Prakash C, Taunk, David R, Magnin, Ligaya M, Simpkins, Jeffrey A, Robl, Aiying, Wang, James G, Robertson, Jovita, Marcinkeviciene, Doree F, Sitkoff, Rex A, Parker, Mark S, Kirby, Lawrence G, Hamann   +11 more
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Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors

Bioorganic & Medicinal Chemistry Letters, 2006
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.
Ravi, Kurukulasuriya, Jeffrey J, Rohde, Bruce G, Szczepankiewicz, Fatima, Basha, Chunqui, Lai, Hwan-Soo, Jae, Martin, Winn, Kent D, Stewart, Kenton L, Longenecker, Thomas W, Lubben, Stephen J, Ballaron, Hing L, Sham, Thomas W, von Geldern   +12 more
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Dipeptidyl peptidase iv inhibitors and diabetes therapy

Frontiers in Bioscience, 2008
Current type 2 diabetes therapies are mainly targeted at stimulating pancreatic beta-cell secretion and reducing insulin resistance. A number of alternative therapies are currently being developed to take advantage of the actions of the incretin hormones Glucagon-Like Peptide-1 (GLP-1) and Glucose-dependent Insulinotropic Polypeptide (GIP).
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Potent Inhibitors of Dipeptidyl Peptidase iv and Their Mechanisms of Inhibition

2006
Dipeptidyl peptidase IV (DP IV) is a proline specific serine protease which cleaves Xaa-Pro-dipeptides from the N-terminus of longer peptides. A series of product analogous amino acid amides containing different structure modifications like substitution of a ring atom, variation of the ring size and/or the introduction of a thioxo amide bond, phosphono
A, Stöckel-Maschek, B, Stiebitz, I, Born, J, Faust, W, Mögelin, K, Neubert   +5 more
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Ketopyrrolidines and ketoazetidines as potent dipeptidyl peptidase IV (DPP IV) inhibitors

Bioorganic & Medicinal Chemistry Letters, 2004
In this paper, the synthesis and structure-activity relationships (SAR) of two classes of electrophile-based dipeptidyl peptidase IV (DPP IV) inhibitors, the ketopyrrolidines and ketoazetidines, is discussed. The SAR of these series demonstrate that the 2-thiazole, 2-benzothiazole, and 2-pyridylketones are optimal S1' binding groups for potency against
Dana, Ferraris, Yao-Sen, Ko, David, Calvin, Tiffany, Chiou, Susan, Lautar, Bert, Thomas, Krystyna, Wozniak, Camilo, Rojas, Vincent, Kalish, Sergei, Belyakov   +9 more
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Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes

Bioorganic & Medicinal Chemistry Letters, 2007
A series of substituted imidazopiperidine amides has been prepared and evaluated for inhibition of dipeptidyl peptidase IV (DPP-4). Substitution at the 1- and 3-positions produced increased selectivity for DPP-4 relative to DPP-8 and DPP-9. Compounds in this series had IC(50) values as low as 5.8 nM for inhibition of DPP-4.
Ping, Chen, Charles G, Caldwell, Robert J, Mathvink, Barbara, Leiting, Frank, Marsilio, Reshma A, Patel, Joseph K, Wu, Huaibing, He, Kathryn A, Lyons, Nancy A, Thornberry, Ann E, Weber   +10 more
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