Results 161 to 170 of about 12,907 (206)

Dipeptide Phosphonates as Inhibitors of Dipeptidyl Peptidase IV

Journal of Medicinal Chemistry, 1994
A series of dipeptides which contained phosphonate analogs of proline and piperidine-2-carboxylic acid (homoproline) have been synthesized and tested as inhibitors of DPP-IV. The rates of inhibition of DPP-IV by these compounds are moderate, but the inhibitors are quite specific. The best inhibitor in the series is Ala-PipP(OPh-4-Cl)2 (13), which has a
B, Boduszek, J, Oleksyszyn, C M, Kam, J, Selzler, R E, Smith, J C, Powers   +5 more
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Azetidine-Based Inhibitors of Dipeptidyl Peptidase IV (DPP IV)

Current Topics in Medicinal Chemistry, 2007
The structure-activity relationships of azetidine-based DPP IV inhibitors will be discussed in detail in the following review. The azetidine-based DPP IV inhibitors can be divided into three main subtypes, the 2-cyanoazetidines, 3-fluoroazetidines and 2-ketoazetidines.
Dana, Ferraris, Sergei, Belyakov, Weixing, Li, Eddie, Oliver, Yao-Sen, Ko, David, Calvin, Susan, Lautar, Bert, Thomas, Camilo, Rojas   +8 more
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Psoriasiform eruption triggered by a dipeptidyl peptidase IV inhibitor

Australasian Journal of Dermatology, 2011
ABSTRACTPsoriatic patients have a higher prevalence of diabetes mellitus type 2 (DM). Since dipeptidyl peptidase IV (DPP‐IV) dysregulation is present in DM and psoriasis, DPP‐IV inhibitors have been proposed as therapeutic agents for both conditions. We report a psoriasiform eruption induced by sitagliptin, a DPP‐IV inhibitor. The role of DPP‐IV in the
Albert, Mas-Vidal, Jorge, Santos-Juanes, Altea, Esteve-Martinez, Luis, Caminal-Montero, Pablo, Coto-Segura   +4 more
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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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