Results 211 to 220 of about 22,026 (263)

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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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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Novel Serine Protease Dipeptidyl Peptidase IV Inhibitor: Alogliptin

Mini Reviews in Medicinal Chemistry, 2012
Alogliptin (codenamed SYR-322) is a recently approved anti-diabetic drug in Japan, which has been under clinical development phase III in USA and Europe. Alogliptin has been developed by Takeda under the brand name "Nesina". Alogliptin is a highly selective ( > 10,000-time selectivity, potent, reversible and durable serine protease dipeptidyl peptidase
Ritesh, Agrawal, Radhe Shyam, Bahare, Pratima, Jain, Subodh Narayan, Dikshit, Swastika, Ganguly   +4 more
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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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Dipeptidyl peptidase-IV inhibitors: fixing type 2 diabetes?

British Journal of Hospital Medicine, 2007
The optimal treatment of type 2 diabetes is currently uncertain. This article reviews a new class of oral hypoglycaemic agents: dipeptidyl peptidase-IV inhibitors. By potentiating the action of incretins they offer a more ‘physiological’ control of blood sugar with fewer side effects, and the possibility of ameliorating the decline in beta cell ...
Hugh F, McIntyre, Paul, Grant
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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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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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Discovery of tight-binding competitive inhibitors of dipeptidyl peptidase IV

International Journal of Biological Macromolecules, 2022
Dipeptidyl peptidase IV (DPP-IV, EC 3.4.14.5) is an abundant serine aminopeptidase that preferentially cleaves N-terminal Xaa-Pro or Xaa-Ala dipeptides from oligopeptides. Inhibitors of DPP-IV activity are used for treating type 2 diabetes mellitus and other diseases. DPP-IV is also involved in tumor progression.
Isel, Pascual Alonso, Pedro A, Valiente, Mario E, Valdés-Tresanco, Yarini, Arrebola, Fabiola, Almeida García, Lisset, Díaz, Gabriela, García, Osmany, Guirola, Daniel, Pastor, Gretchen, Bergado, Belinda, Sánchez, Jean-Louis, Charli   +11 more
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Potent and selective proline derived dipeptidyl peptidase IV inhibitors

Bioorganic & Medicinal Chemistry Letters, 2004
In-house screening of the Merck sample collection identified proline derived homophenylalanine 3 as a DPP-IV inhibitor with modest potency (DPP-IV IC50=1.9 microM). Optimization of 3 led to compound 37, which is among the most potent and selective DPP-IV inhibitors discovered to date.
Scott D, Edmondson, Anthony, Mastracchio, Maria, Beconi, Lawrence F, Colwell, Bahanu, Habulihaz, Huaibing, He, Sanjeev, Kumar, Barbara, Leiting, Kathryn A, Lyons, Ann, Mao, Frank, Marsilio, Reshma A, Patel, Joseph K, Wu, Lan, Zhu, Nancy A, Thornberry, Ann E, Weber, Emma R, Parmee   +16 more
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