Results 251 to 260 of about 22,784 (283)

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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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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A potent dipeptide inhibitor of dipeptidyl peptidase IV

Bioorganic & Medicinal Chemistry Letters, 1998
A series of novel potent inhibitors of dipeptidyl peptidase IV (DPP-IV) has been developed. A brief structure-activity relationship of the inhibitors was investigated. The dipeptide TSL-225, tryptophyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, was identified with the critical structure for the inhibitory activity.
M, Yamada, C, Okagaki, T, Higashijima, S, Tanaka, T, Ohnuki, T, Sugita   +5 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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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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