Results 261 to 270 of about 22,239 (295)

Structure-based design of pyridopyrimidinediones as dipeptidyl peptidase IV inhibitors

Bioorganic & Medicinal Chemistry Letters, 2012
Dipeptidyl peptidase IV (DPP-4) inhibitors have been shown to enhance GLP-1 levels and thereby improve hyperglycemia in type II diabetes. From a small fragment hit, using structure-based design, we have discovered a new class of non-covalent, potent and selective DPP-4 inhibitors.
Betty, Lam, Zhiyuan, Zhang, Jeffery A, Stafford, Robert J, Skene, Lihong, Shi, Stephen L, Gwaltney   +5 more
openaire   +2 more sources

Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors

Bioorganic & Medicinal Chemistry Letters, 2008
The synthesis, selectivity, rat pharmacokinetic profile, and drug metabolism profiles of a series of potent fluoroolefin-derived DPP-4 inhibitors (4) are reported. A radiolabeled fluoroolefin 33 was shown to possess a high propensity to form reactive metabolites, thus revealing a potential liability for this class of DPP-4 inhibitors.
Scott D, Edmondson, Lan, Wei, Jinyou, Xu, Jackie, Shang, Shiyao, Xu, Jianmei, Pang, Ashok, Chaudhary, Dennis C, Dean, Huaibing, He, Barbara, Leiting, Kathryn A, Lyons, Reshma A, Patel, Sangita B, Patel, Giovanna, Scapin, Joseph K, Wu, Maria G, Beconi, Nancy A, Thornberry, Ann E, Weber   +17 more
openaire   +2 more sources

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
openaire   +2 more sources

Neuroprotective Effects of Inhibitors of Dipeptidyl Peptidase-IV In Vitro and In Vivo

2005
For the first time, we demonstrated both neuroprotective and neuroregeneratrive effects of common DPP-IV inhibitors in vitro and in vivo. DPP IV inhibitors protect motor neurons from excitotoxic cell death. They are systemically active and protect striatal innervation of dopaminergic neurons, when administered concurrently with MPTP.
Yong-Qian, Wu, David C, Limburg, Douglas E, Wilkinson, Paul, Jackson, Joseph P, Steiner, Gregory S, Hamilton, Sergei A, Belyakov   +6 more
openaire   +2 more sources

Design and synthesis of long-acting inhibitors of dipeptidyl peptidase IV

Bioorganic & Medicinal Chemistry, 2007
A series of (4-substituted prolyl)prolinenitriles were synthesized and evaluated as inhibitors of dipeptidylpeptidase IV (DPP-IV). Among those tested, the 4beta-[4-(hydroxyphenyl)prolyl]prolinenitriles showed a potent inhibitory activity with a long duration of action. Metabolic formation of the corresponding phenol glucuronates was found to contribute
Takashi, Kondo, Isamu, Sugimoto, Takahiro, Nekado, Kenya, Ochi, Tazumi, Ohtani, Yohei, Tajima, Susumu, Yamamoto, Kazuhito, Kawabata, Hisao, Nakai, Masaaki, Toda   +9 more
openaire   +2 more sources

New Fluorogenic Dipeptidyl Peptidase IV/CD26 Substrates and Inhibitors

1997
Dipeptidyl peptidase IV (DP IV, CD26) is a membrane bound serine protease which ubiquitously occurs in epithelial tissues of mammalian organisms, above all in kidney, liver and intestine1,2 but also on the surface of immune cells3. DP IV is involved not only in activation of B- and T-lymphocytes4,5 and NK-cells6 with peptidase activity but also in the ...
S, Lorey, J, Faust, U, Hermanns, F, Bühling, S, Ansorge, K, Neubert   +5 more
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Synthesis and Evaluation of Thiouracil Derivatives as Dipeptidyl Peptidase IV Inhibitors

Chemical Biology & Drug Design, 2012
A series of thiouracil derivatives were designed, synthesized and screened for in vitro inhibition of dipeptidyl peptidase IV. The SAR study indicated the influence of substituted chemical modifications on thiouracil scaffold. Compounds 8 (IC50 = 0.32 μm), 9 (IC50 = 0.29 μm), and 12 (IC50 = 0.25 μm) showed excellent dipeptidyl peptidase IV inhibition ...
Mani, Sharma, Divya, Singh, Monica, Gupta   +2 more
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Population Pharmacokinetic/Pharmacodynamic Modelling of Dipeptidyl Peptidase IV Inhibitors

Clinical Pharmacokinetics, 2015
The prevalence of type 2 diabetes has dramatically increased over the past decades, causing high morbidity, mortality and healthcare costs. Dipeptidyl peptidase IV (DPP-4) inhibitors, also called ‘gliptins’, are a relatively new group of antidiabetic agents that target the incretin system.
openaire   +2 more sources

Comparative Safety of Sodium–Glucose Cotransporter 2 Inhibitors Versus Dipeptidyl Peptidase 4 Inhibitors and Sulfonylureas on the Risk of Diabetic Ketoacidosis

Diabetes Care, 2022
Ghadeer K Dawwas, James H Flory, Sean Hennessy   +2 more
exaly  

Dipeptidyl Peptidase IV Inhibitors for the Treatment of Diabetes

Journal of Medicinal Chemistry, 2004
openaire   +2 more sources