Zobrazeno 1 - 10
of 46
pro vyhledávání: '"Barbara Leiting"'
Autor:
Sangita B. Patel, Tesfaye Biftu, Nancy A. Thornberry, Reshma A. Patel, Barbara Leiting, Xiaoping Zhang, Joseph K. Wu, Ann E. Weber, Giovanna Scapin, Gui-Bai Liang, Xiaoxia Qian, Suresh B. Singh, Ying-Duo Gao
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3706-3710
Probing with tool molecules, and by modeling and X-ray crystallography the binding modes of two structurally distinct series of DPP-4 inhibitors led to the discovery of a rare aromatic fluorine H-bond and the spatial requirement for better biaryl bin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::819ef4fb415b9c85e948096dd6f6ab25
https://doi.org/10.1016/j.bmcl.2008.05.061
https://doi.org/10.1016/j.bmcl.2008.05.061
Autor:
Nancy A. Thornberry, Michael H. Fisher, Dooseop Kim, Bei B. Zhang, Huaibing He, Xiaoping Zhang, Barbara Leiting, Kathryn A. Lyons, Joseph K. Wu, Emma R. Parmee, Matthew J. Wyvratt, Linda Brockunier, KellyAnn D. Pryor, Ann E. Weber, Sangita B. Patel, George J. Eiermann, Ranabir Sinha Roy, Giovanna Scapin, Aleksandr Petrov, Lan Zhu, Jennifer E. Kowalchick
Publikováno v:
Journal of Medicinal Chemistry. 51:589-602
A series of beta-aminoamides bearing triazolopiperazines have been discovered as potent, selective, and orally active dipeptidyl peptidase IV (DPP-4) inhibitors by extensive structure-activity relationship (SAR) studies around the triazolopiperazine
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ea47e684c0a487b035f98caae89783bb
https://doi.org/10.1021/jm070330v
https://doi.org/10.1021/jm070330v
Autor:
Ann E. Weber, Reshma A. Patel, Joseph K. Wu, Aleksandr Petrov, Frank Marsilio, Jennifer E. Kowalchick, KellyAnn D. Pryor, Nancy A. Thornberry, Barbara Leiting, Kathryn A. Lyons, Giovanna Scapin, Huaibing He, George J. Eiermann, Dooseop Kim
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5934-5939
Various beta-amino amides containing triazolopiperazine heterocycles have been prepared and evaluated as potent, selective, orally active dipeptidyl peptidase IV (DPP-4) inhibitors. These compounds display excellent oral bioavailability and good over
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7e4b1107f9d56431f26f4262e6b4530a
https://doi.org/10.1016/j.bmcl.2007.07.100
https://doi.org/10.1016/j.bmcl.2007.07.100
Autor:
Reshma A. Patel, Huaibing He, David E. Kaelin, Barbara Leiting, Kathryn A. Lyons, Nancy A. Thornberry, Sangita B. Patel, Ann E. Weber, Abigail Lee Smenton, Alexsandr Petrov, George J. Eiermann, Giovanna Scapin, Joseph L. Duffy, Joseph K. Wu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5806-5811
A novel series of 4-arylcyclohexylalanine DPP-4 inhibitors was synthesized and tested for inhibitory activity as well as selectivity over the related proline-specific enzymes DPP-8 and DPP-9. Optimization of this series led to 28 (DPP-4 IC(50)=4.8 nM
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fc3a592642108ba541204b4e670a4dfe
https://doi.org/10.1016/j.bmcl.2007.08.049
https://doi.org/10.1016/j.bmcl.2007.08.049
Autor:
Joseph K. Wu, Reshma A. Patel, Nancy A. Thornberry, Ann E. Weber, Jason M. Cox, Shiyao Xu, Bing Zhu, Barbara Leiting, Kathryn A. Lyons, Scott D. Edmondson, Ranabir Sinha Roy, Bart Harper, Huaibing He, Anthony Mastracchio
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4579-4583
Substituted 3-aminopiperidines 3 were evaluated as DPP-4 inhibitors. The inhibitors showed good DPP-4 potency with superb selectivity over other peptidases (QPP, DPP8, and DPP9). Selected DPP-4 inhibitors were further evaluated for their hERG potassi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::98884c494e47764737b50f0ae2565589
https://doi.org/10.1016/j.bmcl.2007.05.087
https://doi.org/10.1016/j.bmcl.2007.05.087
Autor:
Joseph K. Wu, KellyAnn D. Pryor, Ann E. Weber, George J. Eiermann, Reshma A. Patel, Dooseop Kim, Jinyou Xu, Nancy A. Thornberry, Anthony Mastracchio, Scott D. Edmondson, Jennifer E. Kowalchick, Huaibing He, Barbara Leiting, Kathryn A. Lyons
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3373-3377
A series of beta-aminoamides bearing triazolopiperazines has been prepared and evaluated as potent, selective, orally active dipeptidyl peptidase IV (DPP-4) inhibitors. Efforts at optimization of the beta-aminoamide series, which ultimately led to th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::599f25f09625a28655ac50e27db98260
https://doi.org/10.1016/j.bmcl.2007.03.098
https://doi.org/10.1016/j.bmcl.2007.03.098
Autor:
Joseph K. Wu, Xiaoxia Qian, Barbara Leiting, Ranabir SinhaRoy, Dennis Feng, Huaibing He, Aleksandr Petrov, Nancy A. Thornberry, Ann E. Weber, Bei Zhang, Gui-Bai Liang, Tesfaye Biftu, Xiaoping Zhang, George J. Eiermann, Kathy Lyons
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1903-1907
Following the discovery of N-acyl-1,4-diazepan-2-one as a novel pharmacophore for potent and selective DPP-4 inhibitors, optimization of this new lead with different substitution on the seven-membered ring resulted in several highly potent and select
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::459312720817761e6c76a34503d42ff4
https://doi.org/10.1016/j.bmcl.2007.01.039
https://doi.org/10.1016/j.bmcl.2007.01.039
Autor:
Huaibing He, George J. Eiermann, Nancy A. Thornberry, Dennis Feng, Bei Zhang, Xiaoping Zhang, Tesfaye Biftu, Suresh B. Singh, Ranabir SinhaRoy, Kathy Lyons, Ann E. Weber, Ying-Duo Gao, Joseph K. Wu, Barbara Leiting, Gui-Bai Liang, Sangita B. Patel, Aleksandr Petrov, Xiaoxia Qian, Gerard R. Kieczykowski, Giovanna Scapin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:49-52
Replacement of the triazolopiperazine ring of sitagliptin (DPP-4 IC50 = 18 nM) with 3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one gave dipeptidyl peptidase IV (DPP-4) inhibitor 1 which is potent (DPP-4 IC50 = 2.6 nM), selective, and efficacious in an o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::90c3e0b3be6396416a385fb7d2aa8c88
https://doi.org/10.1016/j.bmcl.2006.09.099
https://doi.org/10.1016/j.bmcl.2006.09.099
Autor:
Reshma A. Patel, Aleksandr Petrov, Frank Marsilio, Barbara Leiting, Kathryn A. Lyons, Anthony Mastracchio, Lan Wei, Jinyou Xu, Ann E. Weber, Nancy A. Thornberry, George J. Eiermann, Joseph F. Leone, Joseph K. Wu, Scott D. Edmondson, Huaibing He, Robert J. Mathvink
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1346-1349
anti-Substituted beta-methylphenylalanine derived amides have been shown to be potent DPP-IV inhibitors exhibiting excellent selectivity over both DPP8 and DPP9. The optimized compound exhibited good pharmacokinetic profiles in three preclinical spec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a1284e8fa423c7dd04e87be5370781f6
https://doi.org/10.1016/j.bmcl.2005.11.052
https://doi.org/10.1016/j.bmcl.2005.11.052
Autor:
Hyun O. Ok, Tesfaye Biftu, Ann E. Weber, Scott D. Edmondson, William P. Feeney, Joseph K. Wu, Kelly Ann Pryor, George R. Lankas, Reshma A. Patel, Aleksandr Petrov, Xiaoping Zhang, Xiaoxia Qian, Nancy A. Thornberry, Dooseop Kim, Andrea Woods, Ranabir Sinha Roy, George J. Eiermann, Chi-Chung Chan, Dawn E. Ippolito, Maria G. Beconi, Lan Zhu, Leah Bitalac Reigle, Huaibing He, Dennis M. Zaller, Barbara Leiting, Kathryn A. Lyons
Publikováno v:
Diabetes. 54:2988-2994
Dipeptidyl peptidase (DPP)-IV inhibitors are a new approach to the treatment of type 2 diabetes. DPP-IV is a member of a family of serine peptidases that includes quiescent cell proline dipeptidase (QPP), DPP8, and DPP9; DPP-IV is a key regulator of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::04d32fb4e0599d1cdc316ba006f027e4
https://doi.org/10.2337/diabetes.54.10.2988
https://doi.org/10.2337/diabetes.54.10.2988