Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Beth B. Pinney"'
Autor:
Namal Chithranga Warshakoon, Beth B. Pinney, Ofer Reizes, Nick K. Kim, Justin Sheville, Chrissy Mitchell, José Méndez-Andino, X. Eric Hu, Jennifer L. Paris, John August Wos, Ritu Tiku Bhatt, Wei Ji, Kenneth M. Meyers
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:5207-5211
A novel series of substituted quinoline analogs were designed and synthesized as potent and selective melanin concentrating hormone (MCH) antagonists. These analogs show potent (nM) activity (12a-k) with a moderate selectivity. Conversely, the confor
Autor:
Julie A. Farmer, Adrian Gregory Switzer, Martin E. Dowty, Timothy B. Field, Adam W. Mazur, Xinrong Tian, Russell James Sheldon, Beth B. Pinney, Steve Berberich, Lalith R. Jayasinghe, Frank H. Ebetino, Doreen Crossdoersen, John August Wos, Cindy Obringer
Publikováno v:
Journal of Medicinal Chemistry. 49:4745-4761
The design, synthesis, and structure-activity relationships (SAR) of a series of novel proline and pyrrolidine based melanocortin receptor (MCR) agonists are described. To validate a conformationally constrained Arg-Nal dipeptide analogue strategy, w
Autor:
Beth B. Pinney, Jeffery C. Hayes, Xinrong Tian, Russell James Sheldon, Mark Gregory Solinsky, Adrian Gregory Switzer, Frank H. Ebetino, Doreen Crossdoersen, John August Wos, Julie A. Farmer, Xuemei Chen, Lixian Gan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1721-1725
The first synthesis of Tic-D-Phe Psi[CH(2)-CH(2)] isostere is described, which features diastereoselective alkylation of the tricyclic lactam 14. The use of this novel dipeptide isostere in the development of melanocortin agonists has been demonstrat
Autor:
Russell James Sheldon, Frank H. Ebetino, Doreen Crossdoersen, Beth B. Pinney, Timothy B. Field, John August Wos, Adam W. Mazur, Xinrong Tian
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:2819-2823
A series of proline based melanocortin ligands has been developed on the basis of initial piperazine leads by using a more conformationally rigid scaffold. A number of these novel ligands showed significant binding affinity for MC3 and MC4 receptors.
Autor:
Frank H. Ebetino, Doreen Crossdoersen, Lily Dong, Mark E. Webster, Beth B. Pinney, Russell James Sheldon, Adrian Gregory Switzer, Cindy Obringer, Mumin Rashid Naeem, Lalith R. Jayasinghe, Anny-Odile Colson, Rajesh K. Mishra, Charles A. Cruze, John August Wos, Steve A. Derose, Mark Gregory Solinsky, Martin E. Dowty, Paula M. Suchanek, Xinrong Tian, Julie A. Farmer, Melissa L. Burklow, Mary Kay Dirr
Publikováno v:
Journal of medicinal chemistry. 51(19)
A study that was designed to identify plausible replacements for highly basic guanidine moiety contained in potent MC4R agonists, as exemplified by 1, led to the discovery of initial nonguanidine lead 5. Propyl analog 23 was subsequently found to be
Autor:
M. Chrissy Mitchell, X. Eric Hu, Nick K. Kim, Namal Chithranga Warshakoon, Anny-Odile Colson, Kenneth M. Meyers, Beth B. Pinney, Wei Ji, José Méndez-Andino, Jan Richard Davis, John August Wos, Ofer Reizes
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(20)
A substituted 4-aminopiperidine was identified as showing activity in an MCH assay from an HTS effort. Subsequent structural modification of the scaffold led to the identification of a number of active MCH antagonists. 3,5-Dimethoxy-N-(1-(naphthalen-
Autor:
Adam W. Mazur, Russell James Sheldon, Nick K. Kim, Julie A. Farmer, Xinrong Tian, John August Wos, Frank H. Ebetino, Doreen Crossdoersen, X. Eric Hu, Adrian Gregory Switzer, Rajesh K. Mishra, Beth B. Pinney
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(17)
The design and synthesis of a series of potent 1,3,4-trisubstituted-2-oxopiperazine based MC4 agonists are described. The tripeptidomimetic analogs (12a,b and 23) and the dipeptidomimetic 27 displayed single-nanomolar binding affinity and agonist pot
Autor:
Xinrong Tian, John A. Wos, Adrian G. Switzer, Steve A. Derose, Rajesh K. Mishra, Mark G. Solinsky, Rashid N. Mumin, Frank H. Ebetino, Lalith R. Jayasinghe, Mark E. Webster, Anny-Odile Colson, Doreen Crossdoersen, Beth B. Pinney, Julie A. Farmer, Martin E. Dowty, Cindy M. Obringer, Charles A. Cruze, Melissa L. Burklow, Paula M. Suchanek, Lily Dong
Publikováno v:
Journal of Medicinal Chemistry; Sep2008, Vol. 51 Issue 19, p6055-6066, 12p