Zobrazeno 1 - 10
of 27
pro vyhledávání: '"Joe F. Lee"'
Autor:
Richard W. Chapman, Kung-I Feng, Aileen House, James Lamca, Robert G. Aslanian, Chander S. Celly, Rongze Kuang, Danlin Gu, Ping Wu, Zhidan Liu, Jianhua Cao, Daniel Prelusky, Ying Huang, Jonathan E. Phillips, Pauline C. Ting, Peng Wang, Daniel Lundell, Joe F. Lee
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:5528-5532
The optimization of oxazole-based PDE4 inhibitor 1 has led to the identification of both oral (compound 16) and inhaled (compound 34) PDE4 inhibitors. Selectivity against PDE10/PDE11, off target screening, and in vivo activity in the rat are discusse
Autor:
Margaret van Heek, Joe F. Lee, Michelle Smith, Mingxiang Lin, Nicolas Zorn, John R. Cook, Robert G. Aslanian, Pauline C. Ting, Scott S. Walker, Hyunjin M. Kim, Jean E. Lachowicz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:985-988
The structure-activity relationship studies of a novel series of carboxylic acid derivatives of pyridine-carboxamides as DGAT-1 inhibitors is described. The optimization of the initial lead compound 6 based on in vitro and in vivo activity led to the
Autor:
Samuel Wainhaus, Sang Q. Lam, Rongze Kuang, Paul M. McNicholas, Andrew J. Zych, Joe F. Lee, Gang Zhou, Todd A. Black, R. Jason Herr, Robert G. Aslanian, John H. Schwerdt, David Won-Shik Kim, Scott S. Walker, Jinhai Yang, Pauline C. Ting, He-Ping Wu, Yiming Xu, Jianhua Cao
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2890-2893
A novel series of pyridazinone analogs has been developed as potent β-1,3-glucan synthase inhibitors through structure-activity relationship study of the lead 5-[4-(benzylsulfonyl)piperazin-1-yl]-4-morpholino-2-phenyl-pyridazin-3(2H)-one (1). The ef
Autor:
Jianhua Cao, Anthony Cacciapuoti, Gang Zhou, Yiming Xu, Robert G. Aslanian, David Won-Shik Kim, Todd A. Black, Pauline C. Ting, He-Ping Wu, Scott S. Walker, Rongze Kuang, Samuel Wainhaus, Paul M. McNicholas, Joe F. Lee, John H. Schwerdt
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1819-1822
A structure-activity relationship study of the lead 5-[4-(benzylsulfonyl)piperazin-1-yl]-4-morpholino-2-phenyl-pyridazin-3(2H)-one 1 has resulted in the identification of 2-(3,5-difluorophenyl)-4-(3-fluorocyclopentyloxy)-5-[4-(isopropylsulfonyl)piper
Autor:
Robert G. Aslanian, Dan Prelusky, Ping Wu, Joe F. Lee, Peng Wang, Aileen House, Jennifer Richard, Jonathan E. Phillips, Dan Lundell, James Lamca, Richard Chapman, Pauline C. Ting
Publikováno v:
European Journal of Pharmacology. 643:274-281
A strategy to overcome the side effect liabilities of oral PDE4 inhibitors has been to deliver the drugs by inhalation. In this report, we identify 1-[[5-(1(S)-aminoethly)-2-[8-methoxy-2-(triflurormethyl)-5-quinolinyl]-4-oxazolyl] carbonyl]-4(R)-[(cy
Autor:
Jing Sun, Corey O. Strickland, John P. Caldwell, Kristin E. Rosner, Pauline C. Ting, Bandarpalle B. Shankar, Shiying Chen, David B. Belanger, Gerald W. Shipps, Vinay Girijavallabhan, Guowei Zhou, Brian J. Lavey, Dansu Li, Razia Rizvi, Peter Orth, Neng-Yang Shih, M. Arshad Siddiqui, Zhaoning Zhu, Wensheng Yu, Zhuyan Guo, Zhidan Liu, Maria David, John J. Piwinski, Daniel Lundell, Henry M. Vaccaro, Joe F. Lee, Jim Spitler, Vincent S. Madison, Xiaoda Niu, Chaoyang Dai, Mckittrick Brian A, Joseph A. Kozlowski, Janeta Popovici-Muller, Rob Mazzola
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4812-4815
The syntheses and structure-activity relationships of the tartrate-based TACE inhibitors are discussed. The optimization of both the prime and non-prime sites led to compounds with picomolar activity. Several analogs demonstrated good rat pharmacokin
Autor:
Neng-Yang Shih, Robert E. West, Robert G. Aslanian, Daniel M. Solomon, Wing C. Tom, Pauline C. Ting, Joe F. Lee, Margaret M. Albanese
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:2643-2646
A novel non-imidazole fluorene oxime 1a has been identified as a histamine H 3 inhibitor, and its structure–activity relationship has been evaluated.
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:491-494
The NK1 and NK2 receptor activity of a series of 5-[(3,5-bis(trifluoromethyl)phenyl)methoxy]-3-(3,4-dichlorophenyl)-4(Z)-(methoxyimino)pentyl-1-piperidines was evaluated. Compounds 11d, 11e, 11f, 12a, and 12k were found to be our most potent inhibito
Publikováno v:
Inorganica Chimica Acta. 243:333-343
Sterically hindered aromatic thiolate ligands have been used to synthesize the first examples of [FeIII(SR)4]1− complexes with monodentate ligands. The reaction of FeCl3 with 4 equiv. of lithium 2,3,5,6-tetramethylbenzenethiolate, Li[S-2,3,5,6-Me4C
Autor:
Daniel M. Solomon, Pauline C. Ting, Sidney R. Smith, Demetris N. Zambas, James Jakway, Carol Terminelli, Joe F. Lee
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:2749-2754
2-[10,11-Dihydro-5-ethoxy-5 H -dibenzo[a,d]cyclohepten-5-yl]-N,N-dimethyl-ethanamine (1) has been found to possess anticytokine activity. The synthesis and structure-activity relationship study of a series of analogues are reported.