Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Yvonne C. Lo"'
Autor:
Robert J. Cherney, Peggy A. Scherle, Matthew E. Voss, Persymphonie B. Miller, Qihong Zhao, Gengjie Yang, Sarah R. King, Gregory D. Brown, Sandhya Mandlekar, Carl P. Decicco, Percy H. Carter, Andrew J. Tebben, Yvonne C. Lo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:3311-3316
We describe an isostere-driven approach to improve upon a previously-described series of capped dipeptide antagonists of CC Chemokine Receptor 2 (CCR2). Modification of the substitution around the isostere was combined with additional changes in a di
Autor:
Sandhya Mandlekar, John V. Duncia, Joel C. Barrish, Robert J. Cherney, Joseph B. Santella, Yang Michael G, Carl P. Decicco, Matthew E. Voss, Mary Ellen Cvijic, Dayton T. Meyer, Yvonne C. Lo, Percy H. Carter, Ruowei Mo, Qihong Zhao, Persymphonie B. Miller, Peggy A. Scherle, Gengjie Yang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2425-2430
We describe the design, synthesis, and evaluation, of γ-lactams as glycinamide replacements within a series of di- and trisubstituted cyclohexane CCR2 antagonists. The lactam-containing trisubstituted cyclohexanes proved to be more potent than the d
Autor:
Peggy A. Scherle, Matthew E. Voss, Dayton T. Meyer, Persymphonie B. Miller, Gengjie Yang, Andrew J. Tebben, Yvonne C. Lo, Robert J. Cherney, Ruowei Mo, Carl P. Decicco, Percy H. Carter
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:3418-3422
Potent sulfone-containing di- and trisubstituted cyclohexanes were synthesized and evaluated as CC chemokine receptor 2 (CCR2) antagonists. This led to the trisubstituted derivative 54, which exhibited excellent binding (CCR2 IC(50)=1.3nM) and functi
Autor:
Yvonne C. Lo, Carl P. Decicco, Dayton T. Meyer, Ruowei Mo, Sandhya Mandlekar, Percy H. Carter, Andrew J. Tebben, Kimberly A. Solomon, Gengjie Yang, David J. Nelson, Robert J. Cherney, Heather Jezak, Peggy A. Scherle, Zelda R. Wasserman
Publikováno v:
Journal of Medicinal Chemistry. 51:721-724
We describe the design, synthesis, and evaluation of novel disubstituted cyclohexanes as potent CCR2 antagonists. Exploratory SAR studies led to the cis-disubstituted derivative 22, which displayed excellent binding affinity for CCR2 (binding IC50 =
Autor:
Robert J. Cherney, Kimberly A. Solomon, Carl P. Decicco, Percy H. Carter, Yvonne C. Lo, Peggy A. Scherle, Sarah R. Friedrich, Andrew J. Tebben, Heather Jezak, Gregory D. Brown, Gengjie Yang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5455-5461
A new series of CCR2 antagonists has been discovered that incorporates intramolecular hydrogen bonding as a strategy for rigidifying the scaffold. The structure–activity relationship was established through initial systematic modification of substi
Autor:
Carl P. Decicco, Meizhong Xu, Rui-Qin Liu, Yvonne C. Lo, Percy H. Carter, Lorin A. Thompson, James M. Trzaskos, Gengjie Yang, Andrew J. Tebben, J. Gerry Everlof, Paul Strzemienski, Peggy A. Scherle, Gregory D. Brown, Matthew E. Voss
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:533-538
Based on the realization that N-alkyl 5-arylidene-2-thioxo-1,3-thiazolidin-4-ones are tumor necrosis factor-alpha antagonists, we discovered two additional classes of antagonists: 3-thioxo-2,3-dihydro-1H-imidazo[1,5-a]indol-1-ones (via rational desig
Autor:
Robert J. Cherney, Carl P. Decicco, Percy H. Carter, David J. Nelson, Gengjie Yang, Kimberly A. Solomon, Yvonne C. Lo, Peggy A. Scherle, Heather Jezak
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5063-5065
A series of cis-3,4-disubstituted piperidines was synthesized and evaluated as CC chemokine receptor 2 (CCR2) antagonists. Compound 24 emerged with an attractive profile, possessing excellent binding (CCR2 IC(50)=3.4 nM) and functional antagonism (ca
Autor:
Mary Ellen Cvijic, Joel C. Barrish, Robert J. Cherney, Carl P. Decicco, Persymphonie B. Miller, Gengjie Yang, Percy H. Carter, Yvonne C. Lo, Ruowei Mo, Anthony D. Pechulis, Dayton T. Meyer, Peggy A. Scherle, Qihong Zhao, Michael A. Guaciaro
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(19)
We describe the design, synthesis, and evaluation of benzimidazoles as benzamide replacements within a series of trisubstituted cyclohexane CCR2 antagonists. 7-Trifluoromethylbenzimidazoles displayed potent binding and functional antagonism of CCR2 w
Autor:
Carl P. Decicco, Percy H. Carter, Robert J. Cherney, Peggy A. Scherle, Bruce F. Molino, Persymphonie B. Miller, Yvonne C. Lo, Ruowei Mo, John B. Brogan, Gengjie Yang
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(3)
A series of trisubstituted cyclohexanes was designed, synthesized and evaluated as CC chemokine receptor 2 (CCR2) antagonists. This led to the identification of two distinct substitution patterns about the cyclohexane ring as potent and selective CCR
Autor:
Robert J. Cherney, Ruowei Mo, Dayton T. Meyer, David J. Nelson, Yvonne C. Lo, Gengjie Yang, Peggy A. Scherle, Sandhya Mandlekar, Zelda R. Wasserman, Heather Jezak, Kimberly A. Solomon, Andrew J. Tebben, Percy H. Carter, Carl P. Decicco
Publikováno v:
Journal of Medicinal Chemistry; Jan2008, Vol. 51 Issue 4, p721-724, 4p