Zobrazeno 1 - 8 of 8 pro vyhledávání: '"Eric A. Wadman"'
1
From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part II: Acyclic replacements for the (3S)-3-benzylpiperidine in a series of potent CCR3 antagonists
Autor: Andrew J. Tebben, Gardner Daniel S, Douglas G. Batt, Paul Davies, Eric A. Wadman, John V. Duncia, Sarah C. Traeger, Percy H. Carter, Patricia K. Welch, Soo S. Ko, Joseph B. Santella
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 18:586-595
Conformational analysis of the 3-benzylpiperidine in CCR3 antagonist clinical candidate 1 (BMS-639623) predicts that the benzylpiperidine may be replaced by acyclic, conformationally stabilized, anti-1,2-disubstituted phenethyl- and phenpropylamines.
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d938b4844c051d618531f3920ea7271a
https://doi.org/10.1016/j.bmcl.2007.11.087
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4
2,4-Disubstituted piperidines as selective CC chemokine receptor 3 (CCR3) antagonists: Synthesis and selectivity
Autor: Carl P. Decicco, Nicole Stowell, George L. Trainor, Robert C. Newton, Nao Asakawa, Steven M. Friedman, Kimberly A. Solomon, Kim Harrison, Patricia K. Welch, Bin Jiang, Paul S. Watson, Maryanne B. Covington, Soo S. Ko, Eric A. Wadman, Paul Davies
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 16:5695-5699
Linear unselective CCR3 antagonist leads with IC(50) values in the 200 nM range were converted into low nM binding compounds selective at CCR3 by moving the piperidine nitrogen substituent to the carbon at the 2-position of the ring. Substitution of
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e00d69b7b8609837c7fb5ea4f7a5b499
https://doi.org/10.1016/j.bmcl.2006.08.012
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5
Discovery of CC Chemokine Receptor-3 (CCR3) Antagonists with Picomolar Potency
Autor: Kimberly A. Solomon, Joseph B. Santella, George L. Trainor, Robert C. Newton, Zhang Wang, Dean A. Wacker, George V. De Lucca, Anuk M. Das, Paul Davies, Ui Tae Kim, Maryanne B. Covington, Danielle M. Graden, Gardner Daniel S, Nicole Stowell, Changsheng Zheng, John V. Duncia, Brian J. Vargo, George C. Emmett, Eric A. Wadman, Carl P. Decicco, Patricia K. Welch, Swamy Yeleswaram, Ann Y. Liauw, Soo S. Ko
Publikováno v: Journal of Medicinal Chemistry. 48:2194-2211
Starting with our previously described(20) class of CC chemokine receptor-3 (CCR3) antagonist, we improved the potency by replacing the phenyl linker of 1 with a cyclohexyl linker and by replacing the 4-benzylpiperidine with a 3-benzylpiperidine. The
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::46c16edc52bde0e47150badd54fc3e04
https://doi.org/10.1021/jm049530m
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6
Selective inhibition of eosinophil influx into the lung by small molecule CC chemokine receptor 3 antagonists in mouse models of allergic inflammation
Autor: Soo S. Ko, Patricia Welch, Krishnaswamy Yeleswaram, Xiaosui Jiang, Percy H. Carter, Maryanne B. Covington, Paul Davies, Anuk M. Das, Candice M. Krauthauser, Robert Newton, Danielle M. Graden, Kimberly A. Solomon, Kim W. McIntyre, Eric A. Wadman, James M. Trzaskos, Krishna Vaddi, Sandhya Mandlekar, Xiao Xia Yang
Publikováno v: The Journal of pharmacology and experimental therapeutics. 318(1)
CC chemokine receptor (CCR) 3 is a chemokine receptor implicated in recruiting cells, particularly eosinophils (EPhi), to the lung in episodes of allergic asthma. To investigate the efficacy of selective, small molecule antagonists of CCR3, we develo
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d9802ecabb6bd2727ee1beb61a95779b
https://pubmed.ncbi.nlm.nih.gov/16614169
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7
N-Arylalkylpiperidine urea derivatives as CC chemokine receptor-3 (CCR3) antagonists
Autor: Dean A. Wacker, James M. Trzaskos, Gregory C. Houghton, Carl P. Decicco, Percy H. Carter, Patricia K. Welch, Douglas G. Batt, Eric A. Wadman, John Roderick, Paul Davies, Yevgeniya I. Orlovsky, Joseph B. Santella
Publikováno v: Bioorganicmedicinal chemistry letters. 15(3)
The synthesis and structure-activity relationships of N-arylalkylpiperidylmethyl ureas as antagonists of the CC chemokine receptor-3 (CCR3) are presented. These compounds displayed potent binding to the receptor as well as functional antagonism of eo
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5eadac300a6542f087d87ed375a42dcb
https://pubmed.ncbi.nlm.nih.gov/15664858
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8
Discovery of N-propylurea 3-benzylpiperidines as selective CC chemokine receptor-3 (CCR3) antagonists
Autor: Kimberley Solomon, George L. Trainor, Maryanne B. Covington, Melissa Estrella, Robert C. Newton, Joseph B. Santella, Nicole Stowell, Paul S. Watson, Cheryl M. Clark, Jeffrey G. Varnes, Paul Davies, John V. Duncia, Eric A. Wadman, Carl P. Decicco, Gardner Daniel S, Patricia K. Welch, Soo S. Ko, Dean A. Wacker
Publikováno v: Bioorganicmedicinal chemistry letters. 14(7)
The discovery of novel and selective small molecule antagonists of the CC Chemokine Receptor-3 (CCR3) is presented. Simple conversion from a 4- to 3-benzylpiperidine gave improved selectivity for CCR3 over the serotonin 5HT(2A) receptor. Chiral resol
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::752de095193da0d8128da3ea9d091ac1
https://pubmed.ncbi.nlm.nih.gov/15026042
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