Zobrazeno 1 - 10
of 52
pro vyhledávání: '"S. Skwish"'
Autor:
A A Seymour, William N. Washburn, Dorothy Slusarchyk, P.J. McCann, B.E. Abboa-Offei, Minsheng Zhang, G.T. Allen, Ravindar N. Girotra, B.H. Frohlich, Michael Cap, Jollie D. Godfrey, Peter T. W. Cheng, R.J. George, C. Shao, Anita D. Russell, S. Skwish, Philip M. Sher, Jon J. Hangeland, A.V. Gavai, T.L. Waldron, Belay Tesfamariam, Yolanda Caringal, T.W. Harper, Tamara Dejneka, Kenneth E.J. Dickinson, Ginger Wu, Syed Z. Ahmed, Amarendra B. Mikkilineni, Hongwei Zhang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4290-4296
Utilization of N-substituted-4-hydroxy-3-methylsulfonanilidoethanolamines 1 as selective beta(3) agonists is complicated by their propensity to undergo metabolic oxidative N-dealkylation, generating 0.01-2% of a very potent alpha(1) adrenergic agonis
Autor:
Liesl G. Fisher, P.J. McCann, D.A. Young, C.M. Arbeeny, S. Skwish, Amarendra B. Mikkilineni, Poss Kathleen M, G.T. Allen, Chongqing Sun, Michael Cap, R.J. George, Dorothy Slusarchyk, B.E. Abboa-Offei, Ravindar N. Girotra, William N. Washburn, Carl P. Ciosek, A.V. Gavai, Belay Tesfamariam, T.W. Harper, Ginger Wu, B.H. Frohlich, D.E. Hillyer, Tammy C. Wang, A A Seymour, Mark S. Bednarz, Philip M. Sher, Kenneth E.J. Dickinson, T.L. Waldron, Arvind Mathur
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:3041-3044
A series of 4-hydroxy-3-methylsulfonanilido-1,2-diarylethylamines were prepared and evaluated for their human beta(3) adrenergic receptor agonist activity. SAR studies led to the identification of BMS-196085 (25), a potent beta(3) full agonist (K(i)=
Autor:
Philip M. Sher, Liesl G. Fisher, Steven M. Seiler, Inge M. Michel, S. Skwish, Gang Wu, Arvind Mathur, Kenneth E.J. Dickinson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:1583-1588
Carboxyl and other negatively charged groups were found to be most effective at producing human β3 adrenergic receptor binding selectivity in 1 (BRL 37344) and related compounds. The sulfonic acid analog 7 (BMS-187413) is a novel and potent β3 adre
Autor:
Liesl G. Fisher, Kenneth E.J. Dickinson, Inge M. Michel, S. Skwish, Steven M. Seiler, Philip M. Sher
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:2253-2258
Novel heterocyclic β 3 adrenergic receptor agonists 2 were prepared and evaluated for their ability to bind to human β 1 , β 2 , and β 3 adrenergic receptors. Stimulatory effects on the β 3 adrenergic receptor were also measured. BMS-187257 ( 4b
Autor:
R.B. Cohen, Kenneth E.J. Dickinson, Zhengxiang Gu, S. Skwish, Michael A. Poss, Randy Serafino, James R. Powell, Carol L. Delaney, Suzanne Moreland, Denis E. Ryono
Publikováno v:
British Journal of Pharmacology. 113:179-189
1. This study compares the activity of BMS-180560 (2-butyl-1-chloro-1-[[1-[2-(2H-tetrazol-5-yl)phenyl]-1H-indol-4- yl]methyl]-1H-imidazole-5-carboxylic acid), an insurmountable angiotensin II (AII) receptor antagonist, with that of losartan and EXP31
Autor:
Kenneth E.J. Dickinson, J. Buote, Denis E. Ryono, John Lloyd, Diane E. Normandin, J.E. Bird, Tamara Dejneka, Suzanne Moreland, E.R. Spitzmiller, Carol L. Delaney, Thomas L. Waldron, S. Skwish
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:195-200
We have synthesized a series of quinoline-4-carboxylic acids that are potent antagonists of the angiotensin II receptor. They show high receptor binding affinities and functional antagonism in rabbit aortic strips. They are also effective in blocking
Autor:
Diane E. Normandin, Kenneth E.J. Dickinson, Denis E. Ryono, J.E. Bird, Thomas L. Waldron, Suzanne Moreland, Tamara Dejneka, Carol L. Delaney, J. Buote, John Lloyd, E.R. Spitzmiller, S. Skwish
Publikováno v:
ChemInform. 25
We have synthesized a series of quinoline-4-carboxylic acids that are potent antagonists of the angiotensin II receptor. They show high receptor binding affinities and functional antagonism in rabbit aortic strips. They are also effective in blocking
Autor:
Inge M. Michel, S. Skwish, Steven M. Seiler, Liesl G. Fisher, Kenneth E.J. Dickinson, Philip M. Sher
Publikováno v:
ChemInform. 28
Novel heterocyclic β 3 adrenergic receptor agonists 2 were prepared and evaluated for their ability to bind to human β 1 , β 2 , and β 3 adrenergic receptors. Stimulatory effects on the β 3 adrenergic receptor were also measured. BMS-187257 ( 4b
Autor:
Robert V. Moquin, Suzanne Moreland, Carol L. Delaney, Sharon B. Williams, S. Skwish, S.Anders Hedberg, Kenneth E.J. Dickinson, Harold N. Weller, Robert Cohen, Arthur V. Miller
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 2:1115-1120
N-Biphenylmethyl benzothiadiazine dioxides were prepared as potential angiotensin-II receptor antagonists. Stability of the compounds is dependent upon the nature of the substituent at position 3 of the benzothiadiazine ring, while potency is depende
Autor:
Z. Merchant, S. Skwish, Dorothy Slusarchyk, P.J. McCann, D.A. Young, M. Morella, Kenneth E.J. Dickinson, Michael Cap, Ravindar N. Girotra, Anita D. Russell, B.E. Abboa-Offei, William N. Washburn, G.T. Allen, A.V. Gavai, Belay Tesfamariam, Peter T. W. Cheng, G. S. Bisacchi, Tammy C. Wang, A A Seymour, T.W. Harper, C.M. Arbeeny, Tamara Dejneka, Amarendra B. Mikkilineni, Poss Kathleen M, Chongqing Sun, Philip M. Sher, T.L. Waldron, R.J. George, B.H. Frohlich, Ginger Wu, Denis E. Ryono
Publikováno v:
Bioorganicmedicinal chemistry letters. 14(13)
A series of N-(4-hydroxy-3-methylsulfonanilidoethanol)arylglycinamides were prepared and evaluated for their human β3 adrenergic receptor agonist activity. SAR studies led to the identification of BMS-201620 (39), a potent β3 full agonist (Ki=93 nM