Výsledky vyhledávání - "Beryl W. Dominy"

Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings 1PII of original article: S0169-409X(96)00423-1. The article was originally published in Advanced Drug Delivery Reviews 23 (1997) 3–25. 1

Autor: Christopher A. Lipinski, Beryl W. Dominy, Paul J. Feeney, Franco Lombardo

Publikováno v: Advanced Drug Delivery Reviews. 46:3-26

Experimental and computational approaches to estimate solubility and permeability in discovery and development settings are described. In the discovery setting 'the rule of 5' predicts that poor absorption or permeation is more likely when there are

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1cacaa5128417838a13b65511ed9ec29
https://doi.org/10.1016/s0169-409x(00)00129-0

Zobrazit plný text záznamu

Direct observation by X-ray analysis of the tetrahedral 'intermediate' of aspartic proteinases

Autor: Robert L. Rosati, Tom L. Blundell, David B. Damon, B. Veerapandian, Andrej Sali, Jon B. Cooper, Beryl W. Dominy, Dennis J. Hoover

Publikováno v: Protein Science. 1:322-328

We report the X-ray analysis at 2.0 A resolution for crystals of the aspartic proteinase endothiapepsin (EC 3.4.23.6) complexed with a potent difluorostatone-containing tripeptide renin inhibitor (CP-81,282). The scissile bond surrogate, an electroph

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9d0964299049ad0fb8748f92b395f9fe
https://doi.org/10.1002/pro.5560010303

Zobrazit plný text záznamu

A unified approach to systematic isosteric substitution for acidic groups and application to NMDA antagonists related to 2-amino-7-phosphonoheptanoate

Autor: L. C. Marinovic, R. T. Ronau, Christopher A. Lipinski, Martin J. Pagnozzi, E. Edward Mena, G. C. Butterfield, Beryl W. Dominy, Bertrand L. Chenard, T. Tsang, Butler Todd W

Publikováno v: Journal of Medicinal Chemistry. 33:1077-1083

A systematic approach to the replacement of acidic groups with potential bioisosteres is described. The strategy involves simple nucleophilic displacement of a common alkyl halide precursor with a variety of mercaptoazoles and related molecules. The

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4d71d71256e38828558dd436f990e8c8
https://doi.org/10.1021/jm00165a030

Zobrazit plný text záznamu

trans-3-Benzyl-4-hydroxy-7-chromanylbenzoic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor

Autor: R. J. Chambers, Kelvin Cooper, M. Ramchandani, M. S. Biggers, G. P. Hingorani, Beryl W. Dominy, Maryrose J. Conklyn, Santo R. Cortina, Gary J. Martinelli, Lawrence A. Reiter, Joseph DiBrino, Piscopio Anthony D, Cathy A. Farrell, Kevin Koch, Kathyrn F. Wright, Robbin Alpert, Henry J. Showell

Publikováno v: Bioorganicmedicinal chemistry letters. 8(14)

The SAR of a series of 2-(7-chromanyl)benzoic acids has been investigated with the aim of identifying potent and selective LTB 4 receptor antagonists that maintain potency in complex biological fluids. We found optimal activity in derivatives with el

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e6b17e329a509ea2992fb5b2c1c356a0
https://pubmed.ncbi.nlm.nih.gov/9873433

Zobrazit plný text záznamu

X-Ray Analysis of a Difluorostatone Renin Inhibitor Bound as the Tetrahedral Hydrate to the Aspartic Protease Endothiapepsin

Autor: Tom L. Blundell, Robert L. Rosati, David B. Damon, Jon B. Cooper, Dennis J. Hoover, Balusubramanian Veerapandian, Beryl W. Dominy

Publikováno v: Advances in Experimental Medicine and Biology ISBN: 9781468460148

In this study we report the X-ray analysis of a complex between the aspartic protease endothiapepsin (EC 3.4.23.6) and an inhibitor bound as a carbonyl hydrate (gem-diol) to the catalytic aspartates of this enzyme, in a manner closely resembling the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::261558ef5b14a1dfe221d3fb23c89ce2
https://doi.org/10.1007/978-1-4684-6012-4_32

Zobrazit plný text záznamu

Dopamine receptor blockade by imidoline and its proposed active conformation

Autor: Susan W. Koch, Beryl W. Dominy, B. Kenneth Koe

Publikováno v: European Journal of Pharmacology. 68:139-146

Imidoline, 1-[2-(N,N-dimethylamino)ethyl]-3-m-chlorophenyl-2-imidazolidinone, has been found to be as potent as chlorpromazine in increasing striatal DOPA accumulation and prolactin secretion in vivo. In contrast, imidoline exhibited only weak inhibi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c77e0c5aa5896cb3945ae051e689a313
https://doi.org/10.1016/0014-2999(80)90314-3

Zobrazit plný text záznamu

Computer graphics modelling of human renin

Autor: Chirgwin John Mitchell, Jasjit S. Bindra, Beryl W. Dominy, Peter M. Hobart, B. L. Sibanda, Tom L. Blundell, Michael Fogliano

Publikováno v: FEBS Letters. 174:102-111

A model has been constructed using computer graphics for human renin based on the sequence derived from that of the gene and the 3-dimensional structure defined at high resolution for other homologous aspartic proteinases. Human renin can adopt a 3-d

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bea27f521be4fe4dfd43c41c5ef12e39
https://doi.org/10.1016/0014-5793(84)81086-8

Zobrazit plný text záznamu

ChemInform Abstract: EIN NEUER WEG ZU PHENAZIN-5,10-DIOXIDEN UND VERWANDTEN VERBINDUNGEN

Autor: J. D. Johnston, M. J. Abu El-Haj, Beryl W. Dominy, Makhluf J. Haddadin, Costas H. Issidorides

Publikováno v: Chemischer Informationsdienst. 3

Bei der Umsetzung der Benzofurazan-N-oxide (Ia)-(Ic) mit den Phenolen (II) entstehen die Phenazin-5,10-dioxide (III) uber diskutierte Zwischenstufen.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7ff2a23d65862663e700950bbefe081b
https://doi.org/10.1002/chin.197224340

Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání