Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Robert Antony David Hull"'
Autor:
Wei Xun, Elliot Lilley, James W. Black, Gillian F. Watt, Paul Wright, Elaine Anne Harper, David A. Sykes, Sonia P. Roberts, Laurence Wright, David John Dunstone, Ildiko Maria Buck, Martin Keith Walker, S. Barret Kalindjian, Ian D. Linney, Iain Mair Mcdonald, Mark E. Shaxted, Eric P. Griffin, John Spencer, Robert Antony David Hull, Michael John Pether, Katherine Isobel Mary Steel
Publikováno v:
Journal of Medicinal Chemistry. 50:3101-3112
Starting from a novel, achiral 1,3,4-benzotriazepine-based CCK2 receptor antagonist, a process of optimization has afforded further compounds of this type that maintain the nanomolar affinity for recombinant, human CCK2 receptors and high selectivity
Autor:
S. Barret Kalindjian, Robert Antony David Hull, Howard B. Broughton, James W. Black, Ildiko Maria Buck, Caroline M. R. Low, Katherine Isobel Mary Steel, David John Dunstone, and Nigel P. Shankley, Jonathan Michael Richard Davies, Iain Mair Mcdonald, Michael John Pether
Publikováno v:
Journal of Medicinal Chemistry. 43:3505-3517
The two hormones cholecystokinin and gastrin share the same C-terminal sequence of amino acids, namely Gly(29)-Trp(30)-Met(31)-Asp(32)-Phe(33)-NH(2). Nevertheless, this congruence has not precluded using this structure to develop selective ligands fo
Publikováno v:
British Journal of Pharmacology. 115:356-360
1. rK10, a weak T-kininogenase isolated from the rat submandibular gland, is a protein belonging to the rat kallikrein family. In the present work, we have studied the biological effects of rK10 with respect to its ability to alter vascular resistanc
Synthesis and pharmacological properties of BW315c and other inotropic 2-arylimidazo[1,2-a]pyrazines
Autor:
Robert Antony David Hull, P. Randall, James W. Black, S. J. Vine, Heather Giles, V. Paul Gerskowitch, David Cambridge, Ramachandran Iyer, Shah Gita Punjabhai, David Stone, Malcolm Stuart Nobbs, Mark V. Whiting, Robert C. Glen, W. Richard King, Paul Barraclough
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 3:509-514
A series of 2-aryl imidazo[1,2-a]pyrazines has been prepared and evaluated for inotropic activity. Sulphoxide 12, BW315C, displayed potent inotropic effects having comparable in vitro and vivo inotropic potencies to those of isomazole. Structure-acti
Publikováno v:
Biochemical Journal. 281:819-828
The submandibular gland of the rat contains several enzymes belonging to the kallikrein family. These include tissue kallikrein, antigen gamma (T-kininogenase), esterase B and tonin. In the present study, a new member of this family, which we have na
Autor:
V. Paul Gerskowitch, David Cambridge, Mark V. Whiting, Janet M. Gillam, Robert Antony David Hull, Paul Barraclough, Steven Smith, Shah Gita Punjabhai, Ramachandran Iyer, Heather Giles, P. Randall, Robert C. Glen, James W. Black, David Firmin
Publikováno v:
Archiv der Pharmazie. 325:225-234
Aryl substituted 1H-imidazo[1, 2-a]imidazole 8, imidazo[2,1-b]thiazole 9, 1,4-dihydroimidazo[4,5-d]imidazole 11, and 1(2),4-dihydroimidazo[4,5-c]pyrazoles 12–17 have been prepared. An X-ray crystallographic study confirmed the structure of 8 and sh
Autor:
Eric P. Griffin, John Gaffen, Sonia P. Roberts, Mark E. Shaxted, David John Dunstone, S. Barret Kalindjian, Robert Antony David Hull, David A. Sykes, Ian D. Linney, John Spencer, Elaine Anne Harper, Katherine Isobel Mary Steel, Iain Mair Mcdonald, Ildiko Maria Buck, Michelle Raynor, Wei Xun, Michael John Pether, Dipa Patel, Paul Wright, Carol Austin, Caroline M. R. Low
Publikováno v:
Journal of medicinal chemistry. 50(20)
A 1,3,4-benzotriazepine was identified as a suitable lead in our effort toward obtaining a non-peptide parathyroid hormone-1 receptor (PTH1R) antagonist. A process of optimization afforded derivatives displaying nanomolar PTH1R affinity, a representa
Autor:
James W. Black, Katherine Isobel Mary Steel, Ildiko Maria Buck, Elliot Lilley, S. Barret Kalindjian, Sonia P. Roberts, Elaine Anne Harper, Mark E. Shaxted, David John Dunstone, Eric P. Griffin, Nigel P. Shankley, David A. Sykes, I. M. Mcdonald, Laurence Wright, Martin Keith Walker, Matthew J. Tozer, Michael John Pether, Paul Wright, Caroline M. R. Low, Ian D. Linney, Robert Antony David Hull, Gillian F. Watt, John Gaffen, Tracey Cooke
Publikováno v:
Journal of medicinal chemistry. 48(22)
The systematic optimization of the structure of a novel 2,4,5-trisubstituted imidazole-based cholecystokinin-2 (CCK(2)) receptor antagonist afforded analogues with nanomolar receptor affinity. These compounds were now comparable in their potency to t
Autor:
James W. Black, Heather Giles, D Firmin, Robert Antony David Hull, Paul Barraclough, Robert C. Glen, D. Collard, Alan Peter Hill, V.P. Gerskowitch, David Cambridge
Publikováno v:
Journal of medicinal chemistry. 33(8)
A series of "A" ring substituted sulmazole and isomazole analogues have been prepared and evaluated as inotropic agents. pKA's, protonation sites, and log P values were measured for selected compounds and their electronic properties were calculated.
Autor:
Mark V. Whiting, James W. Black, Clare O. Kneen, S. J. Vine, V. Paul Gerskowitch, Ramachandran Lyer, Shah Gita Punjabhai, Paul Barraclough, Steven Smith, David Cambridge, Malcolm Stuart Nobbs, Robert Antony David Hull, W. Richard King
Publikováno v:
Archiv der Pharmazie. 323(8)
A series of 2-substituted 1H-imidazo[4,5-b]pyridines and the isomeric 1H-imidazo[4,5-c]pyridine derivatives has been prepared and evaluated as inotropic agents. The 1H-imidazo-[4,5-b] derivatives were found to be consistently more potent than their i