Zobrazeno 1 - 7
of 7
pro vyhledávání: '"Henry Brown"'
Autor:
Leach Colin Andrew, David R. Reavill, Kenneth Wiggall, Colin J. Theobald, David J. Keeling, Robert John Ife, Thomas Henry Brown, Malcolm L. Meeson, Michael E. Parsons
Publikováno v:
Journal of Medicinal Chemistry. 35:3413-3422
Previously, gastric (H+/K+)-ATPase inhibitors such as 2 have been prepared as analogues of 1a on the presumption that the 3-carbethoxy substituent plays a key role in establishing the orientation of the 4-arylamino group. In this paper we explore fur
Autor:
Michael E. Parsons, Leach Colin Andrew, Kenneth Wiggall, David J. Keeling, Thomas Henry Brown, Carolyn A. Price, Shiona M. Laing, Robert John Ife
Publikováno v:
Journal of Medicinal Chemistry. 35:1845-1852
Further work on compounds 1 has identified the 4-position as a site where substantial modifications are tolerated, leading to analogues which are more potent and less toxic than those described previously. The best compound in the series is 13a (SK&F
Autor:
Stephen A. Smith, Geoffrey Stemp, Derek N. Middlemiss, Graham J. Riley, Izzy Boyfield, Maureen A.M. Healy, David G. Cooper, Ron J. King, Amanda Johns, Martyn C. Coldwell, Thomas Henry Brown, David John Nash, Jim J. Hagan, Emma E. Scott, Michael S. Hadley
Publikováno v:
Journal of medicinal chemistry. 39(10)
Autor:
Leach Colin Andrew, David J. Keeling, Colin J. Theobald, Malcolm L. Meeson, Robert John Ife, Michael E. Parsons, Peter Blurton, Thomas Henry Brown
Publikováno v:
Journal of medicinal chemistry. 38(14)
Quinazolines bearing a secondary 4-(arylamino) substituent demonstrate an SAR for inhibition of the gastric (H + /K + )-ATPase different from the previously described 3-acylquinolines, suggesting that, although these compounds are also K + -competiti
Autor:
Robert John Ife, Leach Colin Andrew, Kenneth Wiggall, Thomas Henry Brown, Michael E. Parsons, Colin J. Theobald, David J. Keeling
Publikováno v:
Journal of medicinal chemistry. 38(14)
3-Acyl-4-(arylamino)quinolines were previously identified as gastric (H + /K + )-ATPase inhibitors, and clinical efficacy has been demonstrated for compound 3 (SK&F 96067). In the present study the further structure-activity relationship of this seri
Autor:
Leach Colin Andrew, Kenneth Wiggall, David R. Reavill, David J. Keeling, Shiona M. Laing, Thomas Henry Brown, Robert John Ife, Michael E. Parsons, Carolyn A. Price
Publikováno v:
Journal of medicinal chemistry. 33(2)
The 4-(arylamino)quinoline 4, previously described as an antiulcer compound, is shown to be an inhibitor of the gastric (H+/K+)-ATPase. It is postulated that 1-arylpyrrolo[3,2-c]quinolines 6 act as conformationally restrained analogues of 4. A series
Autor:
D. Saunders, I R Smith, R Griffiths, M Jones, N. E. Sore, R. C. Mitchell, K K Rana, Rodney C. Young, Thomas Henry Brown, Charon Robin Ganellin
Publikováno v:
Journal of Medicinal Chemistry. 31:656-671
A rational approach to the design of centrally acting agents is presented, based initially upon a comparison of the physicochemical properties of three typical histamine H2 receptor antagonists which do not readily cross the blood-brain barrier with