Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Thomas 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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::79cebd31e4331d8b5aab573022f2e5ce
https://doi.org/10.1021/jm00096a018
https://doi.org/10.1021/jm00096a018
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::634fc359e90b5a4b3a2eb6a38fac940b
https://doi.org/10.1021/jm00088a021
https://doi.org/10.1021/jm00088a021
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)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cd885cee591a88eb6461a39e4f561bea
https://pubmed.ncbi.nlm.nih.gov/8642552
https://pubmed.ncbi.nlm.nih.gov/8642552
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c4916b337cd6a2d8d714e94e54e26f02
https://pubmed.ncbi.nlm.nih.gov/7629814
https://pubmed.ncbi.nlm.nih.gov/7629814
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7c2b563fdaafe883b62d28887646dc5f
https://pubmed.ncbi.nlm.nih.gov/7629813
https://pubmed.ncbi.nlm.nih.gov/7629813
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca57c9a61db0398a35beee1fa987bdeb
https://pubmed.ncbi.nlm.nih.gov/2153816
https://pubmed.ncbi.nlm.nih.gov/2153816
Autor:
Thomas Henry Brown, C. Robin Ganellin, Graham J. Durant, Terence F. Walker, D.Anthony Rawlings, Michael E. Parsons, Robert Blakemore, John Colin Emmett
Publikováno v:
European Journal of Medicinal Chemistry. 23:53-62
A series of 2-[2-(5-methyl-4-imidazolylmethylthio)ethylamino]-4-pyrimidones was prepared based on cimetidine 1. The model compound 4 has modest H2-antagonist activity as shown by its ability to antagonise histamine-stimulated tachycardia in guinea pi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6496bc5c9b0ce79e58fbb39f35913f7f
https://doi.org/10.1016/0223-5234(88)90167-5
https://doi.org/10.1016/0223-5234(88)90167-5
Publikováno v:
Fundamental and Applied Toxicology. 7:533-546
Triamterene (2,4,7-triamino-6-phenylpteridine), a widely used diuretic/antihypertensive agent with weak antifolate activity, has been found to be positive in several in vitro assays for mutagenicity. The present studies were undertaken to characteriz
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::dbc2ab17f7fc8482a952b4394a8f116b
https://doi.org/10.1016/0272-0590(86)90104-1
https://doi.org/10.1016/0272-0590(86)90104-1
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d3ee11f9e457cf477c7443c4b93ae6ad
https://doi.org/10.1021/jm00398a028
https://doi.org/10.1021/jm00398a028
Autor:
G. J. Durant, Robert Blakemore, Terence F. Walker, Michael E. Parsons, A. C. Rasmussen, P. Blurton, Thomas Henry Brown, D. A. Rawlings, Charon R. Ganellin
Publikováno v:
European Journal of Medicinal Chemistry. 24:65-72
A series of 2-[2-(5-methyl-4-imidazolylmethylthio)ethylamino]-4-pyrimidones was synthesised based on oxmetidine 2 , in which the methylenedioxyphenyl group of 2 was replaced by a heterocyclic ring. Good H 2 -receptor antagonist activity was retained
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3e087314af44503cd3205a372c99ac1b
https://doi.org/10.1016/0223-5234(89)90166-9
https://doi.org/10.1016/0223-5234(89)90166-9