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Your search keyword '"Crook, Barry"' showing total 3 results
Start Over Author "Crook, Barry" Journal bioorganic & medicinal chemistry letters
3 results on '"Crook, Barry"'

1. Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists

Author

Wilson, David M., Apps, James, Bailey, Nicholas, Bamford, Mark J., Beresford, Isabel J., Brackenborough, Kim, Briggs, Michael A., Brough, Stephen, Calver, Andrew R., Crook, Barry, Davis, Rebecca K., Davis, Robert P., Davis, Susannah, Dean, David K., Harris, Leanne, Heslop, Teresa, Holland, Vicky, Jeffrey, Phillip, Panchal, Terrance A., Parr, Christopher A., Quashie, Nigel, Schogger, Joanne, Sehmi, Sanjeet S., Stean, Tania O., Steadman, Jon G.A., Trail, Brenda, Wald, Jeffrey, Worby, Angela, Takle, Andrew K., Witherington, Jason, and Medhurst, Andrew D.

Published
2013
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2. The discovery of the benzazepine class of histamine H3 receptor antagonists

Author

Wilson, David M., Apps, James, Bailey, Nicholas, Bamford, Mark J., Beresford, Isabel J., Briggs, Michael A., Calver, Andrew R., Crook, Barry, Davis, Robert P., Davis, Susannah, Dean, David K., Harris, Leanne, Heightman, Tom D., Panchal, Terry, Parr, Christopher A., Quashie, Nigel, Steadman, Jon G.A., Schogger, Joanne, Sehmi, Sanjeet S., Stean, Tania O., Takle, Andrew K., Trail, Brenda K., White, Trevor, Witherington, Jason, Worby, Angela, and Medhurst, Andrew D.

Published
2013
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3. The discovery of the benzazepine class of histamine H3 receptor antagonists.

Author

Wilson, David M., Apps, James, Bailey, Nicholas, Bamford, Mark J., Beresford, Isabel J., Briggs, Michael A., Calver, Andrew R., Crook, Barry, Davis, Robert P., Davis, Susannah, Dean, David K., Harris, Leanne, Heightman, Tom D., Panchal, Terry, Parr, Christopher A., Quashie, Nigel, Steadman, Jon G.A., Schogger, Joanne, Sehmi, Sanjeet S., and Stean, Tania O.

Subjects
*BENZAZEPINES, *HISTAMINE, *ANTIHISTAMINES, *PHARMACODYNAMICS, *DRUG development, *PHARMACEUTICAL chemistry
Abstract

Abstract: This Letter describes the discovery of a novel series of H3 receptor antagonists. The initial medicinal chemistry strategy focused on deconstructing and simplifying an early screening hit which rapidly led to the discovery of a novel series of H3 receptor antagonists based on the benzazepine core. Employing an H3 driven pharmacodynamic model, the series was then further optimised through to a lead compound that showed robust in vivo functional activity and possessed overall excellent developability properties. [Copyright &y& Elsevier]

Published
2013
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