Stephen A. Richards
GlaxoSmithKline
4 Papers
13 Citations
Stephen A. Richards is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Chemokine receptor & Reductase. The author has an hindex of 3, co-authored 4 publications.
Chat about Author
Papers
Discovery of GSK837149A, an inhibitor of human fatty acid synthase targeting the β-ketoacyl reductase reaction
María Jesús Vázquez,William J. Leavens,Ronggang Liu,Beatriz Rodriguez,Martin Read,Stephen A. Richards,Deborah A. Winegar,Juan Manuel Domínguez +7 more
TL;DR: Although initial results suggest that cell penetration for these compounds is impaired, they still can be regarded as useful tools with which to probe and explore the β‐ketoacyl reductase active site in FAS, helping in the design of new inhibitors.
57
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
Panayiotis A. Procopiou,Victoria J. Barrett,Nicola Bevan,Keith Biggadike,Peter R. Butchers,Diane M. Coe,Richard Conroy,Edney Dean David,Rita Field,Alison J. Ford,Stephen Barry Guntrip,Brian Edgar Looker,Iain M. McLay,Michael John Monteith,Valerie S. Morrison,Peter J. Mutch,Stephen A. Richards,Rosemary Sasse,Claire E. Smith +18 more
TL;DR: Sulfonamide 29b had the best profile of potency, selectivity, onset, andduration of action on both guinea pig trachea and human bronchus and was found to have low oral bioavailability in rat and dog and also to have long duration of action in an in vivo model of bronchodilation.
44
Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.
Panayiotis A. Procopiou,Christopher Browning,Paul Martin Gore,Sean M. Lynn,Stephen A. Richards,Robert J. Slack,Steven L. Sollis +6 more
TL;DR: The more potent and selective 6-azaphthalazinone core was used to append an H(3) receptor antagonist fragment, and to convert the series into the long acting single-ligand, dual H(1) H( 3) receptor receptor antagonist 44.
11
2,8-Diazaspiro[4.5]decan-8-yl)pyrimidin-4-amine potent CCR4 antagonists capable of inducing receptor endocytosis
Lena Shukla,Laura Ajram,Malcolm Begg,Brian Evans,Rebecca H. Graves,Simon Teanby Hodgson,Sean M. Lynn,Afjal Hussain Miah,Jonathan M. Percy,Panayiotis A. Procopiou,Stephen A. Richards,Robert J. Slack +11 more
TL;DR: A number of potent 2,8-diazaspiro CCR4 antagonists binding to the extracellular allosteric site were synthesised and were found to internalise about 60% of the cell surface receptors, a property which is not commonly shared by small molecule antagonists of chemokine receptors.
6