The influence of drug-like concepts on decision-making in medicinal chemistry
PD Leeson, B Springthorpe - Nature reviews Drug discovery, 2007 - nature.com
The application of guidelines linked to the concept of drug-likeness, such as the'rule of five',
has gained wide acceptance as an approach to reduce attrition in drug discovery and …
has gained wide acceptance as an approach to reduce attrition in drug discovery and …
From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis
B Springthorpe, A Bailey, P Barton… - Bioorganic & medicinal …, 2007 - Elsevier
Starting from adenosine triphosphate (ATP), the identification of a novel series of P2Y 12
receptor antagonists and exploitation of their SAR is described. Modifications of the acidic side …
receptor antagonists and exploitation of their SAR is described. Modifications of the acidic side …
Overcoming undesirable HERG potency of chemokine receptor antagonists using baseline lipophilicity relationships
…, S Ivanova, B Nordén, B Springthorpe… - Journal of medicinal …, 2008 - ACS Publications
The inhibition of the hERG channel by noncardiovascular drugs is a side effect that severely
impedes the development of new medications. To increase hERG selectivity of preclinical …
impedes the development of new medications. To increase hERG selectivity of preclinical …
Scaffold-hopping with zwitterionic CCR3 antagonists: identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of …
…, MWD Perry, RJ Riley, E Roe, B Springthorpe… - Bioorganic & medicinal …, 2012 - Elsevier
… Riley c , Emma Roe c , Brian Springthorpe a , Linda Stein a , Peter Webborn c … Bahl, A.;
Barton, P.; Bowers, K.; Brough, S.; Evans, R.; Luckhurst, CA; Mochel, T.; Perry, MWD; Rigby …
Barton, P.; Bowers, K.; Brough, S.; Evans, R.; Luckhurst, CA; Mochel, T.; Perry, MWD; Rigby …
The discovery of CCR3/H1 dual antagonists with reduced hERG risk
…, H Sanganee, A Sisson, B Springthorpe - Bioorganic & medicinal …, 2012 - Elsevier
A series of dual CCR3/H 1 antagonists based on a bispiperidine scaffold were discovered.
Introduction of an acidic group overcame hERG liability. Bioavailability was optimised by …
Introduction of an acidic group overcame hERG liability. Bioavailability was optimised by …
Which hydroxy? Evidence for species differences in the regioselectivity of glucuronidation in rat, dog, and human in vitro systems and dog in vivo
…, IG Beattie, CA Martin, RJ Riley, B Springthorpe - Drug metabolism and …, 2006 - ASPET
The glucuronidation of (1S,2R,3R,5R)-3-(hydroxymethyl)-5-[7-{[(1R,2S)-2-phenylcyclopropyl]amino}-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl]cyclopentane-1,2-diol
(…
(…
Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H1 antagonists. Part II: Optimising in vivo clearance
…, A Rigby, R Riley, M Soars, B Springthorpe… - Bioorganic & medicinal …, 2012 - Elsevier
The second part of this communication focuses on the resolution of issues surrounding the
series of hydroxyamide phenoxypiperidine CCR3/H 1 dual antagonists described in Part I. …
series of hydroxyamide phenoxypiperidine CCR3/H 1 dual antagonists described in Part I. …
Chemokine CCR3 antagonists
A Bahl, B Springthorpe, R Riley - New drugs and targets for asthma and …, 2010 - karger.com
Chemokines are a superfamily of small molecular mass proteins (~ 8–10 kDa) and are
characterized by their actions on distinct subtypes of leukocytes. Chemokines exert their effects …
characterized by their actions on distinct subtypes of leukocytes. Chemokines exert their effects …
Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H1 antagonists. Part I
…, A Rigby, R Riley, M Soars, B Springthorpe… - Bioorganic & medicinal …, 2012 - Elsevier
The discovery of potent small molecule dual antagonists of the human CCR3 and H 1
receptors is described for the treatment of allergic diseases, for example, asthma and allergic …
receptors is described for the treatment of allergic diseases, for example, asthma and allergic …
[PDF][PDF] DMD# 9282
…, IG Beattie, CA Martin, RJ Riley, B Springthorpe - 2006 - Citeseer
Abbreviations: HPLC, high-performance liquid chromatography; MS, mass spectrometry;
NMR, nuclear magnetic resonance; ROESY, rotating-frame Overhauser effect spectroscopy; …
NMR, nuclear magnetic resonance; ROESY, rotating-frame Overhauser effect spectroscopy; …