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3 results on '"Pimm AD"'

1. The discovery of novel, potent and highly selective inhibitors of inducible nitric oxide synthase (iNOS).

Author

Cheshire DR, Åberg A, Andersson GM, Andrews G, Beaton HG, Birkinshaw TN, Boughton-Smith N, Connolly S, Cook TR, Cooper A, Cooper SL, Cox D, Dixon J, Gensmantel N, Hamley PJ, Harrison R, Hartopp P, Käck H, Leeson PD, Luker T, Mete A, Millichip I, Nicholls DJ, Pimm AD, St-Gallay SA, and Wallace AV

Subjects
Animals, Binding Sites, Computer Simulation, Crystallography, X-Ray, Drug Evaluation, Preclinical, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors pharmacology, Humans, Isoxazoles chemical synthesis, Isoxazoles pharmacology, Mice, Microsomes, Liver metabolism, Nitric Oxide Synthase Type II metabolism, Protein Structure, Tertiary, Pyridines pharmacology, Rats, Enzyme Inhibitors chemistry, Isoxazoles chemistry, Nitric Oxide Synthase Type II antagonists & inhibitors, Pyridines chemistry
Abstract

By careful analysis of experimental X-ray ligand crystallographic protein data across several inhibitor series we have discovered a novel, potent and selective series of iNOS inhibitors exemplified by compound 8., (Copyright © 2011 Elsevier Ltd. All rights reserved.)

Published
2011
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2. Discovery of potent and selective adamantane-based small-molecule P2X(7) receptor antagonists/interleukin-1beta inhibitors.

Author

Furber M, Alcaraz L, Bent JE, Beyerbach A, Bowers K, Braddock M, Caffrey MV, Cladingboel D, Collington J, Donald DK, Fagura M, Ince F, Kinchin EC, Laurent C, Lawson M, Luker TJ, Mortimore MM, Pimm AD, Riley RJ, Roberts N, Robertson M, Theaker J, Thorne PV, Weaver R, Webborn P, and Willis P

Subjects
Adamantane pharmacology, Animals, Benzamides pharmacology, Blood Proteins metabolism, Crystallography, X-Ray, Humans, In Vitro Techniques, Molecular Conformation, Monocytes metabolism, Protein Binding, Rats, Receptors, Purinergic P2X7, Structure-Activity Relationship, Adamantane analogs & derivatives, Adamantane chemical synthesis, Benzamides chemical synthesis, Interleukin-1beta antagonists & inhibitors, Purinergic P2 Receptor Antagonists
Abstract

A novel series of antagonists of the human P2X7 receptor is described. Modification of substituents enabled identification of compounds selective for the rat P2X7 receptor and provides useful pharmacological tools for evaluation of the role of P2X7 in disease.

Published
2007
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3. 1,2-Dihydro-4-quinazolinamines: potent, highly selective inhibitors of inducible nitric oxide synthase which show antiinflammatory activity in vivo.

Author

Tinker AC, Beaton HG, Boughton-Smith N, Cook TR, Cooper SL, Fraser-Rae L, Hallam K, Hamley P, McInally T, Nicholls DJ, Pimm AD, and Wallace AV

Subjects
Acute Disease, Administration, Oral, Amines chemical synthesis, Amines chemistry, Amines pharmacology, Animals, Arthritis, Experimental drug therapy, Cell Line, Chronic Disease, Enzyme Inhibitors chemistry, Enzyme Inhibitors pharmacology, Injections, Intravenous, Isoenzymes antagonists & inhibitors, Nitric Oxide Synthase Type II, Quinazolines chemistry, Quinazolines pharmacology, Rats, Spiro Compounds chemical synthesis, Spiro Compounds chemistry, Spiro Compounds pharmacology, Structure-Activity Relationship, Enzyme Inhibitors chemical synthesis, Nitric Oxide Synthase antagonists & inhibitors, Quinazolines chemical synthesis
Abstract

The discovery of a novel class of nitric oxide synthase (NOS) inhibitors, 2-substituted 1,2-dihydro-4-quinazolinamines, and the related 4'-aminospiro[piperidine-4,2'(1'H)-quinazolin]-4'-amines is described. Members of both series exhibit nanomolar potency and high selectivity for the inducible isoform of the enzyme (i-NOS) relative to the constitutive isoforms in vitro. Efficacy in acute and chronic animal models of inflammatory disease following oral administration has also been demonstrated using these compounds.

Published
2003
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