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Your search keyword '"IA Cumming"' showing total 2 results
Start Over Author "IA Cumming" Journal bioorganic medicinal chemistry letters
2 results on '"IA Cumming"'

1. A novel series of positive modulators of the AMPA receptor: structure-based lead optimization.

Author

Jamieson C, Campbell RA, Cumming IA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Maclean JK, Martin F, Moir EM, Morrow JA, Pantling J, Rankovic Z, and Smith L

Subjects
Allosteric Regulation, Amines chemical synthesis, Amines pharmacokinetics, Animals, Biological Availability, Crystallography, X-Ray, Humans, Models, Molecular, Pyrazoles chemical synthesis, Pyrazoles pharmacokinetics, Rats, Rats, Wistar, Receptors, AMPA chemistry, Stereoisomerism, Structure-Activity Relationship, Amines chemistry, Amines pharmacology, Drug Design, Pyrazoles chemistry, Pyrazoles pharmacology, Receptors, AMPA metabolism
Abstract

Starting from lead compound 1, we demonstrate how X-ray structural data can be used to understand SAR and expediently optimize bioavailability in a novel series of AMPA receptor modulators, furnishing 5 with improved bioavailability and robust in vivo activity., (Copyright © 2010 Elsevier Ltd. All rights reserved.)

Published
2010
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2. A novel series of positive modulators of the AMPA receptor: discovery and structure based hit-to-lead studies.

Author

Jamieson C, Basten S, Campbell RA, Cumming IA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Maclean JK, Moir EM, Morrow JA, Papakosta M, Rankovic Z, and Smith L

Subjects
Allosteric Regulation, Animals, Binding Sites, Crystallography, X-Ray, Drug Design, Drug Evaluation, Preclinical, High-Throughput Screening Assays, Humans, Indazoles chemical synthesis, Indazoles pharmacology, Microsomes metabolism, Protein Structure, Tertiary, Rats, Receptors, AMPA metabolism, Thiophenes chemical synthesis, Thiophenes pharmacology, Indazoles chemistry, Receptors, AMPA chemistry, Thiophenes chemistry
Abstract

Starting from an HTS derived hit 1, application of biostructural data facilitated rapid optimization to lead 22, a novel AMPA receptor modulator. This is the first demonstration of how structure based drug design can be exploited in an optimization program for a glutamate receptor., (Copyright © 2010 Elsevier Ltd. All rights reserved.)

Published
2010
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