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Your search keyword '"Haroldsen, Peter"' showing total 2 results
Start Over Author "Haroldsen, Peter" Journal bioorganic medicinal chemistry letters
2 results on '"Haroldsen, Peter"'

1. Benzobistriazinones and related heterocyclic ring systems as potent, orally bioavailable positive allosteric AMPA receptor modulators.

Author

Mueller R, Rachwal S, Varney MA, Johnson SA, Alisala K, Zhong S, Li YX, Haroldsen P, Herbst T, and Street LJ

Subjects
Administration, Oral, Allosteric Regulation, Animals, Binding Sites, Rats, Receptors, AMPA metabolism, Triazines chemical synthesis, Triazines pharmacokinetics, Heterocyclic Compounds chemistry, Receptors, AMPA chemistry, Triazines chemistry
Abstract

AMPA receptors (AMPARs) are an important therapeutic target in the CNS. A series of substituted benzobistriazinone, benzobispyrimidinone and related derivatives have been prepared with high potency and selectivity for the allosteric binding site of AMPARs. Further improvements have been made to previously reported series of positive AMPAR modulators and these compounds exhibit excellent in vivo activity and improved in vivo metabolic stability with up to 100% oral bioavailability in rat., (Copyright © 2011. Published by Elsevier Ltd.)

Published
2011
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2. Benzotriazinone and benzopyrimidinone derivatives as potent positive allosteric AMPA receptor modulators.

Author

Mueller R, Rachwal S, Lee S, Zhong S, Li YX, Haroldsen P, Herbst T, Tanimura S, Varney M, Johnson S, Rogers G, and Street LJ

Subjects
Allosteric Regulation, Animals, Drug Design, Hippocampus drug effects, Humans, Rats, Structure-Activity Relationship, Pyrimidinones chemistry, Pyrimidinones pharmacology, Receptors, AMPA metabolism, Triazines chemistry, Triazines pharmacology
Abstract

AMPA receptors (AMPARs) have been demonstrated to be an important therapeutic CNS target. A series of substituted benzotriazinone and benzopyrimidinone derivatives were prepared with the aim to improve in vivo activity over the previously reported bis-benzoxazinone based AMPAKINE series from our laboratory. These compounds were shown to be potent, positive allosteric AMPAR modulators that have better in vivo activity and improved metabolic stability over the analogous benzoxazinone derivatives., (Copyright © 2011 Elsevier Ltd. All rights reserved.)

Published
2011
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