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Your search keyword '"Schmidlin T"' showing total 2 results
Start Over Author "Schmidlin T" Publisher elsevier science ltd
2 results on '"Schmidlin T"'

1. Discovery and SAR of potent, orally available and brain-penetrable 5,6-dihydro-4H-3-thia-1-aza-benzo[e]azulen- and 4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulen derivatives as neuropeptide Y Y5 receptor antagonists.

Author

Rueeger H, Gerspacher M, Buehlmayer P, Rigollier P, Yamaguchi Y, Schmidlin T, Whitebread S, Nuesslein-Hildesheim B, Nick H, and Cricione L

Subjects
Administration, Oral, Animals, Azulenes, Biological Availability, Blood, Blood-Brain Barrier, Cycloheptanes pharmacology, Heterocyclic Compounds, 3-Ring chemical synthesis, Heterocyclic Compounds, 3-Ring pharmacokinetics, Heterocyclic Compounds, 3-Ring pharmacology, Heterocyclic Compounds, 4 or More Rings chemical synthesis, Heterocyclic Compounds, 4 or More Rings pharmacokinetics, Heterocyclic Compounds, 4 or More Rings pharmacology, Hypothalamus, Inhibitory Concentration 50, Rats, Structure-Activity Relationship, Cycloheptanes chemical synthesis, Cycloheptanes pharmacokinetics, Receptors, Neuropeptide Y antagonists & inhibitors
Abstract

Combination of structural elements from a potent Y5 antagonist (2) with thiazole fragments that exhibit weak Y5 affinities followed by lead optimisation led to the discovery of (5,6-dihydro-4H-3-thia-1-aza-benzo[e]azulen-2-yl)-piperidin-4-ylmethyl-amino and (4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulen-2-yl)-piperidin-4-ylmethyl-amino derivatives. Both classes of compounds are capable of delivering potent and selective orally and centrally bioavailable NPY Y5 receptor antagonists.

Published
2004
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2. Design, synthesis and SAR of a series of 2-substituted 4-amino-quinazoline neuropeptide Y Y5 receptor antagonists.

Author

Rueeger H, Rigollier P, Yamaguchi Y, Schmidlin T, Schilling W, Criscione L, Whitebread S, Chiesi M, Walker MW, Dhanoa D, Islam I, Zhang J, and Gluchowski C

Subjects
Drug Design, Models, Molecular, Quinazolines chemistry, Quinazolines pharmacology, Structure-Activity Relationship, Quinazolines chemical synthesis, Receptors, Neuropeptide Y antagonists & inhibitors
Abstract

The design of a novel series of NPY-Y5 receptor antagonists is described. Key elements for the design were the identification of weak Y5 hits from a Y1 program, results from a combinatorial approach and database mining. This led to the discovery of the quinazoline 4 and the aryl-sulphonamide moiety as major components of the pharmacophore for Y5 affinity. The synthesis and SAR towards CGP71683A is described.

Published
2000
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