Acetamide scanning around bicyclic thiazoles: SAR at the H₃ receptor.

CHEMMEDCHEM(2011)

Cited 6|Views14
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Abstract
A surprisingly homogeneous SAR against the H3 receptor was revealed for positional acetamide isomers of bicyclic thiazoles fused to various cyclic amines. Pyrroline and azepine rings were used to probe the central position of the amide. In vitro ADMET parameters were measured, and the isomer with the best overall properties was assessed in vivo.
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Key words
bicyclic thiazoles,cognitive disorders,drug-like properties,histamine H-3 receptor,structure-activity relationships
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