Synthesis and evaluation of a new series of 1'-cyclobutyl-6-(4-piperidyloxy)spiro[benzopyran-2,4'-piperidine] derivatives as high affinity and selective histamine-3 receptor (H3R) antagonists.

doi:10.1016/j.bmcl.2012.01.139

Paper

Synthesis and evaluation of a new series of 1'-cyclobutyl-6-(4-piperidyloxy)spiro[benzopyran-2,4'-piperidine] derivatives as high affinity and selective histamine-3 receptor (H3R) antagonists.

Published Mar 15, 2012 · R. Dandu, J. Lyons, R. Raddatz

Bioorganic & medicinal chemistry letters

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10

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Abstract

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In Vitro Study

Study Snapshot

Spirobenzopyran piperidine ether analogs show high affinity and selectivity against histamine-3 receptors, with acceptable in vitro liver microsomal stability and selectivity against CYP P450 enzymes.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Synthesis and evaluation of a new series of 1'-cyclobutyl-6-(4-piperidyloxy)spiro[benzopyran-2,4'-piperidine] derivatives as high affinity and selective histamine-3 receptor (H3R) antagonists.

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