Synthesis of conformationally constrained 5,6,7, 8-Tetrahydroimidazo[1,5-a]pyridine inhibitors of farnesyltransferase.

doi:10.1021/OL0002424

Paper

DOI: 10.1021/OL0002424

Synthesis of conformationally constrained 5,6,7, 8-Tetrahydroimidazo[1,5-a]pyridine inhibitors of farnesyltransferase.

Published Oct 10, 2000 · C. Dinsmore, C. B. Zartman, Walter F. Baginsky

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Abstract

[reaction: see text] Synthesis of the 8-amino-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine ring system was accomplished by intramolecular cyclization of an iminium ion, derived from condensation of an amine and a substituted gamma-(1-imidazolyl)butyraldehyde. The reaction was used to produce conformationally restricted farnesyltransferase inhibitor analogues which exhibit improved in vivo metabolic stability.

Study Snapshot

This study developed conformationally restricted farnesyltransferase inhibitor analogues with improved in vivo metabolic stability by synthesising the 8-amino-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine ring system.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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