Optimization and metabolic stabilization of a class of nonsteroidal glucocorticoid modulators.

Bioorg Med Chem Lett

Metabolic Disease Research, Abbott Laboratories, Dept 4CB, Bldg. AP-10, Rm. L-14, 100 Abbott Park Road, Abott Park, IL 60064-6098, USA.

Published: August 2004

The optimization of a series of nonsteroidal glucocorticoid modulators is reported. Potent selective GR ligands that have improved metabolic stability were discovered typified by the subnanomolar acid 12 (GR binding IC(50)=0.6 nM).

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http://dx.doi.org/10.1016/j.bmcl.2004.06.023DOI Listing

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