Search

Your search keyword '"Lindsay E. Glace"' showing total 2 results
Start Over Author "Lindsay E. Glace" Journal bioorganicmedicinal chemistry letters
2 results on '"Lindsay E. Glace"'

1. Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists

Author

Eugene T. Grygielko, Shawn P. Williams, Lindsay E. Glace, Jeffrey D. Bray, Chaya Duraiswami, James S. Frazee, Kevin P. Madauss, David G. Washburn, Tram H. Hoang, Leahann Lapinski, Walter Trizna, Nicholas J. Laping, and Scott K. Thompson

Subjects
Agonist, Pyrrolidines, medicine.drug_class, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Administration, Oral, Crystallography, X-Ray, Biochemistry, Partial agonist, Pyrrolidine, chemistry.chemical_compound, Drug Discovery, Progesterone receptor, medicine, Animals, Computer Simulation, Molecular Biology, Hormone binding protein, Binding Sites, Organic Chemistry, Rational design, Protein Structure, Tertiary, Rats, chemistry, Nuclear receptor, Estrogen, Drug Design, Models, Animal, Molecular Medicine, Receptors, Progesterone
Abstract

Using the X-ray crystal structure of an amide-based progesterone receptor (PR) partial agonist bound to the PR ligand binding domain, a novel PR partial agonist class containing a pyrrolidine ring was designed. Members of this class of N-alkylpyrrolidines demonstrate potent and highly selective partial agonism of the progesterone receptor, and one of these analogs was shown to be efficacious upon oral dosing in the OVX rat model of estrogen opposition.

Published
2009

2. Synthesis and SAR of amino acid-derived heterocyclic progesterone receptor full and partial agonists

Author

Jaclyn R. Patterson, Scott K. Thompson, Harvey E. Fries, Eugene T. Grygielko, Walter Trizna, Tram H. Hoang, Jeffrey D. Bray, Nicholas J. Laping, Douglas J. Minick, Melanie Nord, Lindsay E. Glace, Rakesh Nagilla, Marlys Hammond, Sharada Manns, and David G. Washburn

Subjects
Agonist, medicine.drug_class, Stereochemistry, Clinical Biochemistry, Triazole, Pharmaceutical Science, Tetrazoles, Biochemistry, Chemical synthesis, Partial agonist, chemistry.chemical_compound, Structure-Activity Relationship, Drug Discovery, Progesterone receptor, medicine, Structure–activity relationship, Animals, Tetrazole, Amino Acids, Molecular Biology, chemistry.chemical_classification, Organic Chemistry, Amino acid, Rats, chemistry, Molecular Medicine, Receptors, Progesterone
Abstract

Two classes of amino acid-derived heterocyclic progesterone receptor ligands were developed to address the metabolic issues posed by the dimethyl amide functionality of the lead compound (1). The tetrazole-derived ligands behaved as potent partial agonists, while the 1,2,4-triazole ligands behaved as potent full agonists.

Published
2009

Catalog

Books, media, physical & digital resources
See catalog results