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Your search keyword '"Lindsay E. Glace"' showing total 2 results
Start Over Author "Lindsay E. Glace" Topic administration, oral
2 results on '"Lindsay E. Glace"'

1. Discovery of orally active, pyrrolidinone-based progesterone receptor partial agonists

Author

Rakesh Nagilla, Sharada Manns, Eugene L. Stewart, Marlys Hammond, Tram H. Hoang, Scott K. Thompson, Walter Trizna, Chaya Duraiswami, Eugene T. Grygielko, Thuy B. Tran, James S. Frazee, Kevin P. Madauss, Johnson Latisha C, Shawn P. Williams, Lindsay E. Glace, David G. Washburn, and Jeffrey D. Bray

Subjects
Agonist, medicine.drug_class, Stereochemistry, Clinical Biochemistry, hERG, Administration, Oral, Pharmaceutical Science, Pharmacology, Biochemistry, Partial agonist, Structure-Activity Relationship, chemistry.chemical_compound, In vivo, Drug Discovery, Progesterone receptor, medicine, Animals, Humans, Pyrrolidinones, Molecular Biology, Binding Sites, biology, Organic Chemistry, Haplorhini, Ether-A-Go-Go Potassium Channels, Rats, Nuclear receptor, chemistry, biology.protein, Molecular Medicine, Receptors, Progesterone, Lead compound
Abstract

We have designed and synthesized a novel series of pyrrolidinones as progesterone receptor partial agonists. Compounds from this series had improved AR selectivity, rat pharmacokinetic properties, and in vivo potency compared to the lead compound. In addition, these compounds had improved selectivity against hERG channel inhibition.

Published
2009
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2. 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

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