Author: "Lindsay E. Glace" - Searchworks@Jio Institute Digital Library Search Results

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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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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

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

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