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Your search keyword '"Louis Locco"' showing total 2 results
Start Over Author "Louis Locco" Journal bioorganic & medicinal chemistry letters
2 results on '"Louis Locco"'

1. 6H-Benzo[c]chromen-6-one derivatives as selective ERβ agonists

Author

Milton L. Hammond, Elizabeth T. Birzin, Wanying Sun, Lovji D. Cama, Louis Locco, Ralph T. Mosley, Susan P. Rohrer, and Sudha Warrier

Subjects
Agonist, Molecular model, Stereochemistry, medicine.drug_class, Fluoroimmunoassay, Clinical Biochemistry, Pharmaceutical Science, Ligands, Biochemistry, Chemical synthesis, Structure-Activity Relationship, Drug Discovery, Coactivator, Benzene Derivatives, Tumor Cells, Cultured, polycyclic compounds, medicine, Estrogen Receptor beta, Humans, Structure–activity relationship, Benzopyrans, Molecular Biology, chemistry.chemical_classification, Molecular Structure, Chemistry, Organic Chemistry, Estrogen Receptor alpha, General Medicine, Selective estrogen receptor modulator, Molecular Medicine, Selectivity, hormones, hormone substitutes, and hormone antagonists, Lactone
Abstract

A series of 6H-benzo[c]chromen-6-one and 6H-benzo[c]chromene derivatives were prepared, and the affinity and selectivity for ERalpha and ERbeta was measured. Many of the analogs were found to be potent and selective ERbeta agonists. Bis hydroxyl at positions 3 and 8 is essential for activity in a HTRF coactivator recruitment assay. Additional modifications at both phenyl rings led to compounds with ERbeta10nM potency and100-fold selectivity over ERalpha.

Published
2006
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2. Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues

Author

Zhixiong Ye, Elizabeth T. Birzin, Meng-Hsin Chen, Louis Locco, Sheng-Shung Pong, Ravi P. Nargund, Rupa M. Parmar, Roy G. Smith, Ying-Duo Gao, Scott D. Feighner, Wanda W.-S. Chan, James M. Schaeffer, Arthur A. Patchett, Raman K. Bakshi, Allan D. Blake, Andrew D. Howard, and Susan P. Rohrer

Subjects
Models, Molecular, Agonist, Molecular model, medicine.drug_class, Clinical Biochemistry, Pharmaceutical Science, Receptors, Cell Surface, Carboxamide, Pharmacology, Biochemistry, Chemical synthesis, Receptors, G-Protein-Coupled, Inhibitory Concentration 50, Structure-Activity Relationship, chemistry.chemical_compound, Drug Discovery, medicine, Animals, Humans, Potency, Receptors, Ghrelin, Molecular Biology, Quinazolinone, Binding Sites, Human Growth Hormone, Chemistry, Organic Chemistry, In vitro, Rats, Kinetics, Drug Design, Quinazolines, Molecular Medicine, Secretagogue, Secretory Rate
Abstract

Quinazolinone derivatives were synthesized and evaluated as non-peptidic growth hormone secretagogues. Modeling guided design of quinazolinone compound 21 led to a potency enhancement of greater than 200-fold compared to human growth hormone secretagogue affinity of a screening lead 4.

Published
2000
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