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Your search keyword '"Luciana Turchetto"' showing total 1 results
Start Over Author "Luciana Turchetto" Publisher wiley
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1. A New Synthetic Approach of N-(4-Amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide (JTC-801) and Its Analogues and Their Pharmacological Evaluation as Nociceptin Receptor (NOP) Antagonists

Author

Isabella Sestili, Daniela Riitano, Anna Borioni, Andrea Rodomonte, Maria Sbraccia, Maria Rosaria Del Giudice, Carlo Mustazza, and Luciana Turchetto

Subjects
medicine.drug_class, Stereochemistry, Narcotic Antagonists, JTC-801, NOP, Molecular Conformation, Carboxamide, Calorimetry, In Vitro Techniques, Binding, Competitive, Chemical synthesis, Nociceptin Receptor, Structure-Activity Relationship, chemistry.chemical_compound, GTP-Binding Proteins, Drug Discovery, medicine, Humans, Potency, Benzamide, Pharmacology, Dose-Response Relationship, Drug, Molecular Structure, Organic Chemistry, Quinoline, Antagonist, General Medicine, Nociceptin receptor, Logistic Models, Opioid Peptides, chemistry, Guanosine 5'-O-(3-Thiotriphosphate), Benzamides, Receptors, Opioid, Aminoquinolines, Pharmacophore, Protein Binding, medicine.drug
Abstract

A series of 4-amino-2-methylquinoline and 4-aminoquinazoline derivatives, including the reference NOP antagonist JTC-801, were synthesized by an alternative pathway and their in vitro pharmacological properties were investigated. 3-Substitution of the quinoline ring resulted very critical for affinity. So 3-methyl derivative 4j showed a similar potency compared with the reference 4h while bulky lipophilic or electron withdrawing groups in the same position strongly decreased affinity. Structural and conformational requirements for affinity were outlined by NOE NMR and computational methods and suggestions for a pharmacophore model design were provided.

Published
2005
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