N-Arylbenzamides: extremely simple scaffolds for the development of novel estrogen receptor agonists
| Autor: | Armando A. Genazzani, Paolo Minazzi, Giovanni B. Giovenzana, Pier Luigi Canonico, Antonio Caldarelli |
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| Rok vydání: | 2011 |
| Předmět: |
Agonist
Hydroxybenzoic acid medicine.drug_class Stereochemistry Drug Evaluation Preclinical Estrogen receptor Chemistry Techniques Synthetic Aminophenols Cell Line Small Molecule Libraries Structure-Activity Relationship Drug Discovery Hydroxybenzoates medicine Humans Structure–activity relationship Receptor Pharmacology Ligand Chemistry General Medicine Combinatorial chemistry Receptors Estrogen Estrogen Benzamides Pharmacophore |
| Zdroj: | Journal of Enzyme Inhibition and Medicinal Chemistry. 28:148-152 |
| ISSN: | 1475-6374 1475-6366 |
| DOI: | 10.3109/14756366.2011.642374 |
| Popis: | The research of estrogen receptor (ER) ligands has benefited in the last decade from the implementation of combinatorial chemistry. The general pharmacophore has been identified and subsequently a multitude of compounds have been synthesized. Surprisingly, up to now simple amides have not been taken into consideration. Here we show that amides resulting from the condensation of hydroxybenzoic acids with aminophenols result in compounds retaining the pharmacophore structure of an ER ligand with a clear estrogenic activity. |
| Databáze: | OpenAIRE |
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