6533b7d3fe1ef96bd1260a5a
RESEARCH PRODUCT
Synthesis of New 2-{[(Phenoxy or Phenyl)acetyl]amino}benzoic Acid Derivatives as 3α-Hydroxysteroid Dehydrogenase Inhibitors and Potential Antiinflammatory Agents
Giuseppe DaidoneSalvatore PlesciaDomenico SchillaciM. L. Bajardisubject
3-Hydroxysteroid Dehydrogenasesmedicine.drug_classStereochemistryCarboxylic acidPharmaceutical ScienceCarboxamideEtherMicrobial Sensitivity TestsIn Vitro TechniquesChemical synthesischemistry.chemical_compoundAnti-Infective AgentsAcetyl chlorideYeastsDrug DiscoverymedicineAnthranilic acidAnimalsAminobenzoatesEnzyme InhibitorsBenzoic acidchemistry.chemical_classificationBacteriabiologyAnti-Inflammatory Agents Non-SteroidalAnti-Bacterial AgentsRatschemistryEnzyme inhibitorbiology.proteindescription
A number of 2-([(phenoxy or phenyl)acetyl]amino)benzoic acid derivatives were prepared in about 50% yield from (phenoxy or phenyl)acetyl chloride and anthranilic acid derivatives. All the compounds were tested as in vitro inhibitors of 3 alpha-hydroxysteroid dehydrogenase, since enzyme inhibition predicts potential antiinflammatory activity in vivo. The most active compounds 3 l, m, s are about 3.5 times more active than acetylsalicylic acid (ASA). Activity is influenced by electronic as well as steric effects.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 1995-10-01 | Archiv der Pharmazie |