Antiallergic activity of 2-phenyl-8-azapurin-6-ones
| Autor: | D. L. Pain, Stuart Malcolm Marshall, P. Knowles, P. Chaplen, Barbara J. Broughton, K. R. H. Wooldridge, Edward Lunt |
|---|---|
| Rok vydání: | 1975 |
| Předmět: |
Male
Aza Compounds Purinones Hydrogen bond Passive Cutaneous Anaphylaxis Anaphylactic reaction Substituent Ring (chemistry) Medicinal chemistry Rats Structure-Activity Relationship chemistry.chemical_compound chemistry Cromolyn Sodium Drug Discovery Disodium cromoglycate Hypersensitivity Animals Molecular Medicine Phenyl group Skin Tests |
| Zdroj: | Journal of Medicinal Chemistry. 18:1117-1122 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | The synthesis and antiallergic activity in the rat passive cutaneous anaphylactic reaction of a series of 2-phenyl-8-azapurin-6-ones are described. Early in the investigation, a linear free-energy equation was established in which the activity was related to the size and hydrogen bonding capacity of the ortho substituent in the phenyl ring. This relationship was used to provide guidance and limits for subsequent work leading to 2-o-propoxyphenyl-8-azapurin-6-one which is 40 times more potent than disodium cromoglycate. It is suggested that good antiallergic activity in this series is associated with coplanarity of the phenyl group with the azapurin-6-one which would be favored by a high degree of hydrogen bonding. |
| Databáze: | OpenAIRE |
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