Benzopyrones. 14. Synthesis and anti-allergic properties of some N-tetrazolylcarboxamides and related compounds
| Autor: | G. P. Ellis, D. Shaw, C. J. Vardey, G. J. P. Becket, I. F. Skidmore, H. K. Wilson |
|---|---|
| Rok vydání: | 1978 |
| Předmět: |
Azoles
Male Tetrazoles In Vitro Techniques Histamine Release Medicinal chemistry Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Hypersensitivity medicine Animals Humans Structure–activity relationship Mast Cells Anaphylaxis Lung Chemistry Passive Cutaneous Anaphylaxis Cromolyn Sodium medicine.disease Rats Chromones Sodium cromoglycate Molecular Medicine Female Histamine |
| Zdroj: | Journal of Medicinal Chemistry. 21:1120-1126 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | A series of chromones containing an acidic group has been synthesized and screened for the ability to inhibit passive cutaneous anaphylaxis and the release of histamine from mast cells of the rat. Many of the chromones contain the N-(5-tetrazolyl)carboxamido group, a novel source of acidity. Others contain a carboxyl, C-(5-tetrazolyl), 5-(4H)-oxotetrazolinyl, or N-(5-tetrazolyl)sulfonamido function. The compounds were compared with cromolyn sodium (sodium cromoglycate) and many were found to be powerful inhibitors of anaphylaxis. The most potent was 7-methoxy-4-oxo-N-(5-tetrazolyl)-4H-1-benzopyran-2-carboxamide (15). Structure-activity relationships among the chromones and also some related compounds are discussed. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|