Indolo[2,1-c][1,4]benzodiazepines: a new class of antiallergic agents
| Autor: | Chih Y. Ho, William Hageman, Francis J. Persico |
|---|---|
| Rok vydání: | 1986 |
| Předmět: |
Ketotifen
Male Serotonin Indoles Stereochemistry medicine.drug_class medicine.medical_treatment Guinea Pigs In vivo tests Amidine chemistry.chemical_compound Benzodiazepines Drug Discovery Cromolyn Sodium medicine Hypersensitivity Animals Anaphylaxis Benzodiazepine Chemistry Passive Cutaneous Anaphylaxis Biological activity Rats Inbred Strains Rats Antiallergic agent Histamine H1 Antagonists Molecular Medicine Antihistamine Oxatomide medicine.drug |
| Zdroj: | Journal of medicinal chemistry. 29(6) |
| ISSN: | 0022-2623 |
| Popis: | A series of 12-(cyclic alkylamino)-6H-indolo[2,1-c][1,4]benzodiazepines were synthesized that possess antihistamine and antiserotonin activities as well as ability to inhibit mediator release. Compound 6a, 12-(4-methyl-1-piperazinyl)-6H-indolo[2,1-c][1,4]benzodiazepine was a more potent inhibitor of serotonin release than disodium cromoglycate (DSCG) and ketotifen and approximately equivalent to oxatomide. In the in vivo tests (PCA and ALA), compound 6a was equivalent or superior to DSCG and oxatomide. These agents have potential for the treatment of a variety of allergic conditions. |
| Databáze: | OpenAIRE |
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