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Synthesis and antiallergy activity of 10-oxo-10H-pyrido[1,2-a]thieno[3,2-d]pyrimidines and 10-oxo-10H-pyrido[1,2-a]thieno[3,4-d]pyrimidines
- Source :
- Journal of medicinal chemistry. 27(4)
- Publication Year :
- 1984
-
Abstract
- Synthesis and antiallergy activity of 10-oxo-10H-pyrido[1,2-a]thieno[3,2-d]pyrimidines (2 and 3) and 10-oxo-10H-pyrido[1,2-a]thieno[3,4-d]pyrimidines (4 and 5) are described. The activity, shown by these compounds in the rat passive cutaneous anaphylaxis (PCA) test, is compared to the PCA data previously reported for a series of 4-oxo-4H-pyrido[1,2-a]thieno[2,3-d]pyrimidines. 10-Oxo-N-1H-tetrazol-5-yl-10H-pyrido[1,2-a]thieno[3,4-d]pyri midine (2b), 10-oxo-7-(1H-tetrazol-5-yl)-10H-pyrido[1,2-a]thieno[3,4-d]py rimidine (4e), and 3,10-dihydro-10-oxo-7-(1H-tetrazol-5-yl)-1H-pyrido[1,2-a]thieno[3, 4-d] pyrimidine (7e) gave a 100% inhibition in the rat PCA test at a dose of 5 mg/kg. The activity displayed by these compounds is comparable to that of the most active compounds in the 4-oxo-4H-pyrido[1,2-a]thieno[2,3-d]pyrimidine series.
- Subjects :
- Pyrimidine
Stereochemistry
Pyridines
Passive Cutaneous Anaphylaxis
Biological activity
Thiophenes
Rats
chemistry.chemical_compound
Structure-Activity Relationship
Pyrimidines
chemistry
Drug Discovery
Lactam
Histamine H1 Antagonists
Molecular Medicine
Animals
Biological Assay
Indicators and Reagents
Subjects
Details
- ISSN :
- 00222623
- Volume :
- 27
- Issue :
- 4
- Database :
- OpenAIRE
- Journal :
- Journal of medicinal chemistry
- Accession number :
- edsair.doi.dedup.....e8d0be907cbfe14373f5f6a18a9561ef