Substituted pyrido[3,2-b]oxazin-3(4H)-ones: synthesis and evaluation of antinociceptive activity.
Bioorg Med Chem
; 6(2): 133-42, 1998 Feb.
Article
in En
| MEDLINE
| ID: mdl-9547936
ABSTRACT
A new series of N-substituted pyrido[3,2-b]oxazinones has been synthesized, pharmacologically evaluated, and compared with acetyl salicylic acid. The compound with the maximal combination of safety and analgesic efficacy was 4-¿3-[4-(4-fluorophenyl-1-piperazinyl)propyl]¿-2H-pyrido[3,2-b]-1, 4-oxazin-3(4H)-one (6c) with ED50 values of 12.5 mg/kg po (mouse phenylquinone writhing test) and 27.8 mg/kg po (rat acetic acid writhing test), respectively. Compound 6c proved to be more active than aspirin with a safety index of 5.1.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Oxazines
/
Pyridines
/
Nociceptors
/
Benzeneacetamides
/
Analgesics
Limits:
Animals
Language:
En
Journal:
Bioorg Med Chem
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
1998
Document type:
Article
Affiliation country:
Francia