Back to Search
Start Over
Isoxazole derivatives as centrally acting muscle relaxants. I Synthesis and activity of 5-(3-aminopropyl)amino-3-phenylisoxazole derivatives
- Source :
- Chemical and Pharmaceutical Bulletin. 34:1634-1642
- Publication Year :
- 1986
- Publisher :
- Pharmaceutical Society of Japan, 1986.
-
Abstract
- A series of 5-amino-3-phenylisoxazole derivatives was synthesized and evaluated as part of a search for new types of centrally acting muscle relaxants. The derivtives with an alkylaminopropyl moiety exhibited muscle relaxant activity comparable to that of tolperisone (1), but this activity was accompanied by strong general central nervous system (CNS) depressant and slight anticonvulsant activities.On the other hand, the derivative with a propanamide moiety exhibited a favorable pharmacological profile for a selective muscle relaxant with little CNS depressant action.
- Subjects :
- Male
Tolperisone
Chemical Phenomena
medicine.drug_class
Stereochemistry
medicine.medical_treatment
Mice
chemistry.chemical_compound
Drug Discovery
medicine
Animals
Moiety
Isoxazole
Oxazoles
Mice, Inbred ICR
Muscle Relaxants, Central
Rats, Inbred Strains
Biological activity
Muscle relaxant
Isoxazoles
General Chemistry
General Medicine
Propanamide
Rats
Chemistry
Anticonvulsant
chemistry
Anticonvulsants
Depressant
medicine.drug
Subjects
Details
- ISSN :
- 13475223 and 00092363
- Volume :
- 34
- Database :
- OpenAIRE
- Journal :
- Chemical and Pharmaceutical Bulletin
- Accession number :
- edsair.doi.dedup.....0b725f9434b743cfbbfa1a2f1e921096