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Isoxazole derivatives as centrally acting muscle relaxants. III. Synthesis and activity of conformationally restricted analogs
- Source :
- Chemicalpharmaceutical bulletin. 35(9)
- Publication Year :
- 1987
-
Abstract
- Conformationally restricted analogs of muscle-relaxant 3-amino-2-methyl-N- (3-phenyl-5-isoxazolyl) propanamides (1) and 5- (3-aminopropylamino) -3-phenylisoxazoles (2) were prepared, and their muscle-relaxant and other pharmacological activities were tested and compared with those of the corresponding acyclic derivatives. 7- (3-Diethylamino-2-methylpropanoyl) -3-phenyl-4, 5, 6, 7-tetrahydroisoxazolo [5, 4-b] pyridine (8) exhibited muscle-relaxant and anticonvulsant activities comparable with those of corresponding acyclic derivatives, i.e. 3-diethylamino-2-methyl-N- (3-phenyl-5-isoxazolyl) propanamides (1e-g), but other types of compounds showed decreased activities. The preferred conformation of the present isoxazole derivatives for muscle-relaxant activity is discussed.7-Benzyl-6-methyl-3-phenyl-4-pyrrolidino-4, 5, 6, 7-tetrahydroisoxazolo [5, 4-b] pyridine (3d) showed moderate central nervous system-depressant activity.
- Subjects :
- Tolperisone
Chemical Phenomena
Stereochemistry
medicine.drug_class
Molecular Conformation
chemistry.chemical_compound
Mice
Drug Discovery
Pyridine
medicine
Avoidance Learning
Structure–activity relationship
Animals
Isoxazole
Oxazoles
Bicyclic molecule
Muscle Relaxants, Central
Biological activity
Muscle relaxant
General Chemistry
General Medicine
Nuclear magnetic resonance spectroscopy
Isoxazoles
Rats
Chemistry
chemistry
medicine.drug
Subjects
Details
- ISSN :
- 00092363
- Volume :
- 35
- Issue :
- 9
- Database :
- OpenAIRE
- Journal :
- Chemicalpharmaceutical bulletin
- Accession number :
- edsair.doi.dedup.....5c6e054603780268e692290d4104833e