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[(3-Aryl-1,2-benzisoxazol-6-yl)oxy]acetic acids. A new diuretic series
- Source :
- Journal of Medicinal Chemistry. 25:36-44
- Publication Year :
- 1982
- Publisher :
- American Chemical Society (ACS), 1982.
-
Abstract
- A series of [(3-aryl-1,2-benzisoxazol-6-yl)oxy]acetic acids was synthesized and tested for diuretic activity in saline-loaded mice and in conscious, water-loaded dogs. The structural requirements for good diuretic activity in both mice and dogs were found to be very specific. In summary, the compounds with the best diuretic activity (13i, 13q, and 13ff) were substituted with a 2-fluorophenyl group at the 3 position and chlorine or bromine at the 7 position. Compound 13ff, [(7-bromo-3-(2-fluorophenyl)-1,2-benzisoxazol-6-yl]oxy]acetic acid (HP 522), was found to be moderately uricosuric in chimpanzees and was selected for further development.
- Subjects :
- Male
Uricosuric
Bromine
Chemistry
medicine.medical_treatment
Aryl
chemistry.chemical_element
Isoxazoles
Uricosuric Agents
Diuretic Activity
Medicinal chemistry
Mice
Structure-Activity Relationship
chemistry.chemical_compound
Acetic acid
Dogs
Biochemistry
Drug Discovery
medicine
Chlorine
Animals
Molecular Medicine
Diuretic
Diuretics
Oxazoles
Subjects
Details
- ISSN :
- 15204804 and 00222623
- Volume :
- 25
- Database :
- OpenAIRE
- Journal :
- Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....57e6d5cbc655d5e268f413b26d07f300