Synthesis and anti-elastase properties of 6-amino-2-phenyl-4H-3,1-benzoxazin-4-one aminoacyl and dipeptidyl derivatives
โ Scribed by Eric Colson; Jean Wallach; Marcelle Hauteville
- Book ID
- 116308393
- Publisher
- Elsevier Science
- Year
- 2005
- Tongue
- English
- Weight
- 149 KB
- Volume
- 87
- Category
- Article
- ISSN
- 0300-9084
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The first solid-phase synthesis of 1,4-benzothiazin-3(4H)-ones and 1,4-benzoxazin-3(4H)-ones is reported. Alkylation of the immobilized 4-hydroxy-3-nitrobenzamide 2a and 3-nitro-4-sulfanylbenzamide 2b, followed by reduction and cyclization gave 4. Further alkylation and acylation was performed on th
IJ Some 1,4-dihydre2H-3,1-benzoxa~in-2-one derivatives were synthesized and tested for pharmacological activity. CPhenyl-6-chloro-l,4-dihydro-2H-3,l-benzoxazin-2-one (Compound 4) exhibited anticonvulsant activity against chemically and electrically induced seizures and low acute toxicity in mice. St