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1,2-dihydro-3,1-benzoxazin-4-one and 4H-1,2-dihydro-pyrido-[2,3-d]-[1,3]-Oxazin-4-one derivatives as potential prodrugs part I: Synthesis

✍ Scribed by Gerhard Schwenker; Jianbing Chen

Publisher
John Wiley and Sons
Year
2010
Tongue
English
Weight
523 KB
Volume
324
Category
Article
ISSN
0365-6233

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✦ Synopsis

Abstract

1‐Mono‐ and previously unknown 1,2‐disubstituted 1,2‐dihydro‐3,1‐benzoxazin‐4‐ones 7 and 9, potential prodrugs of flufenamic acid (6) and mefenamic acid (8), and 4__H__‐1,2‐dihydro‐pyrido‐[2,3‐d]‐[1,3]‐oxazin‐4‐ones 11, potential prodrugs of niflumic acid (10), were prepared; the structures of all new compounds wereconfirmed by spectroscopic methods.

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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