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  • 标题:Synthesis, Antimicrobial and Anti-inflammatory Activity of Some New Benzoxazinone and Quinazolinone Candidates
  • 本地全文:下载
  • 期刊名称:Chemical and Pharmaceutical Bulletin
  • 印刷版ISSN:0009-2363
  • 电子版ISSN:1347-5223
  • 出版年度:2016
  • 卷号:64
  • 期号:3
  • 页码:263-271
  • DOI:10.1248/cpb.c15-00904
  • 语种:English
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:Benzoxazinones and quinazolinones have a wide spectrum of biological activity. In this paper we focused on studying the antimicrobial and anti-inflammatory activities of some newly synthesized benzoxazinone and quinazolinone derivatives. Thus we prepared 2-[α-benzoylaminostyryl]-6,8-dibromo-3,1-benzoxazin-4( H )-one 2 which underwent a reaction with primary and secondary amines, and hydrazine hydrate to give compounds 3 , 4 and 5 , respectively. Treatment of 2 with hydroxylamine hydrochloride, formamide and/or NaN3/AcOH afforded compounds 7 , 8 , 11 and 12 , respectively. Also, compound 2 reacted with maleic anhydride, aromatic hydrocarbons and/or active methylene compounds to produce compounds 13 , 15a – c and 16 , respectively. Most of the newly synthesized compounds showed significant antimicrobial and anti-inflammatory activities comparable to ampicillin, mycostatine and indomethacin positive controls.
  • 关键词:benzoxazinone;quinazolinone;imidazole;tetrazole;antimicrobial;anti-inflammatory
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