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  • 标题:Pharmacophore Based Synthesis of 3-Chloroquinoxaline-2-carboxamides as Serotonin3 (5-HT3) Receptor Antagonist
  • 本地全文:下载
  • 作者:Radhakrishnan Mahesh ; Ramachandran Venkatesha Perumal ; Pandi Vijaya Pandi
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2004
  • 卷号:27
  • 期号:9
  • 页码:1403-1405
  • DOI:10.1248/bpb.27.1403
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:A series of 3-chloroquinoxaline-2-carboxamides were designed and prepared by the condensation of 3-chloro-2-quinoxaloylchloride with appropriate Mannich bases of the p -aminophenol in the microwave environment. The synthesized compounds were evaluated for serotonin3 (5-HT3) receptor antagonistic activities in longitudinal muscle-myenteric plexus (LMMP) preparation from guinea pig ileum against the 5-HT3 agonist, 2-methyl-5-HT. Compound 3g exhibited comparable 5-HT3 antagonistic activity (p A 2 6.4) to that of standard antagonist Ondansetron (p A 2 6.9), while the other compounds exhibited mild to moderate 5-HT3 antagonistic activities.
  • 关键词:quinoxalinecarboxamide;Mannich base;serotonin3 (5-HT3) receptor antagonist
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