期刊文献+

Synthesis and bioactivities of some new 1H-pyrazole derivatives containing an aryl sulfonate moiety 被引量:2

Synthesis and bioactivities of some new 1H-pyrazole derivatives containing an aryl sulfonate moiety
原文传递
导出
摘要 A new series of 1H-pyrazole derivatives 5a-j bearing an aryl sulfonate moiety have been synthesized by a one-pot cyclo-condensation reaction of 2-(3-(dimethylamino)acryloyl)phenyl-4-methyl benzene sulfonates 4a-e and hydrazine hydrate or phenyl hydrazine in ethanol under reflux conditions. Some of the newly synthesized compounds were screened for their anti-inflammatory activity. All synthesized compounds were screened against Gram positive and Gram negative bacterial and fungal strains. The compound 5b was found to be a potent anti-inflammatory agent while the majority of the compounds were found to be active against microbial strains. A new series of 1H-pyrazole derivatives 5a-j bearing an aryl sulfonate moiety have been synthesized by a one-pot cyclo-condensation reaction of 2-(3-(dimethylamino)acryloyl)phenyl-4-methyl benzene sulfonates 4a-e and hydrazine hydrate or phenyl hydrazine in ethanol under reflux conditions. Some of the newly synthesized compounds were screened for their anti-inflammatory activity. All synthesized compounds were screened against Gram positive and Gram negative bacterial and fungal strains. The compound 5b was found to be a potent anti-inflammatory agent while the majority of the compounds were found to be active against microbial strains.
出处 《Chinese Chemical Letters》 SCIE CAS CSCD 2013年第4期325-328,共4页 中国化学快报(英文版)
关键词 PyrazoleEnaminonep-Toluene sulfonyl chlorideAnti-inflammatory activityCOX-2 inhibitors PyrazoleEnaminonep-Toluene sulfonyl chlorideAnti-inflammatory activityCOX-2 inhibitors
  • 相关文献

参考文献25

  • 1CE. Dugowson, P. Gnanashanmugam, Nonsteroidal anti-inflammatory drugs, Phys. Med. Rehabil. Clin. N. Am. 17 (2006) 347-354.
  • 2J.R Vane, RM. Botting, The mechanism of action of aspirin, Thromb. Res. 110 (2003) 255-258.
  • 3S. Hernandez-Diaz, L.A.G. Rodriguez, Association between nonsteroidal anti?inflammatory drugs and upper gastrointestinal tract bleeding/perforation, Arch. Intern. Med. 160 (2000) 2093-2099.
  • 4F. Krotz, T.M. Schiele, V.KIauss, Selective COX-2 inhibitors and risk of myocardial infarction, j. Vase. Res. 42 (2005) 312-324.
  • 5S.M. EI-Moghazy, F.F. Barsoum, H.M. Abdel-Rahman, A.A. Marzouk, Synthesis and anti-inflammatory activity of some pyrazole derivatives, Med. Chern. Res. 21 (2012) 1722-1733.
  • 6S.R Shih, T.Y. Chu, G.R. Reddy, et aI., Pyrazole compound BPR1P0034 with potent and selective anti-influenza virus activity, j. Biomed. Sci. 17 (2010) 13.
  • 7H. Naito, S. Ohsuki, M. Sugimori, R Atsumi, et aI., Synthesis and antitumor activity of novel pyrimidinyl pyrazole derivatives. II. Optimization of the phenyl piper?azine moiety of 1-[5-methyl-l-(2-pyrimidinyl)-4-pyrazolyl]-3-phenylpiperazi?nyl-l-trans-propenes, Chern. Pharm. Bull. 50 (2002) 453-462.
  • 8M. Abdel-Aziz, G.A. Abuo-Rahma, A.A. Hassan, Synthesis of novel pyrazole deri?vatives and evaluation of their antidepressant and anticonvulsant activities, Eur.j. Med. Chern. 44 (2009) 3480-3487.
  • 9P.B.R. Kumar, S. Subramaniyan, K. Yamini, R Suthakaran, Synthesis of some novel 1-H pyrazoles derivatives and their antibacterial activity studies, Russ. j. Chern. 4 (2011) 400-404.
  • 10A. Balbi, M. Anzaldi, C Maccio, et aI., Synthesis and biological evaluation of novel pyrazole derivatives with anticancer activity, Eur. j. Med. Chern. 46 (2011) 5293-5309.

同被引文献6

引证文献2

二级引证文献3

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部