Synthesis and in vitro antimicrobial and antitumor activity of some nitrogen heterocycles

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• 作者：A. I. El-Shenawy
• 关键词：nitrogen heterocycles ; synthesis ; antimicrobial and cytotoxic activities
• 刊名：Russian Journal of Bioorganic Chemistry
• 出版年：2016
• 出版时间：January 2016
• 年：2016
• 卷：42
• 期：1
• 页码：100-105
• 全文大小：227 KB
• 参考文献：1.Wilson, L.J., Li, M., and Portlock, D.E., Tetrahedron Lett., 1998, vol. 39, no. 29, pp. 5135–5138.CrossRef
  2.Belai, I., Tetrahedron Lett., 2003, vol. 44, no. 40, pp. 7475–7477.CrossRef
  3.Brouilette, W.J., Jestkov, V.P., Brown, M.L., Akhtar,M.S., Delorey, T.M., and Brawn, G.B., J. Med. Chem., 1994, vol. 37, pp. 3289–3293.CrossRef
  4.Erik, C.S., Ottosen, R., Petersen, H.J., Bjorking, F., Latini, S., Hjarnaa, V., Bramm, E., and Binderup, L., Bioorg. Med. Chem. Lett., 1997, vol. 7, pp. 3095–3100.CrossRef
  5.Hjarnaa, P.J., Jonsson, E., Latini, S., Dhar, S., Larsson, R., Bramm, E., Skov, T., and Binderup, L., Cancer Res., 1999, vol. 59, pp. 5751–5757.PubMed
  6.Olsen, L.S., Hijamaa, P.J., Latini, S., Holm, P.K., Larsson, R., Bramm, E., Binderup, I., and Madsen, M.W., Inc. Cancer, 2004, vol. 3, pp. 98–105.
  7.Mader, M.M., Curr. Opin. Drug Discov. Devel., 2005, vol. 8, pp. 613–618.PubMed
  8.Ibrahim, H.K., Hasanen, J.A., Zein, M.A., and ElDeen, I.M., Mens Agitat., 2008, vol. 3, pp. 59–72.
  9.Aboubshit, S.A. and Aboubshit, H.A., J. Chem. Pharm. Res., 2012, vol. 4(1), pp. 568–579.
  10.Abd El-Moneim, M., IOSR JAC, 2014, vol. 7, no. 1, pp. 67–76.CrossRef
  11.El-Sakka, S., Mens Agitat., 2008, vol. 2, pp. 57–68.
  12.Schelz, Z., Molnar, J., and Hohmann, J., Fitoterapia, 2006, vol. 77, no. 4, pp. 279–285.CrossRef PubMed
  13.National Committee for Clinical Laboratory Standards. Performance Standards for Antimicrobial Susceptibility Testing, Informational Supplement M100. S13, 12th ed., NCCLS: Wayne, PA,USA, 2003.
  14.Gillespie, S.H., Antimicrobial Susceptibility in Medical Microbiology, Illustrated, London: Butterworth Heinemann, 1994, pp. 234–247.
  15.Chatterjee, S. and Das, S.N., Ind. J. Pharmacol., 1996, vol. 28, pp. 116–119.
  16.Mosmann, T., J. Immunol. Methods, 1983, vol. 65, pp. 55–63.CrossRef PubMed
  17.Vijayen, P., Raghu, C., Ashok, G., Dhanaraj, S.A., and Suresh, B., Indian J. Med. Res., 2004, vol. 120, no. 1, pp. 9–24.
  
• 作者单位：A. I. El-Shenawy (1)
  
  1. Department of Chemistry, Faculty of Science, Benha University, Benha, Egypt
  
• 刊物类别：Biomedical and Life Sciences
• 刊物主题：Life Sciences
  Biochemistry
  Bioorganic Chemistry
  Organic Chemistry
  Biomedicine
  Russian Library of Science
  
• 出版者：MAIK Nauka/Interperiodica distributed exclusively by Springer Science+Business Media LLC.
• ISSN：1608-330X

文摘

5-Phenyl-2-[(3,4,5-trimethoxybenzylidene)hydrazino]-thiazole and 3-[(3,4,5-trimethoxybenzylidene)amino]-4-oxoimidazolidin-2-thione were prepared by cyclization of 1-[(3,4,5-trimethoxybenzyliden)amino]-thiourea with phenacyl bromide and ethyl chloroacetate in the presence of fused sodium acetate. Acetylation of the synthesized compounds with acetic anhydride gave corresponding N-acetyl derivatives. Condensation of the synthesized thione with aromatic aldehydes yielded two 3-substituted 5-arylidene-4oxo-imidazolidin-2-thiones. Acetylation of the latter compounds with acetic anhydride afforded the corresponding N-acetyl-4-oxo-imidazolidin-2-thiones. Some of the synthesized compounds exhibited antimicrobial activity. The cytotoxic activity of the prepared thiazole and imidazolidin-2-thione derivatives was studied on several tumor cell lines. Keywords nitrogen heterocycles synthesis antimicrobial and cytotoxic activities