Archives of Pharmacal Research

  • 제29권1호
  • /
  • Pages.16-25
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  • 2006
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  • 0253-6269(pISSN)
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  • 1976-3786(eISSN)
대한약학회 (The Pharmaceutical Society of Korea)
권호 표지

Synthesis and In Vitro Evaluation of Some Novel Benzofuran Derivatives as Potential Anti-HIV-1, Anticancer, and Antimicrobial Agents

  • Rida, Samia M. (Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Alexandria) ;
  • EI-Hawash, Soad A.M. (Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Alexandria) ;
  • Fahmy, Hesham T.Y. (Department of Pharmaceutical Sciences, College of Pharmacy, South Dakota State University) ;
  • Hazza, Aly A. (Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Alexandria) ;
  • EI-Meligy, Mostafa M.M. (Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Alexandria)
  • 발행 : 2006.01.01
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초록

A novel series of 1-(1-benzofuran-2-yl-ethylidene)-4-substituted thiosemicarbazides (2a-d) along with some derived ring systems: substituted-2,3-dihydro-thiazoles(3a-c, 4a-f) and thiazolidin-4-ones(5a-d and 6a-d), were synthesized. In addition, cyanoacetic acid-(1-benzofuran-2-yl-ethylidene) hydrazide(7) was used to prepare another new series of compounds consisting of substituted pyridin-2(1H)-ones(8a-c); 2-thioxo-2,3-dihydro-thiazoles(9a-d) and 2-thioxo-2,3-dihydro-6H-thiazolo[4,5-d]pyrimidin-7-ones (10a-c, 11a-c). The absolute configuration of compound 5c was determined by X-ray crystallography. The compounds prepared were evaluated for their in vitro anti-HIV, anticancer, antibacterial, and antifungal activities. Among the tested compounds, compounds 5c and 9a produced a significant reduction ㅐ ㄹ the viral cytopathic effect (93.19% and 59.55%) at concentrations $>2.0{\times}10^{-4}\;M\;and\;2.5{\times}10^{-5}\;M$respectively. Compound 9a was confirmed to have moderate anti-HIV activity. Compounds 2a, 2d, and 5c showed mild antifungal activity. However, none of the tested compounds showed any significant anticancer activity.

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