Archives of Pharmacal Research

  • 제25권3호
  • /
  • Pages.258-269
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  • 2002
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  • 0253-6269(pISSN)
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  • 1976-3786(eISSN)
대한약학회 (The Pharmaceutical Society of Korea)
권호 표지

Synthesis of New 2-Thiouracil-5-Sulfonamide Derivatives with Biological Activity

  • Fathalla, O.A. (Department of Medicinal Chemistry, National Research Centre) ;
  • Zaghary, W.A. (Pharmaceutical Chemistry Dept. Helwan University Faculty of Pharmacy) ;
  • Radwan, H.H. (Microbiology Dept. Helwan University Faculty of Pharmacy) ;
  • Awad, S.M. (Organic Chemistry Dept. Helwan University Faculty of Pharmacy) ;
  • Mohamed, M.S. (Organic Chemistry Dept. Helwan University Faculty of Pharmacy)
  • 발행 : 2002.06.01
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초록

2-Thiouracil-5-sulfonylchloride 1 reacted with a series of aromatic and heterocyclic amines to give 2a-j. The same compound 1 was reacted with a series of sulphonamides giving different sulphonamides of type 3a-e. On the other hand compound 1 was allowed to react with p-aminoacetophenone givining compound 4 which in turn was allowed to react with derivatives of alkyl thiosemicarbazides to give thiosemicarbazones of type 5a-e, also compound 4 was monobrominated to give compound 6 which in turn was reacted thiosemicarbazones of some aldehydes to give the corresponding thiazole derivatives 7a-f. In the same time compound 4 was reacted with a series of aromatic and heterocyclic aldehydes givining chalcones 8a-g (Claisen-Schemidt reaction). Also compound 4 was allowed to react with a series of aromatic and heterocyclic aldehydes, ethyl cyano acetate and/or malononitrile, and ammonium acetate giving pyridine derivatives 9a-d and 10a-e respectively. The biological effects of some of the new synthesized compounds was also investigated.

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참고문헌

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