Synthesis of new 2-thiouracil-5-sulfonamide derivatives with biological activity

被引:37
作者
Fathalla, OA [1 ]
Zaghary, WA
Radwan, HH
Awad, SM
Mohamed, MS
机构
[1] Natl Res Ctr, Dept Med Chem, Cairo, Egypt
[2] Helwan Univ, Fac Pharm, Dept Pharmaceut Chem, Helwan, Egypt
[3] Helwan Univ, Fac Pharm, Dept Organ Chem, Helwan, Egypt
关键词
thiouracil-5-sulphonamide-p-phenyl derivatives; anti-microbial; anti-viral; anti-cancer activity;
D O I
10.1007/BF02976623
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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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页码:258 / 269
页数:12
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