STUDY OF THE BIOLOGICAL PROPERTIES OF SEMI- AND THIOSEMICARBAZONES OF CARBONYL DERIVATIVES OF 4-BUTANOLIDES

T. Ghochikyan, A. Galstyan, Hrachik M. Stepanyan, I. Korpakova, A. S. Kinzirsky
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Abstract

Based on carbonyl derivatives of 4-substituted-4-butanolides, the appropriate semi- and thiosemicarbazones have been synthesized. It has been found that some representatives of thiosemicarbazones have pronounced algicidal activity against filamentous green alga Cladophora and blue-green alga (cyanobacterium) Synechocystis and some of the semi- and thiosemicarbazones exhibit moderate antitumor activity. The assessment of the antitumor activity of the compounds was carried out using strains of syngeneic and allogeneic tumor systems as test-objects: lymphocytic leukemia P-388, Lewis lung carcinoma, B16 melanoma and Ehrlich’s ascites tumor. It has also been established that some representatives of thiosemi­carbazones exhibit antimutagenic properties. It has been reliably proven that with the formation of a thiazole ring, all properties disappear and a new property in the series of thiazololactones is revealed – antibacterial․
4-丁内酯羰基衍生物半氨基脲和硫代氨基脲的生物学性质研究
以4-取代4-丁醇内酯的羰基衍生物为基础,合成了相应的半氨基脲和硫代氨基脲。研究发现,一些代表性的硫代氨基脲类化合物对丝状绿藻Cladophora和蓝绿藻(蓝藻)Synechocystis具有明显的杀藻活性,一些半和硫代氨基脲类化合物具有中等的抗肿瘤活性。以淋巴细胞白血病P-388、Lewis肺癌、B16黑色素瘤和Ehrlich腹水瘤为试验对象,对化合物的抗肿瘤活性进行了评价。也已确定,一些代表性的硫代半咔唑类具有抗诱变特性。已经可靠地证明,随着噻唑环的形成,所有的性质都消失了,并在噻唑内酯系列中显示出一种新的性质——抗菌
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