Synthesis, physicochemical characterization, cytotoxicity, antimicrobial, anti-inflammatory and psychotropic activity of new N-[1,3-(benzo)thiazol-2-yl]-蠅-[3,4-dihydroisoquinolin-2(1H)-yl]alkanamides

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• 作者：Alla Zablotskaya ; Izolda Segal ; Athina Geronikaki ; Tatiana Eremkina ; Sergey Belyakov ; Marina Petrova ; Irina Shestakova ; Liga Zvejniece ; Vizma Nikolajeva
• 关键词：Tetrahydroisoquinoline ; Thiazole ; Cytotoxicity ; Psychotropic activity ; Anti-inflammatory activity ; Antimicrobial activity
• 刊名：European Journal of Medicinal Chemistry
• 出版年：December, 2013
• 年：2013
• 卷：70
• 期：Complete
• 页码：846-856
• 全文大小：1026 K

文摘

A series of new N-[(benzo)thiazol-2-yl]-2/3-[3,4-dihydroisoquinolin-2(1H)-yl]ethan/propanamide derivatives was synthesized and characterized by ¹H, ¹³C NMR and IR spectroscopy and mass-spectrometry. A single crystal X-ray study of N-(1,3-benzothiazol-2-yl)-2-[3,4-dihydroisoquinolin-2(1H)-yl]ethanamide is reported to determine its conformational feature. The investigated compounds were found to be active in psychotropic in聽vivo, anti-inflammatory in聽vivo and cytotoxicity in聽vitro screening. They possess marked sedative action, reveal high anti-inflammatory activity, have selective cytotoxic effects and NO-induction ability concerning tumour cell lines. Some of the compounds synthesized demonstrate antimicrobial action. An attempt was made to correlate the biological results with their structural characteristics and physicochemical parameters. Some specific combinations of types of activities for the synthesized compounds have been revealed.