Tripathi M, Verma M, Gujrati V R, Palit G, Shanker K
Department of Pharmacology and Therapeutics, King George's Medical College, Lucknow, India.
Arzneimittelforschung. 1993 Jun;43(6):632-5.
3-(Benzylidene amino)-2-imino-4-thiazolidinones (IIa-c) synthesized by cyclization of substituted thiosemicarbazones (Ia-c) were converted into 2-amino-3-(substituted benzylamino)-4-thiazolidinones (IIIa-c), 2-imino-3-(alpha-aryl azo benzylidene) amino-4-thiazolidinones (IVa-f) and 2-(2-amino-4-oxo-3-thiazolidinyl)-3-aryl-4-isothiazolidinones (VIa-c), IVa-f were finally converted into 5-(arylamino methyl)-2-imino-3-(alpha-aryl azobenzylidene)-amino-4-thiazolidinones (Va-l). These compounds III, V and VI were evaluated for their monoamine oxidase (MAO) inhibitory activity in vitro and various CNS activities in vivo. Some of the compounds exhibited promising CNS activity.
通过取代硫代卡巴腙(Ia-c)环化合成的3-(亚苄基氨基)-2-亚氨基-4-噻唑烷酮(IIa-c)被转化为2-氨基-3-(取代苄基氨基)-4-噻唑烷酮(IIIa-c)、2-亚氨基-3-(α-芳基偶氮亚苄基)氨基-4-噻唑烷酮(IVa-f)和2-(2-氨基-4-氧代-3-噻唑烷基)-3-芳基-4-异噻唑烷酮(VIa-c),IVa-f最终被转化为5-(芳基氨基甲基)-2-亚氨基-3-(α-芳基偶氮亚苄基)-氨基-4-噻唑烷酮(Va-l)。对这些化合物III、V和VI进行了体外单胺氧化酶(MAO)抑制活性和体内各种中枢神经系统活性的评估。其中一些化合物表现出有前景的中枢神经系统活性。