Singh V, Khanna R, Srivastava V K, Palit G, Shanker K
Department of Pharmacology and Therapeutics, King George's Medical College, Lucknow, India.
Arzneimittelforschung. 1992 Mar;42(3):277-80.
10-Hydrazino acetyl phenothiazine (II) has been converted to N-10-acetyl amino phenothiazine-N-phenyl thiourea (III) which have been converted to 3-aryl-1-(10-phenothiazine acetyl amino)-2,3-dihydro-2-thioxo-4,6-(1H,5H) pyrimidinones (IV) on condensation with aryl amines and aryl aldehydes yielded 3-aryl-1-(10-Phenothiazine acetyl amino)-5-(substituted phenyl amino methyl)-2,3-dihydro-2-thioxo-4,6-(1H, 5H) pyrimidinediones (Va-k) and 3-aryl-1-(10-phenothiazine acetyl amino)-5-(substituted phenylidine)-2,3-dihydro-2-thioxo-4,6-(1H, 5H) pyrimidinediones (vl-o). The compounds were screened for their antidepressant activity against a tricyclic antidepressant (imipramine). Compounds Va, Vf, Vm and Vi exhibited activity better than imipramine with no toxicity (ALD50 greater than 1000 mg/kg) but Vi showed some side effects.
10-肼基乙酰吩噻嗪（II）已被转化为N-10-乙酰氨基吩噻嗪-N-苯基硫脲（III），后者与芳胺和芳醛缩合后转化为3-芳基-1-（10-吩噻嗪乙酰氨基）-2,3-二氢-2-硫代-4,6-（1H,5H）嘧啶二酮（IV），生成了3-芳基-1-（10-吩噻嗪乙酰氨基）-5-（取代苯氨基甲基）-2,3-二氢-2-硫代-4,6-（1H,5H）嘧啶二酮（Va-k）和3-芳基-1-（10-吩噻嗪乙酰氨基）-5-（取代苯亚基）-2,3-二氢-2-硫代-4,6-（1H,5H）嘧啶二酮（Vl-o）。对这些化合物针对三环类抗抑郁药（丙咪嗪）进行了抗抑郁活性筛选。化合物Va、Vf、Vm和Vi表现出比丙咪嗪更好的活性且无毒性（半数致死量大于1000 mg/kg），但Vi显示出一些副作用。
