Misra U, Shukla S, Gurtu S, Saxena A K, Shanker K
Department of Pharmacology & Therapeutics King George's Medical College, Lucknow, India.
Boll Chim Farm. 1995 Oct;134(9):492-6.
2-Mercapto-5-[4'-methoxy phenyl thiourea]-1,3,4-thiadiazole (2a-c) prepared by the condensation of 2-amino-5-mercapto-1,3,4-thiadiazole (1) with substituted phenyl isothiocyanates. Further on cyclisation with malonic acid in the presence of acetyl chloride gave the corresponding 2-mercapto-5-[3-(4-methoxy phenyl)-2-thioxo-2-5-dihydro-4, 6-pyrimidionoyl]-1,3,4-thiadiazole (3a-c) [sequence: see text]. This on further reaction with substituted aryl aldehydes in presence of zinc chloride gave 2-mercapto-5-[3-(4'-methoxy phenyl)-2'-thioxo-2',5'-dihydro-4',6' -pyrimidionoyl 5'-phenyl carboxaldehyde]-1,3,4- thiadiazole (4a-g) [sequence: see text]. The compounds were screened for antidepressant activity and compared with antidepressant (imipramine).
2-巯基-5-[4'-甲氧基苯基硫脲]-1,3,4-噻二唑（2a - c）是通过2-氨基-5-巯基-1,3,4-噻二唑（1）与取代苯基异硫氰酸酯缩合制备而成。进一步在乙酰氯存在下与丙二酸环化得到相应的2-巯基-5-[3-(4-甲氧基苯基)-2-硫代-2,5-二氢-4,6-嘧啶酮酰基]-1,3,4-噻二唑（3a - c）[序列：见原文]。该产物在氯化锌存在下与取代芳醛进一步反应得到2-巯基-5-[3-(4'-甲氧基苯基)-2'-硫代-2',5'-二氢-4',6'-嘧啶酮酰基5'-苯基羧醛]-1,3,4-噻二唑（4a - g）[序列：见原文]。对这些化合物进行了抗抑郁活性筛选，并与抗抑郁药（丙咪嗪）进行了比较。
