Modha J, Datta N, Parekh H
Department of Chemistry, Saurashtra University, Gujarat, India.
Farmaco. 2001 Sep;56(9):641-6. doi: 10.1016/s0014-827x(01)01118-1.
Condensation of 5-cyano-2-hydrazino-3-N-methyl-6-phenyl/p-chlorophenyl-3,4-dihydropyrimidin-4-one (3a and 3b) with 2,4-bisalkyl/arylamino-6-chloro-s-triazine (4) gave the corresponding 2,4-bisalkyl/arylamino-6-[5'-cyano-3'-N-methyl]-6'-phenyl/pchlorophenyl-3',4'-dihydropyrimidin-4'-one-2'-yl-hydrazino-s-triazines (5a-n and 6a-n). The compounds 4 have been prepared by the condensation of cyanuric chloride and different alkyl/aryl amines. The reaction between 5-cyano-3-N-methyl-2-methylthio-6-phenyl/p-chlorophenyl-3,4-dihydropyrimidin-4-one (2a and 2b) with hydrazine hydrate furnished 3a and 3b, respectively. The condensation of 6-phenyl/p-chlorophenyl/5-cyano-2-mercapto-3,4-dihydropyrimidin-4-one (1a and 1b) with methyl iodide yielded 2a and 2b, respectively. All the products have been evaluated in vitro for their antimicrobial activity against several microbes and antitubercular activity against Mycobacterium tuberculosis H37 Rv.
5-氰基-2-肼基-3-N-甲基-6-苯基/对氯苯基-3,4-二氢嘧啶-4-酮（3a和3b）与2,4-双烷基/芳氨基-6-氯-s-三嗪（4）缩合，得到相应的2,4-双烷基/芳氨基-6-[5'-氰基-3'-N-甲基]-6'-苯基/对氯苯基-3',4'-二氢嘧啶-4'-酮-2'-基肼基-s-三嗪（5a-n和6a-n）。化合物4是通过三聚氯氰与不同的烷基/芳基胺缩合制备的。5-氰基-3-N-甲基-2-甲硫基-6-苯基/对氯苯基-3,4-二氢嘧啶-4-酮（2a和2b）与水合肼反应分别得到3a和3b。6-苯基/对氯苯基/5-氰基-2-巯基-3,4-二氢嘧啶-4-酮（1a和1b）与碘甲烷缩合分别得到2a和2b。所有产物均已在体外评估了它们对几种微生物的抗菌活性以及对结核分枝杆菌H37 Rv的抗结核活性。
