Thriveni K S, Padmashali B, Siddesh M B, Sandeep C
Department of Chemistry, Sahyadri Science College (Autonomous), Shimoga-577 203, India.
Indian J Pharm Sci. 2014 Jul;76(4):332-8.
Thiophene substituted chalcones (1a-e) were cyclised with thiourea in presence of potassium hydroxide to get 4-substituted-6-(thiophen-2-yl)pyrimidine-2-thiols (2a-e) which were then stirred with methyl iodide to obtain 4-substituted-2-(methylsulfanyl)-6-(thiophen-2-yl)pyrimidines (3a-e). Compounds (3a-e) were refluxed with different N-methylpiperazine and N-phenylpiperazine to afford 4-substituted-2-(4-methylpiperazin-1-yl)-6-(thiophen-2-yl)pyrimidines (4a-e) and 4-substituted-2-(4-phenylpiperazin-1-yl)-6-(thiophen-2-yl)pyrimidines (5a-e). The structures of all the newly synthesised compounds 4b, 4d, 5a and 5b showed good antibacterial activity at 40μg/mlconcentration. Compounds 4a, 4d, 4e, 5c and 5e showed significant antifungal activity at 40 μg/ml concentration compared with standard drugs.
在氢氧化钾存在下,噻吩取代的查耳酮(1a - e)与硫脲环化,得到4 - 取代 - 6 -(噻吩 - 2 - 基)嘧啶 - 2 - 硫醇(2a - e),然后将其与碘甲烷搅拌,得到4 - 取代 - 2 -(甲硫基)- 6 -(噻吩 - 2 - 基)嘧啶(3a - e)。化合物(3a - e)与不同的N - 甲基哌嗪和N - 苯基哌嗪回流,得到4 - 取代 - 2 -(4 - 甲基哌嗪 - 1 - 基)- 6 -(噻吩 - 2 - 基)嘧啶(4a - e)和4 - 取代 - 2 -(4 - 苯基哌嗪 - 1 - 基)- 6 -(噻吩 - 2 - 基)嘧啶(5a - e)。所有新合成的化合物4b、4d、5a和5b的结构在40μg/ml浓度下显示出良好的抗菌活性。与标准药物相比,化合物4a、4d、4e、5c和5e在40μg/ml浓度下显示出显著的抗真菌活性。