Bedi Preet, Mahajan Mohinder P, Kapoor Vijay K
Department of Pharmaceutical Sciences, Guru Nanak Dev. University, Amritsar, Punjab, India.
PDA J Pharm Sci Technol. 2003 Mar-Apr;57(2):109-13.
A series of novel-2-phenyl-1-p-tolyl-4-thiomethyl-1,3-diazabuta-1,3-dienes compounds (5a-5e) possessing morpholino, diethyl amino, pyrrolidino, piperidino and 2-aminopyridino groups respectively at C-4 were prepared by reaction of alpha-aryliminobenzyl isothiocyanates with secondary amines and S-alklyation of the resultant thioureas with aqueous potassium hydroxide. The isothiocyanates were obtained from easily available starting materials. These 1,3-diazabuta-1,3-dienes were obtained in pure form after recrystallization and their structures were established by analytical and spectral data. The synthesized compounds were screened for their antibacterial activity and some of them were found to exhibit significant antibacterial activity.
通过α-芳基亚氨基苄基异硫氰酸酯与仲胺反应，以及所得硫脲与氢氧化钾水溶液的S-烷基化反应，制备了一系列新型的2-苯基-1-对甲苯基-4-硫代甲基-1,3-二氮杂丁-1,3-二烯化合物（5a - 5e），它们在C-4位分别具有吗啉基、二乙氨基、吡咯烷基、哌啶基和2-氨基吡啶基。异硫氰酸酯由易得的起始原料制得。这些1,3-二氮杂丁-1,3-二烯经重结晶后得到纯品，其结构通过分析和光谱数据确定。对合成的化合物进行了抗菌活性筛选，发现其中一些表现出显著的抗菌活性。
