Synthesis of metronidazole based thiazolidinone analogs as promising antiamoebic agents
作者:Mohammad Fawad Ansari、Afreen Inam、Kamal Ahmad、Shehnaz Fatima、Subhash M. Agarwal、Amir Azam
DOI:10.1016/j.bmcl.2020.127549
日期:2020.12
many side effects. The present study describes the synthesis of a series of metronidazole based thiazolidinone analogs via Knoevenagel condensation of 4-[2-(2-methyl-5-nitro-1H-imidazole-1-yl)ethoxy]benzaldehyde 1 with various thiazolidinone derivatives 2-14 to get the new scaffold (15-27) having better activity and lesser toxicity. Six compounds have shown better efficacy and lesser cytotoxicity than
甲硝唑及其衍生物被广泛用于阿米巴病的治疗。但是,甲硝唑被认为是标准药物,但有许多副作用。本研究描述的基于噻唑烷酮类似物的一系列甲硝唑的合成通过4- Knoevenagel缩合[2-(2-甲基-5-硝基-1- ħ咪唑-1-基)乙氧基]苯甲醛1与各种噻唑烷酮衍生物2 -14得到新的支架(15-27),具有更好的活性和更低的毒性。与标准甲硝唑相比,六种化合物对HM1具有更好的疗效,并具有较小的细胞毒性,这是对溶组织变形杆菌的IMSS菌株。这些化合物可能会解决耐药性问题,并可能有效地确定将来针对Eh OASS的药物发现的潜在替代品。