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Synthesis of metronidazole based thiazolidinone analogs as promising antiamoebic agents.
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2020-09-11 , DOI: 10.1016/j.bmcl.2020.127549
Mohammad Fawad Ansari 1 , Afreen Inam 1 , Kamal Ahmad 2 , Shehnaz Fatima 3 , Subhash M Agarwal 3 , Amir Azam 1
Affiliation  

Metronidazole and its derivatives are widely used for the treatment of amoebiasis. However, metronidazole is considered as the standard drug but it has 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 the standard drug metronidazole towards HM1: IMSS strain of Entamoeba histolytica. These compounds may combat the problem of drug resistance and might be effective in identifying potential alternatives for future drug discovery against EhOASS.



中文翻译:

合成基于甲硝唑的噻唑烷酮类似物作为有前途的抗厌氧剂。

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。

更新日期:2020-09-11
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