Synthesis of metronidazole based thiazolidinone analogs as promising antiamoebic agents

被引：13

作者：

Ansari, Mohammad Fawad ^{[1
]}

Inam, Afreen ^{[1
]}

Ahmad, Kamal ^{[2
]}

Fatima, Shehnaz ^{[3
]}

Agarwal, Subhash M. ^{[3
]}

Azam, Amir ^{[1
]}

机构：

[1] Jamia Millia Islamia, Dept Chem, New Delhi 110025, India

[2] Jamia Millia Islamia, Ctr Interdisciplinary Res Basic Sci, New Delhi 110025, India

[3] ICMR Natl Inst Canc Prevent & Res, Bioinformat Div, I-7,Sect 39, Noida 201301, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2020年 / 30卷 / 23期

关键词：

Metronidazole; Thiazolidinone; Amoebiasis; Entamoeba histolytica; Molecular docking; BIOLOGICAL EVALUATION; ANTICANCER ACTIVITY; DERIVATIVES; DESIGN; 4-THIAZOLIDINONES; OPTIMIZATION; DOCKING; GROWTH;

D O I：

10.1016/j.bmcl.2020.127549

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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-1Himidazole-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.

引用

页数：5

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