Mohmmad Younus Wani1, Amir Azam2, Fareeda Athar1
1Centre for Interdisciplinary Research in Basic Sciences, Jamia Millia Islamia (Central University), New Delhi-110025, India.
2Department of Chemistry, Jamia Millia Islamia Central University), New Delhi-110025, India.
As a part of investigation of new antiamoebic agents in this laboratory, herein we describe the synthesis of a new class of nitroimidazole based acylhydrazones. All the compounds were screened for their antiamoebic activity against HM1:IMSS strain of Entamoeba histolytica by microdilution method. To ensure the noncytotoxic nature of the active compounds, screening was done on human hepatocellular carcinoma cell line HepG2 by using MTT assay. To further check the expected bioavailability and druglikeness properties, all the compounds were subjected to molecular properties prediction. Results obtained, revealed that the presence of free -NH and C=O group, besides the presence and position of substituents played a dominant role on the activity of the compounds, where activity seems to be guided by the electron donating/releasing and withdrawing nature of the substituents. Compounds having electron releasing groups attached to the hydrazone pendent were found to be highly antiamoebic and least cytotoxic. All the compounds also showed good oral bioavailability and druglikeness properties, besides, following the Lipinski’s rule of 5. Read more…