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Generally, herbal medicines having remarkable popularity for treating liver ailments, but they are still unacceptable because of the deprivation of herbal drug standardization. Therefore, there is a need for promising synthetic drugs to overcome the critical liver problem. We introduce 1, 3, 4-oxadiazine ring in this study to identify better anti-hepatotoxic agents via a suitable synthetic route. These oxadiazine-based derivatives were structurally confirmed by analytical and spectral data and evaluated for their anti-hepatotoxic potential. Further,  in vitro  hepatotoxicity studies have been done to check the toxicity level in the synthesized compound. Compounds  5a ,  5b ,  5c  and  9d  were selected for further biological evaluation according to  in vitro  results. After that, CCl 4 -induced animal model was used to evaluate  in vivo  anti-hepatotoxicity activity. Compound  5a  with 52.99%, 59.3%, 79.34% and  5b  with 52.16%, 57.65%, 75.10% revealed to be most promising for reduction in level of SGPT, SGOT and ALKP, respectively. Moreover, it was also observed that the compound  5a  with 411.01%, 53.39% and  5b  with 378.63%, 48.9% level of albumin and total protein were respectively. The induced-fit docking results of the compounds  5a  and  5b  reveal some essential binding information and exhibited desirable ADME properties, and obeyed Lipinski's rule of five. In addition, molecular dynamics studies for 100 ns further confirm the protein-ligand complex's stability, supporting the  in vitro  and  in vivo  data, and help in establishing the SAR of synthesized compounds. Two compounds,  5a  and  5 b , exhibited higher anti-hepatotoxic activity than the standard drug silymarin.

Synthesis, biological evaluation and molecular dynamics studies of oxadiazine derivatives as potential anti-hepatotoxic agents