Toxicological profile, in vitro and in vivo antioxidant activities of 4-phenyl-6-(3,4,5-trimethoxyphenyl) pyrimidin-2-ylamine

Abstract

In our search for valuable therapeutics, a series of diarylaminopyrimidine (DAP) analogues have been synthesized and characterized. In this study, one of the DAPs, 4-phenyl-6-(3,4,5-trimethoxyphenyl) pyrimidin-2-ylamine, was assessed for its toxicological profile and screened for in vitro and in vivo antioxidant activities. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging method was used for the in vitro antioxidant studies and the IC₅₀ values obtained were 2.37 μg/mL and 139.60 μg/mL for the standard (ascorbic acid) and DAP, respectively. According to the in vivo studies, 50 mg/kg DAP prevented the increase in the malondialdehyde (MDA) concentration, significantly inhibited the decrease in the level of reduced glutathione (GSH) and normalized superoxide dismutase (SOD) and catalase (CAT) activities in the blood of albino rats in the treated groups compared with those in the ethanol (negative control) group. Oral administration of synthesized DAP at 5000 mg/kg did not produce any toxic or adverse effects and no mortality was recorded after 24 hours. Our findings suggest that 4-phenyl-6-(3,4,5-trimethoxyphenyl) pyrimidin-2-ylamine, holds some promise as a potential starting material for the production of drugs that can mitigate degenerative diseases.