Design, synthesis, α‐glucosidase inhibition, pharmacokinetic, and cytotoxic studies of new indole‐carbohydrazide‐phenoxy‐N‐phenylacetamide derivatives

摘要: A new series of indole‐carbohydrazide‐phenoxy‐N‐phenylacetamide derivatives 7a–l were designed, synthesized, and screened for their α‐glucosidase inhibitory abilities and cytotoxic effects. The results obtained in the α‐glucosidase inhibition assay indicated that most of the synthesized derivatives displayed good to moderate inhibitory abilities (Ki values ranging from 14.65 ± 2.54 to 37.466 ± 6.46 μM) when compared with the standard drug acarbose (Ki = 42.38 ± 5.73 μM). Among them, 2‐mehoxy‐phenoxy derivatives 7l and 7h with 4‐nitro and 4‐chloro substituents on the phenyl ring of the N‐phenylacetamide moiety, respectively, displayed the most inhibition effects. The inhibitory mechanism of these compounds was investigated by molecular docking studies. The in vitro cytotoxicity assay showed that only one compound, 2‐methoxy‐phenoxy derivative 7k with a 4‐bromo substituent on the …