Synthesis of 5-Phenyl-1,2,4-oxadiazole Derivatives and Their Biological Activities As Inhibitors of Acetyl-Co A Carboxylase
Acetyl-Coa Carboxylase(ACC)is a kind of fatty acid synthesis rate-limiting enzyme,which is one of the hot targets of tumor therapy.A series of novel 5-phenyl-l,2,4-oxadiazoles(9a～9i)were obtained through cyclization,condensation,amidation using 3-chloroaniline and methylenesuccin-ic acid as the starting materials.The novel compounds of 9a,9b,9e～9h were characterized by 1H MNR,13 C MNR and MS(ESI).The lipid-water partition coefficients and drug-likeness scores of the target compounds 9a～9i were calculated by Molsoft online software,the acetyl-CoA carboxylase(ACC)inhibitory activity of the compounds was detected by the ADP-GloTM kinase assay kit.The re-sults showed that the inhibitory activity of compound 9g on ACC reached 95.26％at the concentration of 10 μM,which was comparable with that of positive control drug CP-640186.
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维普
