Synthesis And Antifungal Activities Of Derivatives Of Acetophenone

In recent years, acetophenone compounds play an important role in the new ultra high efficient antifungal studies. To design and synthesize various derivatives of acetophenone is a very important way to obtain new compounds with good bioactivities. Ketones causes for the much concern in the benzene compounds because of its Low toxicities, good bioactivities and structural Varieties. For a long time, (o-,m-,p-)hydroxy acetophenone has been studied widely in medical and pharmaceutical applications, whereas it has rarely been studied in antifungal.Allyl acetophenone and their 21 derivatives were synthesized from (o-,m-,p-)hydroxy acetophenone, of which 10 derivatives were first studied. Their structures were characterized by 1H-NMR,EI-MS and IR.The antifungal activity results showed as fowllows: the 28 compounds had differernt inhibition rates on plant pathogenic fungus mycelial growth at concentration of 100 mg/L. Overall, compound WJ₁3, WJ₁5, WJ₁7 had better antifungal activity than that of other derivatives. In comparison with carbendazim, inhibition rates of WJ₁3, WJ₁7 closed to that of carbendazim , while against Fusarium solani, espectively 95.0% and 95.0%. Compound WJ₁7 had the best antifungal activity while against six tested fungi, the inhibition rates of which espectively were 70.0%, 71.4%, 87.2%, 80.0%, 95.0% and 75.0%. Other compounds didn't show good antifungal activities.IC50 results showed as fowllows: Compound WJ₅ against Colletotrichum gloeosporioides had better antifungal activity at lower concentration, while IC50 was 1.67 mg/L. IC50 of Compound WJ₁3 against Fusarium graminearum was 27.50 mg/L; IC50 of Compound WJ₁7 against Fusarium oxysporum f . s p. niveu was 23.00 mg/L; In comparison with WJ₅ and WJ₁3, IC50 of WJ₁7 against Fusarium oxysporum vasinfectum was 41.25 mg/L, while IC50 of WJ₅ and WJ₁3 espectively were 66.00 mg/L and 57.00 mg/L.