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1、Availableonlineatwww.sciencedirect.comEuropeanJournalofMedicinalChemistry44(2009)1773e1778http://www.elsevier.com/locate/ejmechShortcommunicationAclassofpotenttyrosinaseinhibitors:AlkylidenethiosemicarbazidecompoundsJinbingLiu,RihuiCao*,WeiYi,ChunmingMa,Yiqian
2、Wan,BinhuaZhou,LinMa,HuacanSong*SchoolofChemistryandChemicalEngineering,SunYat-senUniversity,135XinGangXiRoad,Guangzhou510275,PRChinaReceived15October2007;receivedinrevisedform28March2008;accepted8April2008Availableonline27April2008AbstractAseriesofalkylidenet
3、hiosemicarbazidecompoundsweresynthesizedandtheirinhibitoryeffectsonthediphenolaseactivityofmushroomtyrosinasewereevaluated.Theresultsshowedthatmostofthesynthesizedcompoundsexhibitedsignificantinhibitoryactivities.Especially,compound1fwasfoundtobethemostpotentin
4、hibitorwithIC50valueof0.086mM,suggestingthatfurtherdevelopmentofsuchcompoundsmaybeofinterest.Ó2008ElsevierMassonSAS.Allrightsreserved.Keywords:Synthesis;Alkylidenethiosemicarbazidecompounds;Tyrosinaseinhibitor1.Introductionfromnatural,syntheticandevenfromsemi-
5、syntheticsources,suchashydroquinone[9],ascorbicacidderivates[10],kojicTyrosinase(EC1.14.18.1)isamultifunctionalcopper-acid(Fig.1)[11],azelaicacid[12],corticosteroids[12],reti-containingenzymewhichiswidelydistributedinplantsnoids[12],arbutin(Fig.1)[12]andtropol
6、one(Fig.1)[13,14].andanimals[1].Itiswellknownthattyrosinasecancata-Amongalltheknowntyrosinaseinhibitors,tropolonelyzethehydroxylationofmonophenolstoo-diphenols(IC50¼0.4mM)wasfoundtobeoneofthemostpotenttyros-(monophenolaseactivity)andtheoxidationofo-diphenolsin
7、aseinhibitors[14].Unfortunately,onlyfewofthereportedtoo-quinone(diphenolaseactivity).Andtheenzymaticcompoundsareusedinmedicinalandcosmeticproductsbe-oxidationofL-tyrosineintomelaninisofconsiderablecauseoftheirloweractivitiesorserioussideeffects.There-importanc
8、eincoloringofskin,hairandeyes,andinfore,itisstillnecessarytosearchanddiscovernovelfoodbrowning[2,3].Inaddition,tyrosinaseisalsorelatedtyrosinaseinhibitorswithhigheractivityandlower
