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英 文 摘 要
StudiesonSynthesisandNO-releaseinvitroActivity
oftheNewDrugsContainingFuroxanylMoiety
ABSTRACT
Nitricoxide困O)isanimportantbiologicalmessengerand
etfectormolecule involved in many pathologicaland
physiologicalprocesseswhichoccurinthebody.Ithasbeen
showntoplayakeyroleincardiovascular,immune,and
nervoussystems.Numerousscholarshavefocusedonthestu勿
ofNOdonor-drugs.
Thereistheevidencethatfuroxans(1,2,5-oxadiazole2-oxides)
areabletogenerateNO,inthepresenceofthiolcofactors.
Usingappropriatesubstituentsattheheteroring,itispossibleto
modulatetherateandamountofNO production.The
pharmacologicalprofileoffuroxanshaspromptedtheinclusion
atthefuroxanringinthedesignofNOreleasingdrugs.
Atpresent,itisblankinresearchinganddevelopingthe
antiatherosclerosisdrugsendowedwithNOdonors.So,inthis
paper,ithasbeenfinishedasfollows:
① 3,4-bisphenylsulfonylfuroxanwassynthesizedrfom
thiophenolbyetherification,oxidationandcyclization.
02Twocompoundswereobtainedbylinkingfuroxanmoieyt
tonicotinicacidandclofibricacid,respectively.
③Nitrosothiolgroupwas chosentobecoupled二;ith
Captopril,soastogetcompound13-
- 一 一 一 一 一 一 一 一 一 一
5
英 文 摘 要
④Compound11,IZ,13andIsosorbideMononitratewere
testedfortheirabilityoftheNO-releaseinvitro.
Objective:TosynthesizenewtypeNOdonor-compounds,to
testthefinalproductsabilityoftheNO-releaseinvitro,andto
trytofindtheleadcompounds.
Methods:①3,4-bisphenylsulfonylfuroxanwaspreparedby
etherification,oxidationandcyclizationfromthiophenol.②By
esterificationandamidation,nicotinicacidwasturnedinto
N-(2--hydroxy-ethyl)nicotinicamide,whichwasthencoupled
with3,4-bisphenylsulfonylfuroxanthroughetherificationto
obtaintheaimcompoundI1.③Theclofibricacidderivative
wasjoinedbyanetherl
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