新型含NS杂环化合物设计合成及其生物活性研究.pdf

ShandongUniversityDoctoralDissertation ABSTRACT Heterocycliccompoundscontainingnitrogenandsulfuratomshaveawiderange ofapplications.Theyarepredominantamongthetypesofcompoundsusedas pharmaceuticals,suchasanticancer,antiviral,antibacterial,anti-inflammation, anti-psychotic,anti-histamine,acesodyne,andcerebrocardiacvascularagentsetc.One ofthereasonsforthewidespreadapplicationsofheterocycliccompoundsin pharmaceuticalsisthattheirstructurescanbesubtlymanipulatedasbuildingblockto constructanactivescaffoldofthepharmacophore,forthespatialfillingatthebinding siteofthedrugreceptors.Anotherimportantfeatureofthestructureofmany heterocycliccompoundsusedinpharmaceuticalisthatitispossibletoincorporate functionalgroupseitherassubstituentsoraspartoftheringsystemitself. Heterocycliccompoundsarewidelydistributedinnatureandareessentialto livingsystems.Manynaturalheterocyclicproductsareinregularclinicaluse,but mostoftheotherheterocycliccompoundsinpharmaceuticalsaresynthesizedin laboratory.Drugsseemtobecloselyrelatedtoheterocycliccompounds,whichare probablyduetotheirhardlydecomposedinthemetabolicprocess,andbetter compatiblewithbiosystem. Inthisdissertation,somenovelheterocyclicringsystemsandtheirderivatives containingnitrogenand/orsulfuratoms,suchasthienothiadiazine,triazoles, pyrazines heterocyclic systems, have been designed, synthesized and pharmacologicallyinvestigated,focusingonsomeseriousdiseasesthatcurrently threatenhumanlife,suchashumanimmunodeficiencyvirus(HIV)causedacquired immunedeficiencysyndrome(AIDS),cardiovasculardiseases(CVDs),cancerand bacteriainfectionetc,andfromwhich,somenewleadcompoundsarefoundtobe valuableinpharmaceuticaldevelopment.Also,thestructure-activityrelationshipof theseheterocycliccompoundshasbeenestablishedforthe加rthermedicinal explorations. l.Design,SynthesisandAnti-HIVActivitiesofANovelClassofNon-Nucleoside Reverse Transcriptase Inhibitors:2,4-Disubstitut