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3取代阿齐霉素衍生物的合成及抗菌活性研究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一、实验部分11A216A217A218A219A216A217A218A219UVA220SHIMADZAA221A222A223A224A224A225A226UV260A227A228A229A230A222A224A231A220SPECTRUMONEA232A233A234A230A222A224A231A226A227A228,KBRA235A236A237A238A239A240A241A242A243A244PARIANMERCURYVX300A245A238A239A240A241A246A247A248A249TMSA250A251A252A237A253A243A244LCQDECAXPPLUSA245A253A243A246A247A248A237A254A255A244X5A245A24A0A254A255A247A248A246A247A248,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,1374MMOLA182A18350MLCH2CL2A184A185A186A187A188A189A190A191A19226MLA193A194A195A19615MLA197A198A199A200A201A202A203A204A205A206A207A208A209A21010A211A212A213A209A210A203A214A215A202A216A217A196NAHCO3A218A21950ML3A220A221A222A223A224A200A225A215A222A223A224A22650MLH2OA220A221A227A228A200A222A223A224A229A230A231A194A232A233A234A200A235A236A237A238CH2CL2A218A239A200A240A241A233A234A200A242A243A244A245A246A247371GA248A249A250835A248MP120123A251A2523A253A254A255A23A15A0A4A17A1A2A17A1A61A138A3A4A5100G,1361MMOLA67A670MLA69A7A8A9A67A101MOLL1A74A25A75A11A12A13A14A16A185A81A19A20A133A21A22A242A25A121A26A27A28A29478GA25A122A30970A25MP112117A31A322OA33A34A353A36A35A37A38A37A38A39A40A5A41A42A43A41A42A443A123A45A46A47A48A49A4142G,240MMOLA50A51100MLCH2CL2A52A53A76A54A55A56A57A58A5956MLA127A60A62A6332MLA129A127A64A53A58A59A89A65A66A68A76A54A70A8010A71A72A73A77A78A79A823A53A83A84A85A86A87A885125GA53A90A91823A92MP117120A93A94112A95A96A97A98A99A100A101A96A97A99A100A1023O2A1035A104A105A104A105A106A107A108A105A107A108A1059A109A1109AA111A1129AA113A114A115A116A117A113A114A115A116AI1A118A119A120A118A119A120A124A125A1262OA128A130A1313A132A1319A134A1359AA136A1379AA139A140A141A142A143A319G,323MMOLA1442A1455A146A147A148A149A15020G,970MMOLA151A15230MLCH2CL2A153A154A1550A156A157A158A159A160A161A162A163DCC20G,970MMOLA144DMAP04G,323MMOLA154A155A164A165A159A160A161A166A167A168A1694A170A171A168A169A172A173A174A154A175A168A169A176A177A178A154A178A176A162A16340MLH2OA1792MOLL1NAOHA180PHA181A18289A154A183A176A154A184A185A186A183A187A17940MLA188A144NACLA151A176A14440MLH2OA189A190A191A192A154A193A194A195A150A196A197A198A154A199A200A201A202CH2CL2A151A203A154A204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,7053C2,6563C3,2647C4,6830C5,21335ME,40333NME2,16433C1,13186PHENYL1C,13539PHENYL2C,12913PHENYL3C,13335PHENYL4C,12678PHENYL5C,13325PHENYL6CA1293O4A132A133A134A135A132A133A134A138A139A134A135A139A1349A140A132A140A1329AA141A1429AA139A1359AA143A144A145A146A147A143A144A145A146AA1484A149A150A151A152A153A154A155A156535A154MP198202A157A158UVMAX/NMA159210A158IR/CM1A1593503OHA1543329OHA1542975ASCH3A1542933ASCH2A1542851SCH3A1541744COA1541577CCA1541235COA1541172COA1583O2NA160A161A162A163A164A161A162A161A1629A165A1669AA168A1699AA164A1629AA170A171A172A173A174AA1755A176A177A178A179A180A181A182A183371A181MP98100A184A185UVMAX/NMA176226A181250A181306A185IR/CM1A1763272OHA1813123OHA1813015OHA1812957ASCH3,1591CCA1811692COA1811268COA1811237COA181764A186A1853O4A187A188A189A187A188A189A190A191A189A191A1899A192A1939AA194A1959AA190A1899AA196A197A198A199A200A197A198AA2016A202A203A204A205A206A207A208A209445A207MP195200A210A211UVMAX/NMA212216A211IR/CM1A2123414OHA2072975ASCH3A2072935ASCH2A2072874SCH3A2071737COA2071567CCA2071277COA2071174COA2071118COA207787A213A21113CNMRCDCL3,300MHZ,A21217598C1,4307C2,7419C3,4188C4,8636C5,7555C6,3627C7,2816C8,6947C9,6251C10,7098C11,7312C12,7821C13,15912ME,7654ME,26476ME,11008ME,36729ANCH3,214410ME,160112ME,207813CH2,90313ME,10249C1,7054C2,6565C3,2626C4,6925C5,21015ME,40093NME2,16432C1,15074PYRIDYL2C,12353PYRIDYL3C,13740PYRIDYL4C,12345PYRIDYL5C,15029PYRIDYL6CA2113O3A214A215A216A215A216A217A218A216A218A2169A219A2209AA221A2229AA223A2249AA225A226A227A228A229A226A227A228AA2307A231A232A233A234A235A236A237A238395A236MP9598A239A240UVMAX/NMA241210A240IR/CM1A2413408OHA2423328OHA2422932ASCH2A2422853SCH3A2421728COA2421576CCA2421172COA2421113COA2403O3A243A244A245A246A247A2449A248A2499AA250A2519AA252A2449AA253A254A255A12A0AA18A167A52A2A3A4A25A122A58601A25MP250253A5A40UVMAX/NMA167212A25278A18IR/CM1A1673311OHA252975ASCH3A252937ASCH2A252875SCH3A251739COA251717COA251638CCA251172COA25771A6A713CNMRCDCL3,300MHZ,A817662C1,4340C2,7332C3,4016C4,8683C5,7819C6,4213C7,2852C8,6950C9,6271C10,7132C11,7443C12,7819C13,16052ME,7884ME,26646ME,11218ME,36969ANCH3,216310ME,162312ME,210113CH2,93013ME,10291C1,7068C2,6588C3,2645C4,6872C5,21295ME,40163NME2,16636C1,11867C2,14581C3,13444PHENYL1C,12831PHENYL2C,12928PHENYL3C,13077PHENYL4C,12928PHENYL5C,12831PHENYL6CA73O2A29A9A10A37A11A13A10A11A139A14A15A14A159AA16A17A16A179AA32A109AA19A20A21A22A23A21A22AA249A26A27A28A30A31A33A34A35492A33MP178181A36A38UVMAX/NMA26214A33276A38IR/CM1A263265OHA333063OHA332932ASCH2A332854SCH3A331709COA331645CCA331594CCA331223COA33766A39A383O3A41A42A43A42A43A42A44A45A46A42A44A459A47A489AA49A50A49A509AA51A429AA53A54A55A56A57A55A56AA5910A60A137A61A62A63A64A65A66283A64MP165168A67A68UVMAX/NMA60260A68IR/CM1A603311OHA642975ASCH3A642937ASCH2A642875SCH3A641739COA641717COA641638CCA641172COA64771A69A683O3,5A70A71A72A73A74A73A70A71A72A73A74A73A75A76A77A73A76A779A78A729AA79A809AA71A739AA81A82A83A84A85A81A82A83A84AA8611A87A88A89A90A91A92A93A94396A92MP161165A95A96UVMAX/NMA97212A92283A96IR/CM1PICTURE82A973240OHA923047OHA923004OHA922931ASCH2A922854SCH3A921716COA921692COA921647CCA921610CCA921208COA921158COA921065COA92838A98A9612体外抗菌活性试验A179A180A181A99A100A101A102A103A187A104A103ATCC25923A105A189A106A107A108A103ATCC49619A105A181A99A100A109A102A103A110A111A112A103ATCC25922A113A114A181A99A100A101A102A197A115A103A116A187A104A1038195A200A201A117A118A119A197A115A202A105A189A106A107A108A1038220A200A201A117A118A119A197A115A202A120A181A99A100A109A102A103A156A121A112A1038227A204A123A124A125A103A116A105A126A127A128A129A130A131A201A132A133A134A135A136A138A139A1403A141A142A143A144A145A146A147A148A149A150A151A140A200I1I11A152A152A153A1531A15311A154A221A155A157A158A159A160A161A162A163A164A165A166A168A169A170AA171EMAA154A172A173A174A169A170A171AZMA154A175A176A177A178A226A182A183A184A185A186A188A190A191A192A193A194A195MICA196A182A198A199A230A203A2051A196二、结果与讨论21A233A206A186A207A20822A235A185A186A188A209A210A203A211A212A213A214A178A223A193A215A216A238A217A199A230A218A2051A219A205A232A178A185A186A188I1A220A220A222A2221A220A220A222A2222A220A220A222A2223A220A220A222A2224A224A225A227A228A229A231A234A236A2288220A237A239A228A240A241A242A243A244A245A246A247A248A249A246A247AA250A251A252A253A2541A255A2542A255A2543A201A0A1A2A3A4A5A6A7A8A5ATCC25922A104A9A10A8A58227A69A223A11A12A13A14A15A16A17A18AA19A163A20A21A221A23A24A25A26A27A13A11A28A29A30A118227A31A223A11A12A13A32A33A34A17A18A103A35A36A242A37A38A39A40A41A42A43A187A44A45ATCC25923A243A189A46A47A48A45ATCC49619A49A50A51A52A43A138A53A54A55A56A57A54A55AA244A37A58A59A60A61A62A247A63A64A65A36A38A39A40A41A42A213A57A54A55AA52A66A43A67A68A70A71A51A45A49A72A45A50A51A37A66A224A58A59A49A60A61A62A253A73A213A74A75A76A165A77A62A8315A217A78A79A80A81A49A82A84A85A86A98A87A108A88A78A89A90A62A91A92A93A94A95A96A60A97A37A99A100A101A95A36TABLE1ANTIBACTERIALEFFECTSOFAZALIDESAGAINSTPATHOGENSA102A105A106MICG/MLA107A109A110ATCC25923A107A109A1108195A111A112A113A114A110ATCC49619A111A112A113A114A1108220A115A116A117A110ATCC25922A118A119A117A1108227I13212816812832I264128646412864I312812812864128128I4641288128128128I512812812864128128I6128128128128128128I7128128128128128128I8128128128128128128I9128128128128128128I10128128128128128128I1112812812812812864A12014128216168A1202161284163232A1203321282163232A1204641286416128128A120512812832128128128A1206321284646432A120764128464128128A120812812832128128128A1209128128128128128128A1201012812816128128128A12011128128128128128128AZM05128053248EMA02512802564646422初步构效关系研究A121C3A122A123A124A125A126A127A128A133A129A221A130A131A132A143A134A135A136A129A137A139A140A141A142A144A141A145A146A147A148A149A150A151A152A153A154A155A156A157A158A159A160A161A162A164A166A153A142A145A146A167A168A129A177A157A169A170A143A162A160A171A169A162A164A166A153A129A144A141A145A146A172A173A129A178A174A175A176A179C3A122A180A181A158A159A160A182A183A184A162A185A142A131A132A162A164A166A137A186A188A144A141A145A146A157A190A191C3A122A180A154A192A193A143A162A194A195A164A166A162A221A130A164A166A142A134A196A197A142A144A141A145A146A198A251A167A199A129A200A202A203A164A166A162A185A204A205A129A206A146A207A208A251A167A209A129A210A211A212A214A235A215A184A142A216A146A129A218A219A203A220A141A222A126A225A142A207A196A226A173A157A227A1919ANA171A162A228A229A197A2039ANA230A228A229A197A142A144A141A145A146A251A167A129A231A2329ANA156A157A171A162A164A166A142A228A229A197A144A141A145A146A233A234A188A236A237A238A155A156A239A157A171A162A164A166A142A228A229A197A129A178A174A175A176A200A202A178A2369ANA156A171A162A164A166A133A240A241A146A245A246A137A186A188A144A141A145A146A157A190A19123药效团模型验证A248A249A250A252A254A255A66A255A33A100A0A59A97A60A6926A61A93A62A51A0A1A2A3A4A69MICA12A53A25A64A6A7A65A102A8A9A198A10A11A13A68A14CATALYSTA15A121A16A17A70A18A19A71A20A55A243A19A71A21A55A243A22A23A74A24A104A75A72A74A24A26A27A28A29A30A31A17A198A32A34A35A36A15A152A35A36A17TATOLCAST10855,RMS0713364,CORREL08754A15WEIGHT115832,CONFIG8166097A201A152A35A36A37A38A39A80A40A41A172A81A42A43A82A240A15A83A44A45A42A152A35A36A200A852A200A86A202A202A201A46A11A13A17A87A235A47A48A10A37A38A88A49A50A179A15A91A55A52A53A54A562A57A582A63A67A73A76A77A78A79A84A89A90A92A94A95A92A96A98A99A101A103A105A106A107A108A109A110A111A107A112A63A67A73A76A84A89A90A92A94A95A96A98A99A101A103A105A106A107A109A110A111A107A95A92A96A106A107A112A106A107MG/LA111A107A112A111A107MG/LFITA112A113A67A114A115A116A117A113A67A115A116KCAR/MOLI1190132536790I2116645565931065I3236128525153115536I9141128549633790323II151145954866II21554165455855004II32406325257560II622332526977159385II72516452135913599II93248645141121044II1114051285514690688A178A1182A119A120A122A123A124A125A126A127A128A129A130A131A132A133A134A135A136A137A119A120A122A138A139A137A140A141A142A127A143A144A145A146A147A148A149A150A151A127A153I1A119A13
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