简介：

简介：Aseriesoffuroxan-basednitricoxide-releasingmatrinederivatives(10a-f)weresynthesized.Thebiologicalevaluationshowedthatcompounds10a,10b,10eand10fhadstrongercytotoxicactivitiesthan5-fluorouracilagainsthumanhepatomacells(HepG2)invitro.

简介：Fromthepress-residueofthefreshroottuberofTrichosantheskirilowiiMaxim(Cu-curbitaceae),anewribosome-inactivatingprotein(RIP),trichobitacin,wasisolated.IthastheactivityofRNAN-glycosidaseandcaninhibitthegrowthofhumanplacentaltrophoblasticcells.Itsmolecularweightis27,228Da(ES-MS)andpI9.6.ItisasinglechainbasicRIP.Itsaminoacidcompositionwasdetermined.ItisanewRIP.Itconsistsof0.7~0.9%galactoseandmaybeaglycoprotein.ItsA’-andC-terminalaminoacidisAspandAla,respectively.ItsN-terminalpreliminaryaminoacidsequencehasbeendetermined.

简介：Thetwocompounds,2,2-dimethyl-4-S-(N,N-dimethyldithiocarbamato)-5-(1,2,4-triazol-l-yl)-propione(1)and2,2-dimethyl-4-S-(N,N-diethyldithiocarbamato)-5-(1,2,4-triazol-1-yl)-3-propione(2),werepreparedbyreactingN,N-dialkyldithiocarbamatesodiumwith2,2-dimethyl-4-bromo-5-(1,2,4-triazol-1-yl)-propione.Theirstructureswereidentifiedbyelementalanalysis,IRand^1HNMRspectroscopy.Thestructureof1hasbeendeterminedbyX-raysinglecrystalstructureanalysis.ItcrystallizesinmonoclinicsystemwithspacegroupP21/c,a=1.2315(3)nm,b=1.2057(2)nm,c=1.2532(3)nm,β=118.55(3)°,Z=4,V=1.6345(6)nm^3,Dc=1.221g/cm^3,μ=0.324mm^-1,F(000)=640,finalR1=0.0449.ThereisobviouspotentiallyweakC—H...Nintermolecularinteractioninthecrystal,whichstabilizesthecrystalstructure.Theresultofthebiologicaltestshowedthatthetwocompoundshavefungistasisandplantgrowthregulatingactivities.

简介：TwoN-dichloroacetyloxazolidinesweresynthesizedwithasimple,mildandconvenientmethod.AllthecompoundswerecharacterizedbyIR,^1HNMRandelementalanalysis.Thepreliminarybiologicaltestshowedthatthecompoundsprotectedmaizeagainstinjurybysomeherbicidestosomeextent.

简介：Aseriesofethyl6-alkoxy-7-phenyl-4-hydroxy-3-quinolinecarboxylatesweredesignedandsynthesized.Theirstructureswereconfirmedby~1HNMR,~(13)CNMR,IRandHRMS.ThebiologicalactivitieswereprimarilyevaluatedagainstEimeriatenellaaccordingtoAnticoccidialIndex(ACI)methodinvivo.Theresultsshowedthatcompounds5e,5fand5iexhibitedanticoccidialactivitiesagainstE.tenellaat27mgkg~(-1).

简介：Shortpeptidesbasedonthetripeptides,Leu-Arg-ProandLeu-Lys-Pro,weresynthesizedbymicrowaveassistedsolid-phasesynthesismethod,inordertomakeasearchforpotentialinhibitorsforangiotensinI-convertingenzyme(ACE)withminimumsideeffectsinthetreatmentofhypertension.OnepeptidewiththesequenceLeu-Arg-Pro-Phe-PheshowsthestrongestinhibitiontowardsACEwithanIC50valueof0.26μmol/Linvitro.Thestudyofstructure-activityrelationshipshowsthattheintroductionofabulkygroupintotheN-terminalofthisseriesofinhibitorsmayenlargesterichindrance,resultinginthepoorinhibitoryactivitytowardsACE.TheinhibitoryactivitydecreasedinturnwhenL-Pro,D-ProorAc6cwasattheC-terminalrespectively.ThebindinginteractionbetweeneachoftheseinhibitorsandtesticularACE(tACE)wasperformedbymoleculardocking.TheresultssuggestthatLeu-Arg-Pro-Phe-PhemainlyoccupiedtheS1subsiteoftACE,andmadecontactwithtACEviasevenH-bonds.ItappearedthatthesiteonthepeptidethatboundwithtACEwasinfluencedbytheconfigurationoftheaminoacid,LorD-form,attheC-terminalofthepeptide.

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简介：AseriesofnovelN-（3-furan-2-yl-1-phenyl-1H-pyrazol-5-yl）amidesderivativesweredesignedandsynthesized.Theirstructureswereconfirmedby1HNMR,13CNMRandHRMS.Alltitlecompoundswereevaluatedfortheirherbicidalandantifungalactivities.Preliminarybioassayresultsindicatedthatthetitlecompoundsshowedgoodtomoderateherbicidalactivityat1000mg/L.Compound6qpresentedthebestactivityagainstDigitariasanguinalis（L）Scop.,AmaranthusretroflexusL.andArabidopsisthalianawithaninhibitiondegreeoffive.Compound6dalsoshowedaninhibitiondegreeoffiveagainstD.sanguinalis.Inaddition,at50mg/L,mostcompoundsexhibitedgoodinvitroantifungalactivityagainstSclerotiniasclerotiorum,withcompound6cshowingover90%antifungalactivityagainstS.sclerotiorumandPelliculariasasakii.

简介：二新-hydroxy氨基的联合酸的secoiridoids，命名serinosecologanin(1)和threoninosecologanin(2)，从忍冬装饰用的梨树的花芽的一篇水的摘录被孤立。他们包括绝对配置的不平常的结构被分光镜的数据分析决定，并且从共同发生的secologanin(3)和secologanic酸(4)由semisynthesis证实了。从曲霉属菌尼日尔从杏仁和hesperidinase对-glucosidase加重1和2项展出抵抗活动，他们也在激活血小板的因素与抑制率导致的老鼠polymorphonuclear白血球对glucuronidase的版本显示出活动(34.9 ；± ；3.1)%并且(53.6 ；± ；2.6)%分别地。

简介：一系列2,4,5-triaryl在vitro作为ALK5禁止者代替了1H-pyrazol-3(2H)-ones,，是desigened，综合并且评估。大多数混合物在1μmol/L展出了显著ALK5抑制活动并且没在30μmol/L显示重要cytotoxicities。

简介：一系列5-phenyl-3H-spiro[indoline-3,2-[1,3,4]thiadiazol]-2-one类似物被综合并且他们的Bcl-2蛋白质禁止的活动被学习。铅混合物原来用荧光被识别基于极化的竞争有约束力的试金。在调查的10混合物之中，1k分别地显示出好有约束力的亲密关系到Bcl-xL和Mcl-1，与8.9mol/L和3.4mol/L的抑制常数。当复合1c完成了紧密的有约束力的亲密关系到Bcl-xL时(Ki=0.16mol/L)，有潜力是新铅混合物。