新型过渡金属配合物的合成、表征及生物活性研究

为了寻找更好的生物活性化合物,以1-苯基-3-甲基-5-吡唑啉酮和苯甲酰氯为原料,二氧六环为溶剂,回流反应合成了4-酰基吡唑啉酮配体及4种过渡金属配合物,通过元素分析、红外光谱、差热-热重分析、紫外光谱等对其结构进行了表征,表明配合物组成分别为:Cu(L)2、Zn(L)2、Ni(L)2、Mn(L)2;同时利用抑菌圈大小...     

过渡金属配合物的合成、性质及生物活性研究

金属配合物药物在疾病的治疗中起着重要的作用,过渡金属钴的配合物在药物学、配位化学和生物无机化学学科具有重要的作用.钴是组装配位聚合物时常选用的金属元素,钴离子易与含氮、氧配位原子的配体形成配合物,能与羧基以多种配位方式组成不同类型的配合物.含羧基类配体是常用的有机配体,具有良好的柔韧性,通常能形成结构新颖的配合物.其分...     

烯效唑Fe(Ⅱ)配合物的合成、结构及生物活性研究

合成了新的配合物[FeL_4Cl_2](L=(E)-1-对氯苯基-2-(1,2,4-三唑-1-基)-4,4-二甲基-1-戊烯-3-醇,采用元素分析EA、红外光谱IR和X射线单晶衍射方法对配合物的组成及结构迚行表征。该配合物晶体属于三斜晶系,P-1空间群,晶胞参数如下:a=8.989 6(5)(?), b=13.0714(9)(?), c=14.717 5(12)(?),α=93.089(3)°,β=99.809(3)°,γ=104.408 (4)°, V=1 642.1(2)?~3,Dc=1.308 g?cm~(-3), F(000)=676。研究了配合物及烯效唑对苹果干腐Ⅰ、苹果轮纹Ⅱ、小麦赤霉Ⅲ和葡萄黑豆Ⅳ四种病菌的抑制活性。结果表明:配合物的抑菌活性优于配体。对于葡萄黑豆病菌Ⅳ,配合物毒力指数是配体的3.66倍。与配体相比,FeCl_2与烯效唑配位后可提高生物活性。     

稀土三元配合物的合成、表征及其生物活性研究

以氯化镧、席夫碱、邻菲啰啉为原料,制备了新型稀土镧三元配合物,通过元素分析、紫外光谱、红外光谱、透射电子显微镜等手段对其进行了表征,确定了三元配合物的化学组成为La(L)phen(NO3)3C2H5OH.CH3OH。抗菌实验结果表明,配合物对大肠杆菌和金黄色葡萄球菌的抑菌圈直径分别为26 mm和20 mm,最小抑菌浓度分别为60 mg/L和130 mg/L,具有较强的抑制作用,且对大肠杆菌的抑制效果较强。     

吡啶羧酸铬配合物的合成及其生物活性

报道了3种吡啶羧酸铬配合物的合成,其结构经元素分析,IR,^1HNMR和MS表征。以2－吡啶甲酸铬配合物饲喂猪的试验表明,它是一种很有效的饲料添加剂。     

稀土联咪唑对羟基苯甲酸配合物的合成、表征及生物活性

以稀土氯化镧、联咪唑和对羟基苯甲酸为原料,制备了一种新型稀土三元配合物,通过元素分析、红外光谱、紫外光谱、XRD、TEM对其进行表征,确定了该配合物的化学组成为:La(Hbiim)3N(Hbiim=2,2’-联咪唑,N=对羟基苯甲酸)。抗菌实验结果显示,三元配合物抑菌圈直径为13～17 mm,说明配合物对大肠杆菌、金黄色葡萄球菌具有一定的抑制作用,且对金黄色葡萄球菌的抑制效果较好,抗菌谱广。     

氨荒酸三丁基锡配合物的合成及生物活性初步研究

合成了１０个新的氨荒酸三丁基锡配合物,利用元素分析、ＩＲ、＾１ＨＮＭＲ表征了其结构。生物活性初步研究表明,某些配合物具有一定的杀菌活性。     

稀土钐二元、三元配合物的合成、表征及其生物活性研究

以氯化钐、2-氨基嘧啶和钼酸钠为原料,制备了两种新型稀土钐二元、三元配合物,通过元素分析、紫外光谱、红外光谱等手段对其进行了表征,确定了二元配合物的化学组成为Sm2(AP)(H2O)2Cl3(AP=2-氨基嘧啶),三元配合物的化学组成为:Sm3(AP)(MoO4)2(CH3OH)4Cl5。抗菌结果表明,二元配合物对大肠杆菌和金黄色葡萄球菌的抑菌圈直径分别为13 mm和15 mm,三元配合物分别为13 mm和13 mm,两种配合物对大肠杆菌、金黄色葡萄球菌都有一定的抑制作用。采用MTT法对两种配合物诱导癌细胞凋亡能力做了初步研究,两种配合物的半数抑制浓度IC50在0.001~0.01 mg/mL之间,证明其具有诱导癌细胞凋亡的作用。     

吡啶鎓阳离子对镍配合物的合成及表征

合成了马来二氰基二硫烯镍(Ⅱ)配合物[1-NaPhthMePyNH_2]_2[Ni(mnt)_2]([1-NaPhthMePyNH_2]~+为1-(1′-奈苄基)-2-氨基吡啶鎓离子),并用元素分析,UV,IR,单晶X射线衍射表征了其组成和结构。结果表明:配合物系三斜晶系,空间群P_(-1),a=0.764 78(15)nm,b=0.949 88(19)nm,c=1.360 9(3)nm,α=92.491(2)°,β=103.784(2)°,γ=105.723(2)°,V=918.0(3),Z=1。     

Zn(Ⅱ)配合物合成及生物活性研究进展

综述了近年来Zn(Ⅱ)配合物的合成及生物活性研究,对发展前景作了展望。     

槲皮素镁的合成、表征及其生物活性研究

介绍了槲皮素镁的合成方法,通过紫外光谱、红外光谱、核磁氢谱和同步热分析进行了表征。氢谱显示镁离子在3-OH和3’-OH位置与槲皮素配位,同步热分析确证了这个结果。通过1,1-二苯基-2-三硝基苯肼(DPPH)法测定了槲皮素镁清除自由基的能力,结果显示,槲皮素镁清除自由基的能力没有槲皮素强。经常食用含有槲皮素的黄酮类蔬菜和水果,如洋葱、苹果、柑橘等,可清除体内的自由基,使机体免受自由基的损伤,对降低人体内重金属离子的含量起着重要的作用。     

Synthesis,Characterization and Biological Evaluation of Transition Metal Complexes Derived from N,S Bidentate Ligands

Two bidentate NS ligands were synthesized by the condensation reaction of S-2-methylbenzyldithiocarbazate (S2MBDTC) with 2-methoxybenzaldehyde (2MB) and 3-methoxybenzaldehyde (3MB). The ligands were reacted separately with acetates of Cu(II), Ni(II) and Zn(II) yielding 1:2 (metal:ligand) complexes. The metal complexes formed were expected to have a general formula of [M(NS)₂] where M = Cu²⁺, Ni²⁺, and Zn²⁺. These compounds were characterized by elemental analysis, molar conductivity, magnetic susceptibility and various spectroscopic techniques. The magnetic susceptibility measurements and spectral results supported the predicted coordination geometry in which the Schiff bases behaved as bidentate NS donor ligands coordinating via the azomethine nitrogen and thiolate sulfur. The molecular structures of the isomeric S2M2MBH (1) and S2M3MBH (2) were established by X-ray crystallography to have very similar l-shaped structures. The Schiff bases and their metal complexes were evaluated for their biological activities against estrogen receptor-positive (MCF-7) and estrogen receptor-negative (MDA-MB-231) breast cancer cell lines. Only the Cu(II) complexes showed marked cytotoxicity against the cancer cell lines. Both Schiff bases and other metal complexes were found to be inactive. In concordance with the cytotoxicity studies, the DNA binding studies indicated that Cu(II) complexes have a strong DNA binding affinity.     

Caffeine-Cyclodextrin Complexes as Solids: Synthesis,Biological and Physicochemical Characterization

Mechanochemical and in-solution synthesis of caffeine complexes with α-, β-, and γ-cyclodextrins was optimized. It was found that short-duration, low-energy cogrinding, and evaporation (instead of freeze-drying) are effective methods for the formation and isolation of these complexes. The products obtained, their pure components, and their mixtures were examined by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), FT-IR and Raman spectroscopy. Moreover, molecular modeling provided an improved understanding of the association process between the guest and host molecules in these complexes. The complexes were found to exhibit high toxicity in zebrafish (Danio rerio) embryos, in contrast to pure caffeine and cyclodextrins at the same molar concentrations. HPLC measurements of the caffeine levels in zebrafish embryos showed that the observed cytotoxicity is not caused by an increased caffeine concentration in the body of the organism, as the concentrations are similar regardless of the administered caffeine form. Therefore, the observed high toxicity could be the result of the synergistic effect of caffeine and cyclodextrins.     

Synthesis,Characterization and Catalytic Activities of Palladium(II) Nitroaryl Complexes

Two palladium(II) nitroaryl complexes trans-[bromo(p-nitrophenyl)bis(triphenylphosphine)palladium(II)] 1 and trans-[bromo(2,4-dinitrophenyl)bis(triphenylphosphine)palladium(II)] 2 have been synthesized. The complexes were characterized by FTIR and NMR (¹H, ¹³C and ³¹P) spectroscopy and elemental analysis. The molecular structure of complex 2, as confirmed by X-ray crystallography, reveals that the Pd atom and its neighboring groups (two PPh₃, Br and phenylene group) lie in a slightly distorted square plane. In the UV–Vis spectra of the complexes 1 and 2, the palladium to aryl charge transfer bands were observed. The emission peaks from the singlet excited states (S₁ → S₀) were observed in the photoluminescence spectra of the complexes. The thermal stability of the complexes has been studied by thermal gravimetric analysis (TGA). TGA data showed that both complexes are thermally stable up to 200 °C, and complex 1 is more stable than 2. The catalytic efficiency of the new palladium(II) complexes was studied as demonstrated using the Sonogashira coupling reactions with good yields. The experimental results suggest that the Sonogashira coupling reactions can be performed at moderate temperature (50 °C) using these new palladium(II) complexes as catalysts.     

阿魏酸双苄酯的合成及生物活性研究

摘要：以DMSO为溶剂,以阿魏酸与氯化苄在碱性条件下反应,合成了阿魏酸双苄酯,产率为94．32％、纯度为98．5％。通过紫外光谱、红外光谱、核磁共振氢谱、质谱及X-单晶衍射对产物结构进行了表征。用微量量热法证明了阿魏酸双苄酯对大肠杆菌具有一定的抑制作用,其最小抑茵浓度（MIC）为29．81btg·mL-1。通过紫外光谱、荧光光谱和粘度测定研究了阿魏酸双苄酯与ct-DNA的相互作用,证明其作用方式为经典插入方式,对ct-DNA的猝灭是由于形成复合物所引起的静态猝灭,与ct-DNA的结合常数为1．58×10。L·mol-1。     

Ruthenium(III) Complexes of Heterocyclic Tridentate (ONN) Schiff Base: Synthesis,Characterization and its Biological Properties as an Antiradical and Antiproliferative Agent

The current work reports the synthesis, spectroscopic studies, antiradical and antiproliferative properties of four ruthenium(III) complexes of heterocyclic tridentate Schiff base bearing a simple 2′,4′-dihydroxyacetophenone functionality and ethylenediamine as the bridging ligand with RCHO moiety. The reaction of the tridentate ligands with RuCl₃·3H₂O lead to the formation of neutral complexes of the type [Ru(L)Cl₂(H₂O)] (where L = tridentate NNO ligands). The compounds were characterized by elemental analysis, UV-vis, conductivity measurements, FTIR spectroscopy and confirmed the proposed octahedral geometry around the Ru ion. The Ru(III) compounds showed antiradical potentials against 2,2-Diphenyl-1-Picrylhydrazyl (DPPH) and 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radicals, with DPPH scavenging capability in the order: [(PAEBOD)RuCl₂] > [(BZEBOD)RuCl₂] > [(MOABOD)RuCl₂] > [Vit. C] > [rutin] > [(METBOD)RuCl₂], and ABTS radical in the order: [(PAEBOD)RuCl₂] < [(MOABOD)RuCl₂] < [(BZEBOD)RuCl₂] < [(METBOD)RuCl₂]. Furthermore, in vitro anti-proliferative activity was investigated against three human cancer cell lines: renal cancer cell (TK-10), melanoma cancer cell (UACC-62) and breast cancer cell (MCF-7) by SRB assay.     

脂肪仲胺合成及应用

本文介绍了脂肪仲胺的反应原理、生产工艺及其应用。     

4-酰基吡唑啉酮过渡金属配合物的合成、表征及生物活性研究

合成了4种4-酰基吡唑啉酮过渡金属配合物,通过元素分析、红外光谱、差热-热重分析、紫外光谱等对其结构进行了表征,同时对2种细菌和6种真菌进行了生物活性测试。结果表明,在不同浓度梯度下,配合物对细菌均有一定的抑制作用,大部分配合物对真菌有好的抑制作用,特别是对米曲霉菌和白地霉菌的抑制效果最好。     

4-酰基吡唑啉酮过渡金属配合物的合成、表征及生物活性研究

为了寻找更好的生物活性化合物,合成了两种4-酰基吡唑啉酮类过渡金属配合物,通过元素分析、红外光谱、差热-热重分析、紫外光谱等对其结构进行了表征,同时对两种细菌和3种真菌进行了生物活性测试。结果表明,在不同浓度梯度下,化合物对细菌都有一定的抑菌性,大部分化合物对真菌有好的抑菌性,特别是对米曲霉菌和白地霉菌的抑制效果最好。