1,2,4-噁二唑类化合物的合成及抗菌活性研究

以对溴苯腈为原料,通过多步反应合成了一系列3-(吗啉苯基)-5-取代-1,2,4-异噁唑类化合物和3-(吗啉苯基)-5-取代-4,5-二氢-1,2,4-噁二唑类化合物,并用1HNMR、13C NMR和MS进行了结构确证。这些化合物对测试的部分革兰氏阳性菌,如金黄色葡萄球菌、耐甲氧西林金黄色葡萄球菌、表皮葡萄球菌、粪肠球菌显示出一定的抗菌活性,但与噁唑烷酮类上市药物利奈唑胺相比,抗菌活性有明显下降。这一结果表明对于化合物的抗菌活性,1,2,4-噁二唑杂环不如噁唑烷酮结构有效。     

三芥子酸甘油酯类似物的合成及抑菌活性

以N-(2-溴乙基)邻苯二甲酰亚胺或N-(4-溴丁基)邻苯二甲酰亚胺和硫氢化钠为起始原料,通过取代、肼解、亲核加成等反应合成了10个三芥子酸甘油酯(erucin)类似物,通过核磁共振氢谱、碳谱及质谱对其结构进行了确认。采用比浊法初步测试了其对大肠杆菌、金黄色葡萄球菌、白色葡萄球菌、藤黄八叠球菌、枯草芽孢杆菌、蜡状芽孢杆菌和四联球菌等7种菌的生长抑制活性,测试结果显示,化合物对测试菌种都表现出较好的生长抑制活性,其中苄硫乙基-1-硫代异硫氰酸酯(5e)和苄硫基丁基-1-硫代异硫氰酸酯(5j)活性最高,对大肠杆菌的最低生长抑制浓度仅为7.8μg/m L,对金黄色葡萄球菌的最低生长抑制浓度也仅为15.6μg/m L和31.2μg/m L。     

Synthesis and antibacterial activity of novel 10, 11-epoxy acylide erythromycin derivatives

A series of novel acylide derivatives have been synthesized from clarithromycin A via a facile procedure. The C-3 modifications involved replacing the natural C-3 cladinosyl group in clarithromycin core with different aryl-piperzine sidechain via chemical synthesis. Meanwhile a distinctive intermediate with 10,11-epoxy moiety was obtained. The structure and stereochemistry of this novel structure were confirmed via NMR and X-ray crystallography. Potential anti-bacterial activities against both Grampositive and Gram-negative bacteria were reported. Because of existence of C10,11-epoxide, these derivatives can be used as intermediates for further structural modification.     

Synthesis and antibacterial activity of hydroxylated 2-arylbenzothiazole derivatives

Abstract

N-acyliminium reagents formed in situ from benzothiazole and alkyl chloroformates react with hydroxyarenes in a Friedel-Crafts manner, providing access to 2-(hydroxyaryl)-benzothiazolines with antibacterial properties.     

水杨酰肼Schiff碱的合成、表征及抑菌活性

Sehiff碱具有多个氧、氮配位原子,是一类重要的生物配体,某些Schiff碱具有抗癌、抗病毒、抑制细菌生长等生物活性。本文制备了两个水杨酰肼类Schiff碱化合物,并探讨了结构组成、波谱性能及抑菌活性。     

苄基三苯基季鏻盐的合成及其晶体结构和抗菌活性测定

合成了1种苄基三苯基季鏻盐——氯化苄基三苯基季鏻盐([BzTPP]+Cl-);利用元素分析、红外光谱、电子喷雾质谱和X射线单晶衍射对其进行了组成分析和结构表征;采用二倍稀释法测定了其抗菌活性,并与季鏻盐[BzTPP]2[CoCl4]和[BzTPP]2[MnCl4]进行了对比.结果表明,合成的季鏻盐[BzTPP]+Cl-属于正交晶系,Pbca空间群,晶胞参数为:a=1.388 0(1)nm,b=1.717 0(2)nm,c=1.817 5(2)nm,α=β=γ=90°,V=4.131 3(7)nm3,Z=8,Dc=1.191g/cm3,GOOF=1.002,R1=0.038 4,wR2=0.113 6.该季鏻盐由Cl-离子和[BzTPP]+阳离子组成,阴、阳离子之间存在C-H…Cl氢键.与此同时,三种季鏻盐对大肠杆菌、金葡萄球菌及沙门氏菌均具有较好的抗菌活性.     

三氯新的结构改造及抑菌活性初探

本论文对三氯新的结构进行了改造,合成了四个未见文献报道的三氯羟基二苯醚衍生物,它们的结构均经红外、核磁、高分辨质谱证实.对新化合物进行了抗金黄色葡萄球菌和大肠杆菌活性的测试,其中有一个新化合物在20ug/mL浓度下对两种菌都有活性.     

新型N-取代苯甲酰基-N′-(4-甲基苯并噻唑-2-基)硫脲衍生物的合成、晶体结构及抑菌活性

以取代苯甲酸和2-氨基-4-甲基苯并噻唑为原料合成5个新型N-取代苯甲酰基-N′-(4-甲基苯并噻唑-2-基)硫脲衍生物,化合物结构经元素分析、IR、1 H NMR和13 C NMR表征,X-射线单晶衍射测定了N-(4-甲氧苯甲酰基)-N′-(4-甲基苯并噻唑-2-基)硫脲(化合物1)的晶体结构,该晶体为单斜晶系,P21/c空间群,选择广西主要经济作物中常见的病原菌,对目标化合物进行室内抑菌活性测试,实验结果发现该类化合物具有一定的抑菌活性.     

4-烷氧基苯甲醛-4-氨基安替比林希夫碱的合成及抑菌活性

报道了4-氨基安替比林与4-烷氧基苯甲醛缩合反应生成希夫碱的合成和抑菌活性,分子结构由1HNMR、IR和元素分析表征;抑菌活性测定结果表明,化合物(5a,5d,5e,5f,5g)对金黄色葡萄球菌、大肠杆菌、枯草杆菌、黑霉菌、青霉菌(抑菌环直径15.3 ～ 21.70 mm)均有较好的抑菌活性,其中化合物(5f)对黑霉菌(抑菌环直径26.20 mm)有优良的抑菌活性.     

Design, synthesis and anti-HBV activity of novel bis（trifluoroethyl）phosphonomethyl ether derivatives of acyclovir

A series of novel bis(trifluoroethyl)phosphonomethyl ether derivatives of acyclovir was synthesized and their in vitro anti-HBV activity was evaluated in HepG2 2.2.15 cells.In contrast to acyclovir,most of the described phosphonates emerged as potent inhibitors of HBV replication.Especially,the most active compound 11 with IC_(50)value of 2.92μmol/L was 33 times more potent than acyclovir with IC_(50)value of 100μmol/L.     

Synthesis and bioactivity evaluation of some novel sulfonamide derivatives

A simple and convenient method for the synthesis of biologically active sulfonamide derivatives was achieved. All the title compounds were characterized by spectral and elemental analysis. They were further screened in vitro for their abilities towards antibacterial, antifungal and antioxidant activities. The compound N,N'-(3,3′-dimethoxybiphenyl-4,4′-diyl)bis(4-fluorobenzenesulfonamide) (5b) and N-(3-(9H-carbazol-4-yloxy)-2-hydroxypropyl)-4-fluoro-N-isopropylbenzenesulfonamide (5e) exhibited good activity when compared to the standard bactericide, Chloramphenicol and fungicide, Ketoconazole respectively. The compounds (2S)-N-((2S,4S)-5-(4-Chloro-phenylsulfonamido)-4-hydroxy-1, 6-diphenylhexan-2-yl)-3-methyl-2-(2-oxotetrahydropyrim-idin-1(2H)-yl)butan-amide (4f) and (2S)-N-((2S,4S)-5-(4-fluorophenylsulfonamido)-4-hydroxy-1,6-diphenyl-hexan-2-yl)-3-methyl-2-(2-oxotetrahydropyrimidin-1(2H)-yl)bu-tana-mide (5f) exhibited good antioxidant activity when compared with standard antioxidant, Ascorbic acid.     

Ultrasound mediated green synthesis of rhodanine derivatives: Synthesis,chemical behavior,and antibacterial activity

A variety of rhodanine derivatives were synthesized via a three-component reaction of carbon disulfide, amines, and dialkyl acetylenedicarboxylate in polyethylene glycol under conventional stirring or ultrasound irradiation. The sonochemical-assisted procedure provides an improved and accelerated conversion when compared to the conventional reaction, with increased rate of reaction and quality of product obtained. The product formed, 2a, could be readily converted to bis-rhodanine under microwave conditions. Moreover, the pyranothiazoles 9a,b were prepared from the corresponding rhodanines 2a,b and malononitrile. Fifteen compounds were screened for their antibacterial activities against nine human, animal and plant pathogenic Gram-positive and Gram-negative bacteria using the agar well diffusion method. Out of these derivatives, compounds 2g and 2h were the most effective against all tested bacteria.     

Synthesis, antibacterial and antifungal activity of some derivatives of 2-phenyl-chromen-4-one

Some derivatives of 2-phenyl-chromen-4-one (flavone ring) have been synthesized and tested for antibacterial and antifungal activities along with their chalcone precursors against four human pathogenic bacteria and five plant mould fungi. The structures of the synthesized compounds were elucidated by UV, IR and¹H NMR spectroscopic techniques, and elemental analysis. The antibacterial and antifungal screens of the synthesized compounds were performed in vitro by the filter paper disc diffusion method and the poisoned food technique.     

氯取代二苯基苯甲酰基吡唑酮席夫碱的合成与抑菌活性

酰基吡唑啉酮及其席夫碱是一类杂环β─二酮螯合剂。其活性的双酮配位基可以同多种金属或稀土离子形成大量的配合物,是金属和稀土离子良好的萃取剂和螯合剂[1~5],是一类优良的荧光材料中间体,同时表现出一定的抗菌、抗病毒性能[6~11],目前在药理、生物活性试剂、冶金、染料、发     

Synthesis of nitrogen-containing monoterpenoids with antibacterial activity

Abstract

Incorporation of the Beckmann rearrangement into the presented research resulted in the formation of nitrogen-containing terpenoid derivatives originating from naturally occurring compounds. Both starting monoterpenes and obtained derivatives were subjected to estimation of their antibacterial potential. In the presented study, Staphylococcus aureus was the most sensitive to examined compounds. The Minimal Inhibitory Concentration (MIC) experiments performed on S. aureus demonstrated that the (?)-menthone oxime (?)-8 and (+)-pulegone oxime (+)-13 had the best antibacterial activity among the tested derivatives and starting compounds. Their MIC₉₀ value was 100?µg/mL. The obtained derivatives were also evaluated for their inhibitory activity against bacterial urease. Among the tested compounds, three active inhibitors were found – oxime 14 and lactams (?)-15 and 16 limited the activity of Sporosarcina pasteurii urease with K_i values of 174.3?µM, 43.0?µM and 4.6?µM, respectively. To our knowledge, derivative 16 is the most active antiureolytic lactam described to date.     

2,5-二(2-氨基乙氧甲基)噻吩合成及抑菌活性

噻吩烷基胺及其衍生物对疟疾、麻风、真菌、病毒和某些肿瘤均有较强的药理活性[1～ 2 ] ,因此合成和开发这类新物质具有重要的意义。以前 ,由 2 噻吩甲醛合成的噻吩类衍生物药物较多[3] ,但对噻吩双取代衍生物的合成研究还未引起重视。因此 ,为了探索这类化合物的性质和抑菌效果。我们合成了未见文献报道的 2 ,5 二 ( 2 氨基乙氧甲基 )噻吩 ,通过多种测试手段 ,确定了它的组成结构 ,其合成路线如下 :1　实验部分1 1　仪器与试剂Ｎｉｃｏｌｅｔ1 70Ｓ红外光谱仪 (ＫＢｒ压片 ) ,ＰＥ 2 4 0Ｃ型元素分析仪 ,ＥＭ 360 60ＭＨｚ核磁共振仪。…     

吡啶联喹唑啉酮衍生物的设计、合成与抗菌活性研究

以靛红酸酐为起始原料,设计并合成了14个结构新颖的吡啶联喹唑啉酮类衍生物.所有化合物经1 H NMR、13 C NMR和高分辨质谱(HRMS)表征确证其结构.初步抗菌活性结果显示,该类化合物对水稻白叶枯病菌(Xanthomonas oryzae pv.Oryzae,Xoo)、猕猴桃溃疡病菌(Pseudomonassyr...     

PMBP缩磺胺席夫碱及其铜配合物的合成与抑菌活性

4-酰基吡唑啉酮类化合物是一类重要的有机配体.其所具有的酮式和烯醇式异构体并存且含有多个配位原子的特性使得该类化合物在与金属离子配位时存在多种配位方式,从而形成单核、同双核、异双核和多核等金属配合物[1-5].     

新型常山碱类似物的合成

鸡球虫病是由艾美球虫属(Eimeria)球虫寄生于鸡肠上皮细胞内引起的一种寄生虫病,对鸡的致病率高,危害严重.据估计,全球每年因鸡球虫病造成的经济损失可达20亿美元.目前防治本病仍然以饲料中系统地添加化学药物的方法为主[1-2].但由于对药物长期连续或不合理使用,鸡球虫产生了严重的耐药性,导致抗球虫药物使用年限缩短,防治失败或效果不佳,造成很大的经济损失,解决方法之一是不断研制新的抗鸡球虫药物[2-3].     

几个新型呋喃氨基腈衍生物的合成及抗菌活性

用5-甲基-4-乙氧羰基呋喃氨基腈与芳醛反应制得Schiff碱,再采用NaBH4还原Schiff碱,得到3个新型5-甲基-4-乙氧羰基呋喃氨基腈衍生物.利用核磁共振谱(1H NMR)、红外光谱(IR),质谱(EI-MS)表征了产物的结构;并初步测定了产物的抗菌活性.结果表明,目标化合物的抗菌活性一般.