Synthesis and in vitro-Anti-hepatitis B Virus Activities of Several Ethyl 5-Hydroxy-1H-indole-3-carboxylates

IntroductionHepatitis B caused by a virus(HBV)is a commoninfectious disease in the world.According to WHO,700million people have been infected with HBVin theworld[1,2].HBV infection causes severe liver diseasesuch as cirrhosis and may also eventually lead…     

Synthesis and in vitro Anti-hepatitis B Virus Activity of Some Ethyl 5-Hydroxy-4-substituted Aminomethyl-2-sulfinylmethyl-1H-indole-3-carboxylates

A novel series of ethyl 5-hydroxy-4-substituted aminomethyl-2-sulfinylmethyl-1H-indole-3-carboxylates 8a―8j and 11e―11f was synthesized and evaluated in HepG2.2.15 cells for their anti-hepatitits B virus(HBV) acti-vity and cytotoxicity.Among them,six compounds showed more potent inhibitory activity than lamivudine.Compound 8e exhibited the most significant anti-HBV activity with an IC50 value of 1.62 μmol/L,which was 33-times more potent than the reference drug lamivudine(IC50=54.78 μmol/L).     

Synthesis and Anti-influenza Virus Activity of Ethyl 6-Bromo-5-hydroxyindole-3-carboxylate Derivatives

A series of ethyl 6-bromo-5-hydroxyindole-3-carboxylate derivatives were synthesized and their in vitro anti-influenza virus activity was evaluated. All the compounds were characterized by ^1H NMR and MS.     

3-羟基-1-金刚烷甲基乙烯基醚的合成

以3-羟基-1-金刚烷甲醇和乙炔为原料,庚烷为溶剂,叔丁醇钾为催化剂,氧化锌为助催化剂,于140℃/1.0 MPa反应3.0 h合成了3-羟基-1-金刚烷甲基乙烯基醚,收率85%,纯度≥99.5%,其结构经IR确证。     

生物合理设计光系统Ⅱ抑制剂研究 (Ⅶ)──2-氰基-3-甲硫基-3-芳氨基丙烯酸乙酯的合成及其Hil反应抑制活性

合成了化合物2-氰基-3-甲硫基-3-芳氨基丙烯酸乙酯(2a_2w),产物结构通过¹HNMR和元素分析证实,测定了所有化合物的Hil反应抑制活性.生物活性测定结果表明,部分化合物均表现出良好的抑制活性,初步分析了标题化合物结构与活性间的关系.     

Synthesis of 5-Deoxy-5-Acyloxyiminoavermectin B1 Derivatives

The avermectins1 are a unique collection of naturally occurring macrocyclic lactones with broad spectrum of anthelmintic and insecticidal activities. Their remarkable biological activity and complex molecular architecture stimulated significant interest in the scientific community. Much research has been carried out on these compounds. Many derivatives of avermectin have much more bioactivities and have been commercially utilized2-5. Here we describe the synthesis of 5-deoxy-5-acyloxyimi…     

Synthesis and in vitro anti-hepatitis B virus activity of 1H-benzimidazol-5-ol derivatives

<正>A series of 1H-benzimidazol-5-ol derivatives were synthesized and evaluated for their anti-hepatitis B virus(HBV) activity and cytotoxicity in HepG2.2.15 cells.Half of the tested compounds were found to be potent against HBsAg secretion with IC_(50) values less than 100μmol/L.Compounds 14c,14d,and 14e showed significant inhibitory activity to the viral antigen HBeAg.     

（3-氧代苯并异噻唑啉-2-基）羧酸烷酯的合成及抑菌活性研究

以1,2-苯并异噻唑啉-2（3H）-酮为原料,通过＂一锅法＂制备了8种（3-氧代苯并异噻唑啉-2-基）羧酸烷酯,结构经IR、1H NMR和元素分析确认。抑菌活性实验表明,化合物在浓度为2mg/L时对亚心型扁藻、球等鞭金藻和蛋白核小球藻的生长都有抑制活性,其中部分化合物（2c～2h）对球等鞭金藻和蛋白核小球藻的生长有优良...     

Synthesis and Crystal Structure of Methyl 3-（5- Bromo-1-ethyl-1H-indole-3-carbonyl）aminopropionate

Methyl 3-(5-bromo-1-ethyl-1H-indole-3-carbonyl)aminopropionate has been syn-thesized by the acylation of 5-bromo-3-trichloroacetylindole with β-alanine methyl ester,followed by alkylation with ethyl iodide,in 82.6% yield.Its crystal structure was gotten and determined by X-ray diffraction method.The crystal is of monoclinic,space group P2 1 /c with a=11.7927(8),b=14.9342(8),c=9.0060(5),β=101.558(6)°,V=1553.93(16)3,Z=4,D c=1.510 g/cm 3,λ=0.71073,μ(MoKα)=2.656 mm-1,M r=353.22 and F(000)=720.The structure was refined to R=0.0401 and wR=0.0825 for 1704 observed reflections with I > 2σ(I).In the crystal structure,intermolecular N(2)-H(2)···O(1) hydrogen bond and weak intermolecular bonds (C(1)-H(1) O(1) and C(10)-H(10B) O(2)) are formed,and π-π stacking also exists.     

Thermal-Induced Dimerization Cyclization of Ethyl N-(Styrylcarbamoyl)acetates: Formation of 4-Hydroxy-2(1H)-pyridone-3- carboxamide Derivatives

Thermal-induced dimerization cyclization of ethyl N-(styrylcarbamoyl)acetate derivatives has been investigated, leading to 4-hydroxy-2(1H)-pyridone-3-carboxamide derivatives with good yields in diphenyl ether on 200–210 °C. Ethyl N-(styrylcarbamoyl)acetate derivatives readily provided the intermolecular cyclization products 4-hydroxy-2(1H)-pyridone-3-carboxylates on reflux in xylene. In addition, several related 3-acetyl-4-hydroxy-5-phenylpyridin-2(1H)-ones have been prepared. It provided an efficient preparation of 4-hydroxy-2(1H)-pyridone-3-carboxamide derivatives.     

1,2,3—噻二唑衍生物的合成及其生物活性

自1976年Arndt等合成植物生长调节剂噻苯隆[1]似来，有关含1，2，3一噻二唑化0合物的生物活性的研究就不断有报道[2～5]．为了寻找新的具有较好生物活性的化合物，本文以5-氨基-1，2，3-噻二唑为中间体合成了5种不同取代基的磺酰脲类化合物、3种SChiff碱类化合物及吡唑类、酰亚胺类化合物各1种，共10种新化合物．其反应式如下：1实验部分MT－3型元素分析仪；Schimadzu-IR-435型红外光谱仪，KBr压片；Jeolfx－90Q型或BrukerAC－P200型核磁共振仪（CDCI。，DMSO－de，TMS）；VGZAB－HS型质谱仪；Yanaco熔点仪（温度计未经校正）…     

Synthesis and biological evaluation of ethyl 6-alkoxy-7-phenyl-4-hydroxy-3-quinolinecarboxylates against Eimeria tenella

<正>A series of ethyl 6-alkoxy-7-phenyl-4-hydroxy-3-quinolinecarboxylates were designed and synthesized.Their structures were confirmed by ~1H NMR,~(13)C NMR,IR and HRMS.The biological activities were primarily evaluated against Eimeria tenella according to Anticoccidial Index(ACI) method in vivo.The results showed that compounds 5e,5f and 5i exhibited anticoccidial activities against E.tenella at 27 mg kg~(-1).     

A solvent-free synthesis of ethyl 3,5-diaryl-1H-pyrrole-2-carboxylates via triethylphosphite mediated reductive cyclization of ethyl 2-nitro-5-oxo-3,5-diarylpentanoates under microwave irradiation

Ethyl 3,5-diaryl-1H-pyrrole-2-carboxylates have been synthesized in good yields from ethyl 2-nitro-5-oxo-3,5-diarylpentanoates by treatment with triethylphosphite under microwave irradiation. The integrity of the mechanism proposed has been augmented by ³¹P NMR and EIMS experiments.     

2-羟基-3-羧基-5-磺酸基苯重氮氨基偶氮苯与汞的显色反应及其应用

研究了2－羟基－3－羧基－5－磺酸基苯重氮氨基偶氮苯（HCSDAA）与汞（Ⅱ）的显色反应。在乳化剂OP存在下和pH10．0～10．5的缓冲介质中，汞（Ⅱ）与HCSDAA形成1：2的红色络合物，其最大吸收波长是522nm，对比度为91nm，表观摩尔吸光系数为1．63×105L·mol－1·cm－1。汞（Ⅱ）在0～0．55mg／L范围内服从比尔定律。本方法操作简便，选择性较好，直接用于头发和废水的分析，6次测定的相对标准偏差分别为2．1％和27％，平均值与双硫腙法一致，回收率分别是94．8％～101．6％和98．7％～103．0％。     

3-甲基-5-苯砜基-3E-戊烯-1-醇的立体专一性合成

3-甲基-5-苯砜基-3E-戊烯-1-醇(1)是合成某些萜类化合物的重要中间体.它具有反式烯丙基苯砜基双键.Julia等曾报道用含砜基的环丙基醇的开环重排反应来实现这类化合物的立体选择性合成,但其开环前体不易得到.本文以4-羟基-2-丁酮(2)为起始原料,经4步反应立体专一性地合成了标题化合物1.合成路线短、操作简便、易于大量制备.合成路线用方程式表示如下:     

5-苄氧亚氨基-5-脱氧阿维菌素B1a的合成

以阿维菌素B1a为原料经过选择性氧化合成5-氧代-5-脱氧阿维菌素B1a, 再与O-取代羟胺盐酸盐反应合成了5个5-苄氧亚氨基-5-脱氧阿维菌素B1a (4a～4e), 通过¹H NMR, ¹³C NMR, MS, IR确证了它们的结构. 生测结果表明它们对于棉铃虫和甜菜夜蛾有一定的杀虫活性.     

Synthesis,Characterization and Biological Activities ofN-Acyl-3-(3-pyridyl)-5-aryl-pyrazoles

Ten novel N-acyl-3-(3-pyridyl)-5-aryl-pyrazoles were synthesized by Claisen condensation of the aryl methyl ketones with ethyl nicotinate, the cyclization with hydrazine hydrate and the N-acylation with acyl chloride in turn. The structures of all the compounds synthesized were confirmed by means of Fourier transform infrared(FTIR), ¹H NMR, mass spectroscopy and elemental analysis. The biological activities of the title compounds were examined by disc diffusion method against Escherichia coli, Staphylococcus aureus, Pyricularia oryzae and Rhizoctnia solani. All the N-acyl-3-(3-pyridyl)-5-aryl-pyrazoles exhibited a certain degree of antibacterial and antifungal activities. Comparatively, compounds 3c and 3d exhibited much significant antibacterial and antifungal activities than the other pyrazole derivatives.     

Design,Synthesis and Biological Activities of Novel N-Aryl-1H-pyrazole-5-carboxylate Derivatives

In an attempt to search for potent fungicide, a series of novel N-aryl-1H-pyrazole-5-carboxylate derivatives was designed and synthesized. Their chemical structures were characterized by ¹H NMR spectra and high resolution mass spectrometry(HRMS). The preliminary bioassay results indicated that some target compounds displayed better fungicidal activities against certain fungi at 50 μg/mL or favorable antitumor activities at 5 μg/mLcompared with chlorothalonil and 5-fluorouracil, respectively. The structure-activity relationship demonstrated that the introduction of ester group and amide bond was favorable to the improvement of activities against Physalospora piricola and Phytophthora capsici.     

5-卤代-1H-1,2,4-三氮唑-3-羧酸乙酯及其衍生物的合成

以5-氨基-1H1,2,4-三氮唑-3-羧酸乙酯为原料,经Sandmeyer反应合成了5-X-1H-1,2,4-三氮唑-3-羧酸乙酯(X=C1,Br,I)(1a-1c),1a-1c再分别与α-2′,4′-二氟苯乙酮反应合成了3个5-卤代-1-1H-1,2,4-三氮唑-3-羧酸乙酯衍生物(2a-2c),其结构通过元素分析,IR,UV和^1H NMR进行了表征。