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Facile and efficient synthesis of quinoline-4-carboxylic acids under microwave irradiation 被引量:9
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作者 Zhu, Hui Yang, Ri Fang +1 位作者 Yun, Liu Hong Li, Jin 《Chinese Chemical Letters》 SCIE CAS CSCD 2010年第1期35-38,共4页
A facile and efficient method for the preparation of 2-non-substituted quinoline-4-carboxylic acids is described via the Pfitzinger reaction of isatins with sodium pyruvate following consequent decarboxylation under m... A facile and efficient method for the preparation of 2-non-substituted quinoline-4-carboxylic acids is described via the Pfitzinger reaction of isatins with sodium pyruvate following consequent decarboxylation under microwave irradiation. 展开更多
关键词 Quinoline-4-carboxylic acids Pfitzinger reaction Microwave irradiation
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QSAR and Pharmacophore Studies of Thiazolidine-4-carboxylic Acid Derivatives as Novel Influenza Neuraminidase Inhibitors Using HQSAR, Topomer CoMFA and CoMSIA 被引量:8
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作者 孙家英 王建超 梅虎 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2013年第5期744-750,共7页
In order to understand the chemical-biological interactions governing their activities toward neuraminidase (NA), QSAR models of 28 thiazolidine-4-carboxylic acid derivatives with inhibitory influenza A virus were d... In order to understand the chemical-biological interactions governing their activities toward neuraminidase (NA), QSAR models of 28 thiazolidine-4-carboxylic acid derivatives with inhibitory influenza A virus were developed. The obtained HQSAR (hologram quantitative structure activity relationship), Topomer CoMFA and CoMSIA (comparative molecular similarity indices analysis) models were robust and had good exterior predictive capabilities. Moreover, QSAR modeling results elucidated that hydrogen bonds highly contributed to the inhibitory activity, then electrostatic and hydrophobic factors. Squared multiple correlation coefficients (R2) of HQSAR, Topomer CoMFA and CoMSIA models were 0.994, 0.978 and 0.996, respectively. Squared cross-validated correlation coefficients (Q2) of HQSAR, Topomer CoMFA and CoMSIA models were in turn 0.951, 919 and 0.820. Furthermore, squared multiple correlation coefficients for the test set (R2test) of HQSAR, CoMFA and CoMSIA models were 0.879, 0.912 and 0.953, respectively. Squared cross-validated correlation coefficients for the test set (Q2ext) of HQSAR, Topomer CoMFA and CoMSIA models were 0.867, 0.884 and 0.899, correspondingly. 展开更多
关键词 QSAR thiazolidine-4-carboxylic acid derivatives HQSAR Topomer CoMFA COMSIA
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LC-MS/MS analysis of 2-aminothiazoline-4-carboxylic acid as a forensic biomarker for cyanide poisoning 被引量:2
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作者 Jorn CC Yu Sarah Martin +3 位作者 Jessica Nasr Katelyn Stafford David Thompson Ilona Petrikovics 《World Journal of Methodology》 2012年第5期33-41,共9页
AIM: To demonstrate the potential of using 2-aminothiazoline-4-carboxylic acid(ATCA) as a novel biomarker/forensic biomarker for cyanide poisoning. METHODS: A sensitive method was developed and employed for the identi... AIM: To demonstrate the potential of using 2-aminothiazoline-4-carboxylic acid(ATCA) as a novel biomarker/forensic biomarker for cyanide poisoning. METHODS: A sensitive method was developed and employed for the identification and quantification of ATCA in biological samples, where the sample extraction and clean up were achieved by solid phase extraction(SPE). After optimization of SPE procedures, ATCA was analyzed by high performance liquid chromatographytandem mass spectrometry. ATCA levels following the administration of different doses of potassium cyanide(KCN) to mice were measured and compared to endogenous ATCA levels in order to study the significance of using ATCA as a biomarker for cyanide poisoning.RESULTS: A custom made analytical method was established for a new(mice) model when animals were exposed to increasing KCN doses. The application of this method provided important new information on ATCA as a potential cyanide biomarker. ATCA concentration in mice plasma samples were increased from 189 ± 28 ng/mL(n = 3) to 413 ± 66 ng/mL(n = 3) following a 10 mg/kg body weight dose of KCN introduced subcutaneously. The sensitivity of this analytical method proved to be a tool for measuring endogenous level of ATCA in mice organs as follows: 1.2 ± 0.1 μg/g for kidney samples, 1.6 ± 0.1 μg/g for brain samples, 1.8 ± 0.2 μg/g for lung samples, 2.9 ± 0.1 μg/g for heart samples, and 3.6 ± 0.9 μg/g for liver samples. CONCLUSION: This finding suggests that ATCA has the potential to serve as a plasma biomarker / forensic biomarker for cyanide poisoning. 展开更多
关键词 Forensic science BIOMARKER Cyanide poisoning 2-aminothiazoline-4-carboxylic acid LC-MS/MS
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Highly Efficient Synthesis of Novel Fluorine Bearing Quinoline-4-carboxylic Acid and the Related Compounds as Amylolytic Agents 被引量:1
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作者 Mohammed S. T. Makki Dina A. Bakhotmah Reda M. Abdel-Rahman 《International Journal of Organic Chemistry》 2012年第1期49-55,共7页
Highly efficient syntheses of novel fluorine bearing quinoline-4-carboxylic acids and the related compounds had been achieved from cyclocondensation of 2-amino-5-fluorophenyl glyoxylic acid 1 with benzoyle asetanilide... Highly efficient syntheses of novel fluorine bearing quinoline-4-carboxylic acids and the related compounds had been achieved from cyclocondensation of 2-amino-5-fluorophenyl glyoxylic acid 1 with benzoyle asetanilides 2 in boiling DMF, to give the target 3. Decarboxylation of 3 produced 6-fluoro-2-phenyl-3-(substituted amino)-keto-quinolines 4, while that reaction underwent refluxing, afforded 7-fluoro-1-(aryl)-3-phenyl-pyrrolo[3,4-c] quinoline-2,9-diones 5. Structure of the products has been established from their elemental and spectral analysis. All targets exhibited a high to moderate activity against some Aspergillus fungi as amylolytic agents. 展开更多
关键词 Amylolytic Activity Amylolytic AGENTS ASPERGILLUS fungi Efficient Synthesis Fluoroquinoline Quinoline-4-carboxylic acidS
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Synthesis of (2S,4S)-2-Substituted-3- (3-Sulfanylpropanoyl)-6- Oxohexahydropyrimidine-4-Carboxylic Acids as Potential Antihypertensive Drugs
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作者 Andrei Ershov Dmitry Nasledov +1 位作者 Igor Lagoda Valery Shamanin 《Journal of Materials Science and Chemical Engineering》 2015年第6期7-12,共6页
Proceeding from natural amino acid L-asparagine and commercially available aldehydes a stereoselective synthesis was developed of (2S,4S)-2-alkyl(aryl)-3-(3-sulfanylpropanoyl)-6-oxohexahy- dropyrimidine-4-carboxylic a... Proceeding from natural amino acid L-asparagine and commercially available aldehydes a stereoselective synthesis was developed of (2S,4S)-2-alkyl(aryl)-3-(3-sulfanylpropanoyl)-6-oxohexahy- dropyrimidine-4-carboxylic acids, potential antihypertensive drugs, inhibitors of the angiotensin converting enzyme. 展开更多
关键词 Synthesis of (2S 4S)-2-Substituted-3- (3-Sulfanylpropanoyl)-6- Oxohexahydropyrimidine-4-carboxylic acidS AS POTENTIAL ANTIHYPERTENSIVE DRUGS
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Esterification and Chemoselective Synthesis of R-Tetrahydrothiazo-2-thione-4-carboxylic Esters Catalyzed by TiCl_4
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作者 SHANG Yan-mei LI Jing +2 位作者 SONG Zhi-guang LI Ye-zhi HUANG Hua-min 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2007年第4期430-432,共3页
A series of esters of R-tetrahydrothiazo-2-thione-4-carboxylic acid [ R-TTCA ] was synthesized by direct esterifica- tion of R-TTCA with alcohols(CH3OH, C2H5OH, n-C3HTOH, i-C3HTOH, n-C4H9OH, sec-C4H9OH) in the prese... A series of esters of R-tetrahydrothiazo-2-thione-4-carboxylic acid [ R-TTCA ] was synthesized by direct esterifica- tion of R-TTCA with alcohols(CH3OH, C2H5OH, n-C3HTOH, i-C3HTOH, n-C4H9OH, sec-C4H9OH) in the presence of TiCl4 as the catalyst at room temperature without using any other solvent or dehydrant in high yields, 91.6%-99.1% for primary alcohols and 55%- 80% for secondary alcohols. The catalyst has a strong chemoselec-tive activity for the esterification of primary alcohols with R-TTCA in the presence of secondary alcohols. Owing to high yield, high chemoselectivity, and mild conditions used, this is an efficient method for the esterification of prima-ry alcohols with R-TTCA. 展开更多
关键词 R-Tetrahydrothiazo-2-thione-4-carboxylic acid TICl4 CHEMOSELECTIVITY ESTERIFICATION
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Structure and Luminescent Property of a Novel 4-Hydroxyquinoline-2-carboxylate Based Zn(Ⅱ) Complex 被引量:4
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作者 盖艳丽 杨明 +3 位作者 冯蕊 陈莲 江飞龙 洪茂椿 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2012年第2期179-184,共6页
A 3D coordination polymer [Zn2(hqc)2(H2O)]n has been obtained from the reaction of 4-hydroxyquinoline-2-carboxylic acid (H2hqc) with zinc(II) salt under hydrothermal condition, and characterized by elemental a... A 3D coordination polymer [Zn2(hqc)2(H2O)]n has been obtained from the reaction of 4-hydroxyquinoline-2-carboxylic acid (H2hqc) with zinc(II) salt under hydrothermal condition, and characterized by elemental analysis, IR, TGA, PXRD and X-ray single-crystal diffraction. The complex crystallizes in the monoclinic system, space group P21/c with a = 14.305(2), b = 9.132(2), c = 15.356(2), β = 103.586(7)o, V = 1949.9(4)3, Z = 4, Dc = 1.782 g/cm3, μ = 2.508 mm-1, Mr = 523.06, F(000) = 1048, T = 293(2) K, λ(MoKα) = 0.71073, S = 1.008, the final R = 0.0329 and wR = 0.0745 for 3849 observed reflections (I 〉 2σ(I)). The title complex features a 3D framework via Zn(2) linking the 1D {Zn1(hqc)2}n chains. Thermogravimetric analysis shows that its framework is highly thermally stable up to 556 ℃ in the solid state. 展开更多
关键词 ZINC 4-hydroxyquinoline-2-carboxylic acid 3Dframework luminescence properties
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Synthesis, Structure and Electrochemical Property of a New 3D Ag(I) Coordination Polymer Constructed by Biphenyl-2,2ˊ,4,4ˊ-tetracarboxylate
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作者 王记江 唐龙 +3 位作者 侯向阳 高楼军 付峰 张美丽 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2014年第5期729-734,共6页
A new 3D Ag(I) coordination polymer, [Ag8(btc)2(bpp)2]n(1, H4btc = biphenyl- 2,2ˊ,4,4ˊ-tetracarboxylic acid, bpp = 1,2-bis(4-pyridyl)propane), has been hydrothermally synthesi- zed and characterized by sin... A new 3D Ag(I) coordination polymer, [Ag8(btc)2(bpp)2]n(1, H4btc = biphenyl- 2,2ˊ,4,4ˊ-tetracarboxylic acid, bpp = 1,2-bis(4-pyridyl)propane), has been hydrothermally synthesi- zed and characterized by single-crystal X-ray diffraction analysis, elemental analysis and IR spectroscopy. Complex 1 crystallizes in the triclinic system, space group P1 with a = 13.4899(8), b = 13.4928(8), c = 16.4575(10) , α = 102.7640(10), β = 108.8100(10), γ = 101.4940(10)°, V = 2644.1(3) 3, Z = 2, Dc = 2.401 Mg·m-3, μ = 2.978 mm-1, F(000) = 1840, the final R = 0.0481 and wR = 0.0955 for 6794 observed reflections with I 〉 2σ(I). Complex 1 features a 3D framework formed by Ag(I)-carboxylate chains containing [Ag16(COO)16] secondary building block. Furthermore, thermal stability and electrochemical property of 1 are also investigated in detail. 展开更多
关键词 biphenyl-2 4 4ˊ-tetracarboxylic acid Ag(I) electrochemical property
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Design, Synthesis, Antifungal Activities and SARs of (R)-2-Aryl-4,5-dihydrothiazole-4-carboxylic Acid Derivatives 被引量:2
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作者 Jingbo Liu Yuxin Li Youwei Chen Xuewen Hua Yingying Wan Wei Wei Haibin Song Shujing Yu Xiao Zhang Zhengming Li 《Chinese Journal of Chemistry》 SCIE CAS CSCD 2015年第11期1269-1275,共7页
Based on the structure of natural product 2-aryl-4,5-dihydrothiazole-4-carboxylic acid, a series of novel (R)-2-aryl-4,5-dihydrothiazole-4-carboxylic acid derivatives were designed and synthesized. Their structures ... Based on the structure of natural product 2-aryl-4,5-dihydrothiazole-4-carboxylic acid, a series of novel (R)-2-aryl-4,5-dihydrothiazole-4-carboxylic acid derivatives were designed and synthesized. Their structures were characterized by ^1H NMR, ^13C NMR and HRMS. The single crystal structure of compound 9b was determined by X-ray diffraction analysis. The antifungal activities were evaluated for the first time. The bioassay results indicated that most compounds exhibited moderate to good antifungal activities. The antifungal activities of compound 13a (against Cercospora arachidicola Hori), 13d (against Alternaria solani), and 16e (against Cercospora arachidieola Hori) were 61.9%, 67.3% and 61.9%, respectively, which are higher than those of the commercial fungicides chlorothalonil and carbendazim. Moreover, compound 13d exhibited excellent antifungal activities against 7 kinds of the fungi tested (66.7%, 77.3%, 63.0%, 87.9%, 70.0%, 70.0% and 80.0% at 50 μg/mL). Therefore, 13d can be used as a new lead structure for the development of antifungal agents. 展开更多
关键词 (R)-2-aryl-4 5-dihydrothiazole-4-carboxylic acid SYNTHESIS antifungal activity structure-activity relationship
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Application of L-thiazolidine-4-carboxylic acid monolayer in electrochemical determination of copper(Ⅱ) 被引量:1
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作者 CUI Xin1,FU YingZi1,2,LI MiaoSi1,CHEN Min2,HE Xuan1,LIU XiaoHua1 & FENG XiaoMing1 1Key Laboratory of Green Chemistry & Technology,Ministry of Education College of Chemistry,Sichuan University,Chengdu 610064,China +1 位作者 2Key Laboratory of Luminescence and Real-Time Analysis,Ministry of Education College of Chemistry and Chemical Engineering,Southwest University,Chongqing 400715,China 《Science China Chemistry》 SCIE EI CAS 2010年第1期257-262,共6页
L-Thiazolidine-4-carboxylic acid monolayer was prepared on gold electrodes through the self-assembly approach.Such novel thioether-based monolayer could efficiently preconcentrate Cu2+,which provided a simple,stable a... L-Thiazolidine-4-carboxylic acid monolayer was prepared on gold electrodes through the self-assembly approach.Such novel thioether-based monolayer could efficiently preconcentrate Cu2+,which provided a simple,stable and reproducible method for the determination of Cu2+.The modified electrodes were stable enough to be continuously used for one week(more than 30 times regeneration) with lower than 10% decrease in the response.They retained their initial activity for more than one month if used once a day.The calibration curve was linear for Cu2+ from 0.6 to 158.8 μg L?1 with a detection limit of 0.38 μg L?1.The relative standard deviation was 3.2% for a series of six successive measurements.The proposed method was applied in the determination of Cu2+ in mineral water and human hair samples. 展开更多
关键词 L-thiazolidine-4-carboxylic acid COPPER IONS gold electrode THIOETHER MONOLAYER
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QSAR and Docking Studies of Thiazolidine-4-carboxylic Acid Derivatives as Neuraminidase Inhibitors 被引量:1
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作者 TONG Jian-Bo WANG Tian-Hao +1 位作者 WU Ying-Ji FENG Yi 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2020年第4期651-661,共11页
In order to understand the chemical-biological interactions governing their activities toward neuraminidase(NA),QSAR models of 28 thiazolidine-4-carboxylic acid derivatives with inhibitory influenza A virus were devel... In order to understand the chemical-biological interactions governing their activities toward neuraminidase(NA),QSAR models of 28 thiazolidine-4-carboxylic acid derivatives with inhibitory influenza A virus were developed.Here a quantitative structure activity relationship(QSAR)model was built by three-dimensional holographic atomic vector field(3D-HoVAIF)and multiple linear regression(MLR).The estimation stability and prediction ability of the model were strictly analyzed by both internal and external validations.The correlation coefficient(R2)of established MLR model was 0.984,and the cross-validated correlation coefficient(Q2)of MLR model was 0.947.Furthermore,the cross-validated correlation coefficient for the test set(Qext 2)was 0.967.The binding mode pattern of the compounds to the binding site of integrase enzyme was confirmed by docking studies.The results of present study indicated that this model can aid in designing more potent neuraminidase inhibitors. 展开更多
关键词 3D-QSAR thiazolidine-4-carboxylic acid derivatives 3D-HoVAIF molecular designing molecular docking
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Resolution of racemic R.S-α-arylethylamine by a new resolving agent (R)thiazolidine-2-thione-4-carboxylic acid 被引量:1
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作者 李叶芝 郭纯孝 +1 位作者 卜卫明 黄化民 《Science China Chemistry》 SCIE EI CAS 1998年第4期361-370,共10页
Racemic R.S-α-arylethylamine was resolved by R (-) thiazolidine-2-thione-4-carboxylic acid, a new resolving agent abbreviated as [R (-) TTCA], by which R (-) TTCA.S(-) arylethylamine salts2a-2e, [α] D 20 =-47.24... Racemic R.S-α-arylethylamine was resolved by R (-) thiazolidine-2-thione-4-carboxylic acid, a new resolving agent abbreviated as [R (-) TTCA], by which R (-) TTCA.S(-) arylethylamine salts2a-2e, [α] D 20 =-47.24° — 64.40° and optically active R(+)-a-arylethylamines3a – 3e, 74. 54%-94. 45% e, e., were obtained. Optically active S (-) -α-arylethylamines4a-4e, 72.84%-90.36% e.e., were obtained by the decomposition of2a-2e in basic solutions. The influence of substitutive group of the benzene ring on the basicity of the amino group was studied by semiempirical PM3 method. The structures of the R (-) TTCA.S (-) -α-phenylethylamine salt (2a(R-S) configuration) and R (-) TTCA-R(+)-a-phenylethylamine salt (2a(R-R) configuration) have been established by means of X-ray diffraction. They crystallize in a monoclinic system. Space group isP21. The cell constants of2a(R-S) configuration were obtained as follows: α = 1.387 8(2), b = 0.664 05(101,c = 1.580 O(2) nm; β = 90.844(10)° Z = 4; those obtained for2a(R-R) configuration were α = 1.080 6(2),b = 0.584 80(12),c = 1.2188(2) nm, β= 110.38(3)dg, V = 0.7220nm3,Z = 2. There are intermolecular hydrogen bonds in the crystals of the two kinds of configurations of the amine salt. The hydrogen bond number in the unit cell of R (-) TTCA.S (-)-α-phenylethylamine salt is twice as much as that of R (-) TTCA.R(+)-a-phenylethylamine salt. 展开更多
关键词 new resolving agent R(-) thiazolidine-2-thione-4-carboxylic acid R(+)-a-arylethylamine S(-)-α-arylethylamlne resolution electronic structure crystal structure intermolecular hydrogen bond
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Drug discovery based on the structure of FKBP12: Design, synthesis and evaluation of L-1,4-thiazane-3-carboxylic acid derivatives as neuroimmunophilin ligands
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作者 NIE AiHua XIAO JunHai +4 位作者 WANG LiLi LIAO GuoChao LIU HongYing REN Shen LI Song 《Science China Chemistry》 SCIE EI CAS 2007年第3期405-417,共13页
By choosing neuroimmunophilin FKBP12 as a therapeutical target, we have attempted to discover a new structural drug for treating neurodegenerative disease. This drug should possess neurotrophic activity and not affect... By choosing neuroimmunophilin FKBP12 as a therapeutical target, we have attempted to discover a new structural drug for treating neurodegenerative disease. This drug should possess neurotrophic activity and not affect the immune system. Based on the crystal structure of FKBP12, FK506 and Calcineurin complex, a series of small organic molecules were designed. These molecules were to have the ability of binding to FKBP12 in a virtual screening. By using a solution parallel synthetic method, these compounds were synthesized. The neuroprotective and neuroregenerative activities of these compounds were evaluated by binding assays, PC12 cells survival and neurite outgrowth model, chick dorsal root ganglion cultures (DRG) and 6-OHDA lesioned mice sympathetic nerve endings model. The evaluation results of these compounds showed that compound N308 has great promise as a candidate for a neuroprotective and neuroregenerative agent. 展开更多
关键词 FKBP12 L-1 4-thiazane-3-carboxylic acid derivatives DESIGN SYNTHESIS NEUROTROPHIC activity
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Syntheses, Structures, and Properties of Three Coordination Polymers: [Cd_2(bpp)_(1.5)(Hbpp)(phen)_2]_n, [Mn_3(Htptc)_2(phen)_2(H_2O)_2]_n, and {[Cu(btc)_(0.5)(1,4-bib)]·2H_2O}_n
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作者 丁元帅 范黎明 +2 位作者 逄越 张修堂 田来进 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2014年第4期569-578,共10页
Hydrothermal reactions of three aromatic polycarboxylic acids and the transitional metal cations in the presence of phen and 1,4-bib afford three new coordination polymers: [Cd2(bpp)1.5(Hbpp)(phen)2]n (1), [... Hydrothermal reactions of three aromatic polycarboxylic acids and the transitional metal cations in the presence of phen and 1,4-bib afford three new coordination polymers: [Cd2(bpp)1.5(Hbpp)(phen)2]n (1), [Mn3(Htptc)2(phen)2(H2O)2]n (2), and {[Cu(btc)0.5(1,4- bib)]·2H2O}n(3) (H2bpp = 2,6-bis(4'-carboxyphenyl)-4-phenylpyridine, H4tptc = terphenyl-2,5,2',5'-tetracar- boxylic acid, H4btc =biphenyl-2,2',4,4'-tetracarboxylic acid, phen =1,10-phenanthroline, and 1,4-bib = 1,4-bis(1H-imidazol-1-yl)benzene). Their structures have been determined by single- crystal X-ray diffraction analyses, elemental analyses, IR spectra, and powder X-ray diffraction (PXRD) analyses. In compound 1, the CdII cations are linked by bpp2- to form one ladder structure, based on which a 3D network is constructed with the help of non-covalent interactions. The topology of 2 is a 3D (3,4,5)-connected framework with the Point Schl?fli symbol of (42.6)2(43.62.8)(45.64.8)2. Compound 3 shows an unprecedented 3D (4,4)-connected framework with the Point Schl?fli symbol of (64.82)2(65.8). Moreover, the luminescent property of 1 has been investigated. 展开更多
关键词 2 6-bis(4'-carboxyphenyl)-4-phenylpyridine biphenyl-2 2' 4 4'-tetracarboxylic acid terphenyl-2 5 2' 5'-tetracarboxylic acid 1 10-phenanthroline 1 4-bis(imidazol-1-yl)butane
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A Facile Synthesis of 9,10-Dimethoxybenzo[6,7]- ox-epino[3,4-<i>b</i>]quinolin-13(6<i>H</i>)-one and Its Derivatives
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作者 Dingqiao Yang Xiuli Liang +1 位作者 Xiongjun Zuo Yuhua Long 《International Journal of Organic Chemistry》 2013年第2期119-124,共6页
A concise and efficient method for the synthesis of novel 9,10-imethoxybenzo[6,7]oxepino[3,4-b]quinolin13(6H)-one and its derivatives 7a-p has been developed via the intramolecular Friedel-Crafts acylation reactions o... A concise and efficient method for the synthesis of novel 9,10-imethoxybenzo[6,7]oxepino[3,4-b]quinolin13(6H)-one and its derivatives 7a-p has been developed via the intramolecular Friedel-Crafts acylation reactions of 6,7-dimethoxy-2-(phenoxymethyl)quinoline-3-carboxylic acids 6a-p with polyphosphoric acid (PPA) as catalyst and solvent under mild conditions. The key intermediates 6a-p were prepared through the in situ formation of ethyl 6,7-dimethoxy-2-(phenoxymethyl)quinoline-3-carboxylates 5a-p followed by hydrolysis with aqueous ethanolic sodium hydroxide solution. The novel synthetic method has the advantages of good yields, easy work-up, and environmentally friendly character, which may provide a novel highly efficient process for making quinoline and related azaheterocycle libraries. 展开更多
关键词 The Intramolecular Friedel-Crafts Acylation Reaction: 9 10-Dimethoxybenzo [6 7]oxepino[3 4-b]quinolin-13(6H)-one and Its DERIVATIVES 6 7-Dimethoxy-2-(phenoxymethyl)quinoline-3-carboxylic acid: Ethyl 7-dimethoxy-2-(phenoxymethyl)quinoline-3-carboxylate: PPA
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Indole Alkaloids from the Roots of Ervatamia hainanensis 被引量:4
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作者 Jian Peng HUANG Zi Ming FENG +2 位作者 Chong Fei ZHENG Pei Cheng ZHANG Yang Min MA 《Chinese Chemical Letters》 SCIE CAS CSCD 2006年第6期779-782,共4页
Two new indole alkaloids, named ibogamine-18-carboxylic acid, 3, 4-didehydro-7, 8-dioxo-methyl ester 1, ibogamine-18-carboxylic acid, 16, 17-didehydro-9, 17-dihydro-9-hydroxy (2-oxopropyl)-methyl ester 2, were isola... Two new indole alkaloids, named ibogamine-18-carboxylic acid, 3, 4-didehydro-7, 8-dioxo-methyl ester 1, ibogamine-18-carboxylic acid, 16, 17-didehydro-9, 17-dihydro-9-hydroxy (2-oxopropyl)-methyl ester 2, were isolated from Ervatamia hainanensis. Their structures were elucidated on the basis of spectroscopic methods. 展开更多
关键词 Ervatamia hainanensis indole alkaloid ibogamine-18-carboxylic acid 3 4-didehydro-7 8-dioxo-methyl ester ibogamine- 18-carboxylic acid 16 17-didehydro-9 17-dihydro-9-hydroxy-(2-oxopropyl)-methyl ester.
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Synthesis,Structure,and Magnetic Property of One Snake-shaped Copper(Ⅱ)-organic Compound:Cu[Cu_2(PP)_2](CBPC)_2]·2(H_2O) 被引量:3
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作者 范黎明 李大成 +2 位作者 魏培海 张修堂 窦建民 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2011年第10期1381-1386,共6页
One novel copper(II)-organic compound,namely Cu[Cu2(PP)2](CBPC)2]·2(H2O)(1,H2CBPC = 1-[(2'-carboxybiphenyl-4-yl)methyl]-2-propylimidazole-4-carboxylic acid,HPP = 3-(2-pyridyl)pyrazole),was designed... One novel copper(II)-organic compound,namely Cu[Cu2(PP)2](CBPC)2]·2(H2O)(1,H2CBPC = 1-[(2'-carboxybiphenyl-4-yl)methyl]-2-propylimidazole-4-carboxylic acid,HPP = 3-(2-pyridyl)pyrazole),was designed and synthesized under hydrothermal conditions.X-ray diffraction analysis reveals that two Cu(II)ions in the quasi-planar dimmer of [Cu2(PP)2] are linked by the carboxylate oxygen atoms on the phenyl ring and the imidazole ring,respectively,yielding one snake-shaped structure.Magnetic measurements reveal that compound 1 shows the strongly antiferromagnetic property.Crystal data of 1:C58H52Cu3N10O10,Mr = 1239.72,monoclinic,P21/c,a = 14.900(7),b = 15.029(7),c = 12.308(6),β = 102.519(9)o,V = 2691(2)3,Z = 2,Dc = 1.530 g/cm3,F(000)= 1274,μ = 1.246 mm-1,R = 0.0416,wR = 0.0780(I 2σ(I))and S = 0.999. 展开更多
关键词 1-[(2'-carboxybiphenyl-4-yl)methyl]-2-propylimidazole-4-carboxylic acid 3-(2-pyridyl)pyrazole) copper(II) magnetism TGA XPS
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Hydrothermal Synthesis and Crystal Structure of One Novel 1-D Copper(Ⅱ)-organic Framework:{[Cu_2(PP)_2(CBPC)]_2·7H_2O}_n 被引量:2
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作者 魏培海 吴小园 +5 位作者 范黎明 李大成 张修堂 窦建民 刘新征 石聪文 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2010年第12期1774-1779,共6页
One novel 1-D copper(Ⅱ)-organic compound,namely {[Cu2(PP)2(CBPC)]2·7H2O}n(1,H2CBPC=1-[(2'-carboxybiphenyl-4-yl)methyl]-2-propylimidazole-4-carboxylic acid,HPP=3-(2-pyridyl)pyrazole),was synthesized ... One novel 1-D copper(Ⅱ)-organic compound,namely {[Cu2(PP)2(CBPC)]2·7H2O}n(1,H2CBPC=1-[(2'-carboxybiphenyl-4-yl)methyl]-2-propylimidazole-4-carboxylic acid,HPP=3-(2-pyridyl)pyrazole),was synthesized under hydrothermal conditions.X-ray diffraction analyses reveal that the two Cu(Ⅱ) ions in the distorted dimer [Cu2(PP)2] of 1 are linked by the carboxylate oxygen atoms on the phenyl and imidazole rings,respectively,forming one interesting snake-like chain.Single-crystal X-ray analyses reveal that it crystallizes in monoclinic,space group C2/c with a=30.656(8),b=12.715(3),c=22.405(5),β=122.758(3)°,V=7344(3)3,Z=4,Mr=1681.65,Dc=1.521 g/cm3,F(000)=3464,μ=1.221 mm-1,the final R=0.0453 and wR=0.1023 for 4617 observed reflections with Ⅰ 〉2σ(Ⅰ). 展开更多
关键词 1-[(2'-carboxybiphenyl-4-yl)methyl]-2-propylimidazole-4-carboxylic acid 3-(2-pyridyl)pyrazole) copper(Ⅱ) TGA XPS crystal structures
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Synthesis of two new thiazolidines and their hepatoprotective effects 被引量:1
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作者 杨艳 Liu Wanshun +2 位作者 Han Baoqin Fu Chenwei Sun Haizhou 《High Technology Letters》 EI CAS 2005年第4期437-442,共6页
Two new 2-substituted thiazolidine-4(R)-carboxylic acids (TCAs), 2-glusosaminal-TCA (GIcNH2Cys) and 2-N-acetyl-glueosanlinal-TCA (GlcNAeCys), were synthesized. Their protective effects against liver toxicity i... Two new 2-substituted thiazolidine-4(R)-carboxylic acids (TCAs), 2-glusosaminal-TCA (GIcNH2Cys) and 2-N-acetyl-glueosanlinal-TCA (GlcNAeCys), were synthesized. Their protective effects against liver toxicity induced by acetaminophen (APAP) were investigated in a mice model. The resuits demonstrate that administration of TCAs ( i. p. , 800 mg/kg) 30 min after APAP challenge efficiently decrease ALF, AST, and LDH levels in liver. GlcNAcCys shows the best proteetive eftects, decreasing ALT, AST and LDH levels to 63%, 18.4% and 37% of the APAP group respectively. Comparison with the control showed that APAP greatly decreases total sulfhydlyl (T-SH) levels (43%), non-protein hound sulfhydryl (NP-SH) levels (50%) and total antioxidative capabilities (57%) in the liver 24 hr after challenge. TCAs treatments 30min after APAP challenge significantly elevate sulfhydryl levels and total antioxidative capabilities. APAP administration also markedly (P 〈 0.05) increases liver lipid peroxidation to 1.65 and 1.17 times that of the control 4 hr and 24 hr after APAP administration respectively. TCAs treatments can inhibit lipid peroxidation as measured by decreased malondialdehyde (MDA) contents in liver. The histopathological results also further confirm the hepatoprotective effects of TCAs. In conclusion, our data show that TCAs, GleNAcCys particularly, have hepatoprotective anti antioxidant etfects. 展开更多
关键词 thiazolidine-4(R)-carboxylic acids ACETAMINOPHEN lipid peroxidation total antioxidative capability
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Antioxidant activity of N-acetyl-glucosamine based thiazolidine derivative
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作者 李春雷 Yang Yan Han Baoqin Liu Wanshun 《High Technology Letters》 EI CAS 2007年第4期441-446,共6页
N-acetyl-glucosamine, the monomer of chitin, was cyclo-condensed with L-cysteine to prepare thiazolidine derivative: 2-N-acetyl-glucosamine-thiazolidine-4(R)-carboxylic acid (GlcNAcCys). The stability of GlcNAcCy... N-acetyl-glucosamine, the monomer of chitin, was cyclo-condensed with L-cysteine to prepare thiazolidine derivative: 2-N-acetyl-glucosamine-thiazolidine-4(R)-carboxylic acid (GlcNAcCys). The stability of GlcNAcCys was evaluated by high performance liquid chromatography (HPLC) measurement. The results showed that GlcNAcCys was more stable than other TCA derivatives, especially in alkaline condition. The direct in vitro antioxidative properties of GlcNAcCys were investigated by using UV radiation-induced lipid peroxidation (LPO) in mitochondria and nuclei and . OH-induced LPO in red blood cell (RBC) ghosts models. UV radiation caused dose-dependent LPO in both mitochondria and nuclei. This effect was catalyzed by addition of Fe^2 + while prevented by co-incubation with GlcNAcCys. When nuclei and mitochondria was treated with 100μl, 300μl, 500μl of GlcNAcCys and co-incubated at 37℃ for 30min, LPO was decreased to 96%, 72%, 68% in nuclei and 95%, 72%, 68% in mitochondria when compared to the UV radiation group respectively. Hydroxyl radicals (. OH) generated by Fenton reaction induced LPO in RBC ghosts. Pretreatment of RBC ghosts with GlcNAcCys could induce antioxidant RBC ghosts and inhibit concentration-dependent malondialdehyde (MDA) formation in antioxidant RBC ghosts. Its inhibition percent was 14%, 35%, 36%, 42% at 10, 20, 30, 40mg/ml respectively. In a conclusion, the data suggest that GlcNAcCys has antioxidant ability and can significantly inhibit lipid peroxidation in biological samples tested in vitro. 展开更多
关键词 thiazolidine-4(R)-carboxylic acid N-acetyl-glucosamine antioxidant lipid pemxidation
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