- Facile synthesis and in vitro properties of 1-alkyl- and 1-alkyl-N-propargyl-1,2,3,4-tetrahydroisoquinoline derivatives on PC12 cells
[作者:Kitabatake, M; Nagai, J; Abe, K; Tsuchiya, Y; Ogawa, K; Yokoyama, T; Mom, K; Taguchi, K; Horiguchi, Y,期刊:European Journal of Medicinal Chemistry, 页码:4034-4043 , 文章类型: Article,,卷期:2009年44-10]
- The synthesis of several 1-alkyl-1,2,3,4-tetrahydroisoquinolines, which may play an important role in Parkinson's disease, has been achieved by modified Pictet-Spengler cyclization of the formyliminium ion. The direct cy...
- Predicting the activity of drugs for a group of imidazopyridine anticoccidial compounds
[作者:Si, HZ; Lian, N; Yuan, SP; Fu, AP; Duan, YB; Zhang, KJ; Yao, XJ,期刊:European Journal of Medicinal Chemistry, 页码:4044-4050 , 文章类型: Article,,卷期:2009年44-10]
- Gene expression programming (GEP) is a novel machine learning technique. The GEP is used to build nonlinear quantitative structure-activity relationship model for the prediction of the IC50 for the imidazopyridine antico...
- Active site directed docking studies: Synthesis and pharmacological evaluation of cis-2,6-dimethyl piperidine sulfonamides as inhibitors of acetylcholinesterase
[作者:Girisha, HR; Chandra, JNNS; Boppana, S; Malviya, M; Sadashiva, CT; Rangappa, KS,期刊:European Journal of Medicinal Chemistry, 页码:4057-4062 , 文章类型: Article,,卷期:2009年44-10]
- Hypocholinergic function associated with Alzheimer's disease (AD) is well-accepted hypothesis, in this regard, many research attempts have been made to elevate the reduced cholinergic neurotransmission, among them two ma...
- Synthesis and in vitro antibacterial activity of 7-(4-alkoxyimino-3-amino-3-methylpiperidin-1-yl)fluoroquinolone derivatives
[作者:Chai, Y; Wan, ZL; Wang, B; Guo, HY; Liu, ML,期刊:European Journal of Medicinal Chemistry, 页码:4063-4069 , 文章类型: Article,,卷期:2009年44-10]
A series of novel 7-(4-alkoxyimino-3-amino-3-methylpiperidin-1-yl)fluoroquinolone derivatives were designed, synthesized and characterized by H-1 NMR, MS and HRMS. These fluoroquinolones were evaluated for in vitro an...
- Fluorescence spectroscopic investigation of the interaction between chloramphenicol and lysozyme
[作者:Ding, F; Zhao, GY; Huang, JL; Sun, Y; Zhang, L,期刊:European Journal of Medicinal Chemistry, 页码:4083-4089 , 文章类型: Article,,卷期:2009年44-10]
- The interactions between chloramphenicol and lysozyme were studied using fluorescence, UV/vis and circular dichroism spectra. The results proved the mechanism of fluorescence quenching of lysozyme by chloramphenicol is d...
- QSAR study of Akt/protein kinase B (PKB) inhibitors using support vector machine
[作者:Dong, XW; Jiang, CY; Hu, HY; Yan, JY; Chen, J; Hu, YZ,期刊:European Journal of Medicinal Chemistry, 页码:4090-4097 , 文章类型: Article,,卷期:2009年44-10]
- A three-class support vector classification (SVC) model with high prediction accuracy for the training, test and overall data sets (95.2%, 88.6% and 93.1%, respectively) was developed based on the molecular descriptors o...
- Diamine-based human histamine H-3 receptor antagonists: (4-Aminobutyn-1-yl)benzylamines
[作者:Dvorak, CA; Apodaca, R; Xiao, W; Jablonowski, JA; Bonaventure, P; Dugovic, C; Shelton, J; Lord, B; Miller, K; Dvorak, LK; Lovenberg, TW; Carruthers, NI,期刊:European Journal of Medicinal Chemistry, 页码:4098-4106 , 文章类型: Article,,卷期:2009年44-10]
- A series of (4-aminobutyn-1-yl)benzylamines were prepared and the SAR around three key areas: (1) the amine attached to the butynyl linker ((RRN-)-R-3-N-4); (2) the benzylamine moiety ((RRN-)-R-1-N-2); and (3) the point ...
- Synthesis and antitubercular activity of palladium and platinum complexes with fluoroquinolones
[作者:Vieira, LMM; de Almeida, MV; Lourenco, MCS; Bezerra, FAFM; Fontes, APS,期刊:European Journal of Medicinal Chemistry, 页码:4107-4111 , 文章类型: Article,,卷期:2009年44-10]
- The fluoroquinolones are an important family of synthetic antimicrobial agents being clinically used over the past thirty years. In addition, some fluoroquinolones have been used in the development of anticancer drugs, a...
- An efficient steroid pharmacophore-based strategy to identify new aromatase inhibitors
[作者:Neves, MAC; Dinis, TCP; Colombo, G; Melo, MLSE,期刊:European Journal of Medicinal Chemistry, 页码:4121-4127 , 文章类型: Article,,卷期:2009年44-10]
- Aromatase, an enzyme involved in the conversion of androgens into estrogens, is an important target for the endocrine treatment of breast cancer. Aromatase inhibition is usually achieved with steroids structurally relate...
- Quantitative structure activity relationship (QSAR) of piperine analogs for bacterial NorA efflux pump inhibitors
[作者:Nargotra, A; Sharma, S; Koul, JL; Sangwan, PL; Khan, IA; Kumar, A; Taneja, SC; Koul, S,期刊:European Journal of Medicinal Chemistry, 页码:4128-4135 , 文章类型: Article,,卷期:2009年44-10]
- Quantitative structure activity relationship (QSAR) analysis of piperine analogs as inhibitors of efflux pump NorA from Staphylococcus aureus has been performed in order to obtain a highly accurate model enabling predict...
- Novel 3,3 '-diindolylmethane derivatives: Synthesis and cytotoxicity, structural characterization in solid state
[作者:Maciejewska, D; Rasztawicka, M; Wolska, I; Anuszewska, E; Gruber, B,期刊:European Journal of Medicinal Chemistry, 页码:4136-4147 , 文章类型: Article,,卷期:2009年44-10]
- A series of 3,3'-dindolylmethane derivatives have been synthesized and their structures were characterized in solid state by C-13 CP/MAS NMR and two of them by X-ray diffraction measurements. They exhibited well expresse...
- Synthesis, characterization and in vitro antimicrobial activity of novel 2-thioxo-4-thiazolidinones and 4,4 '-bis (2-thioxo-4-thiazolidinone-3-yl)diphenylsulfones
[作者:El-Gaby, MSA; Ali, GAMEH; El-Maghraby, AA; El-Rahman, MTA; Helal, MHM,期刊:European Journal of Medicinal Chemistry, 页码:4148-4152 , 文章类型: Article,,卷期:2009年44-10]
- 2-Thioxo-4-thiazolidinones (3a,b) were achieved by cyclocondensation of isothiocyanatosulfonamides (1a,b) with sulfanylacetic acid at reflux temperature in dioxane in the presence of triethylamine. Compound (3a) was expl...
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