- Synthesis of lipophilic dimeric C-7/C-7-linked ciprofloxacin and C-6/C-6-linked levofloxacin derivatives. Versatile in vitro biological evaluations of monomeric and dimeric fluoroquinolone derivatives as potential antitumor, antibacterial or antimycobacterial agents
[作者:Azema, J; Guidetti, B; Korolyov, A; Kiss, R; Roques, C; Constant, P; Daffe, M; Malet-Martino, M,期刊:European Journal of Medicinal Chemistry, 页码:6025-6038 , 文章类型: Article,,卷期:2011年46-12]
- The synthesis of C-7/C-7-linked ciprofloxacin (CP) and C-6/C-6-linked levofloxacin (LV) derivatives with modulated lipophilicity is described herein. The synthesized compounds, along with the monomeric analogs described ...
- Comparative studies on interactions of baicalein, baicalin and scutellarin with lysozyme
[作者:Huang, Y; Cui, LJ; Wang, JM; Huo, K; Chen, C; Zhan, WH; Dou, YH,期刊:European Journal of Medicinal Chemistry, 页码:6039-6045 , 文章类型: Article,,卷期:2011年46-12]
- The interactions of baicalein, baicalin and scutellarin with lysozyme (LYSO) were studied by fluorescence and UV spectroscopy. The results showed that all the three flavones can quench the fluorescence of LYSO via static...
- Synthesis and in vitro anticancer activity of 6,7-methylenedioxy (or 5-hydroxy-6-methoxy)-2-(substituted selenophenyl)quinolin-4-one analogs
[作者:Chen, CT; Hsu, MH; Cheng, YY; Liu, CY; Chou, LC; Huang, LJ; Wu, TS; Yang, XM; Lee, KH; Kuo, SC,期刊:European Journal of Medicinal Chemistry, 页码:6046-6056 , 文章类型: Article,,卷期:2011年46-12]
- 6,7-Methylenedioxy (or 5-hydroxy-6-methoxy)-2-(substituted selenophenyl)quinolin-4-ones and their isosteric compounds were synthesized and evaluated for anticancer activity. Structure activity relationships (SAR) of thes...
- Synthesis and biological activity of novel N-cycloalkyl-(cycloalkylaryl)-2-[(3-R-2-oxo-2H-[1,2,4]triazino[2,3-c]quinazoline-6-yl)thio]acetamides
[作者:Berest, GG; Voskoboynik, OY; Kovalenko, SI; Antypenko, OM; Nosulenko, IS; Katsev, AM; Shandrovskaya, OS,期刊:European Journal of Medicinal Chemistry, 页码:6066-6074 , 文章类型: Article,,卷期:2011年46-12]
- In this paper the novel N-cycloalkyl-(cycloalkylaryl)-2-[(3-R-2-oxo-2H-[1,2,4]triazino[2,3-c]quinazoline-6-yl)thio]acetamides synthesis by aminolysis of activated by thionyl chloride or carbonyldiimidazole [(3-R-2-oxo-2H...
- Synthesis and kinetic testing of new inhibitors for a metallo-beta-lactamase from Klebsiella pneumonia and Pseudomonas aeruginosa
[作者:Mohamed, MS; Hussein, WM; McGeary, RP; Vella, P; Schenk, G; Abd El-hameed, RH,期刊:European Journal of Medicinal Chemistry, 页码:6075-6082 , 文章类型: Article,,卷期:2011年46-12]
- There are currently no clinically useful inhibitors against metallo-beta-lactamases (MBLs), enzymes that confer resistance against a broad spectrum of commonly used antibiotics and that are produced by an increasing numb...
- Copper(II) chloride mediated synthesis and DNA photocleavage activity of 1-aryl/heteroaryl-4-substituted-1,2,4-triazolo[4,3-a]quinoxalines
[作者:Aggarwal, R; Sumran, G; Kumar, V; Mittal, A,期刊:European Journal of Medicinal Chemistry, 页码:6083-6088 , 文章类型: Article,,卷期:2011年46-12]
- A new class of photonucleases, 1-aryl/heteroaryl-4-substituted-1,2,4-triazolo[4,3-a]quinoxalines (4) was synthesized in a facile and efficient manner via copper(II) chloride mediated oxidative intramolecular cyclization ...
- Total synthesis and bioactivity of the marine alkaloid pityriacitrin and some of its derivatives
[作者:Zhang, PY; Sun, XF; Xu, B; Bijian, K; Wan, SB; Li, GG; Alaoui-Jamali, M; Jiang, T,期刊:European Journal of Medicinal Chemistry, 页码:6089-6097 , 文章类型: Article,,卷期:2011年46-12]
- We report herein the chemical synthesis and biological evaluation of p-carboline alkaloid pityriacitrin and some of its new derivatives. Using tryptophan or 5-hydroxytryptophan and 5-substituted indole-3-glyoxals as the ...
- Identification of human IKK-2 inhibitors of natural origin (Part II): In Silico prediction of IKK-2 inhibitors in natural extracts with known anti-inflammatory activity
[作者:Sala, E; Guasch, L; Iwaszkiewicz, J; Mulero, M; Salvado, MJ; Blade, C; Ceballos, M; Valls, C; Zoete, V; Grosdidier, A; Garcia-Vallve, S; Michielin, O; Pujadas, G,期刊:European Journal of Medicinal Chemistry, 页码:6098-6103 , 文章类型: Article,,卷期:2011年46-12]
- Human inhibitor NF-kappa b kinase 2 (hIKK-2) is the primary component responsible for activating NF-kappa B in response to various inflammatory stimuli. Thus, synthetic ATP-competitive inhibitors for hIKK-2 have been dev...
- Synthesis and inhibition study of monoamine oxidase, indoleamine 2, 3-dioxygenase and tryptophan 2,3-dioxygenase by 3,8-substituted 5H-indeno[1,2-c]pyridazin-5-one derivatives
[作者:Reniers, J; Meinguet, C; Moineaux, L; Masereel, B; Vincent, SP; Frederick, R; Wouters, J,期刊:European Journal of Medicinal Chemistry, 页码:6104-6111 , 文章类型: Article,,卷期:2011年46-12]
- Previous studies on 5H-indeno[1,2-c]pyridazin-5-one derivatives as inhibitors of MAO-B revealed that it was possible to increase the MAO-B inhibitory potency of 5H-indeno[1,2-c]pyridazin-5-ones by substituting the centra...
- Solvent-free, microwave assisted Knoevenagel condensation of novel 2,5-disubstituted indole analogues and their biological evaluation
[作者:Biradar, JS; Sasidhar, BS,期刊:European Journal of Medicinal Chemistry, 页码:6112-6118 , 文章类型: Article,,卷期:2011年46-12]
- A rapid, efficient and environmental benign methodology for the preparation of 2,5-disubstituted indole analogues is developed. 2,5-Disubstituted indole-3-carboxaldehydes (1a-c) undergo Knoevenagel condensation with barb...
- Synthesis and biological assessment of diversely substituted furo[2,3-b]quinolin-4-amine and pyrrolo[2,3-b]quinolin-4-amine derivatives, as novel tacrine analogues
[作者:Martins, C; Carreiras, MC; Leon, R; de los Rios, C; Bartolini, M; Andrisano, V; Iriepa, I; Moraleda, I; Galvez, E; Garcia, M; Egea, J; Samadi, A; Chioua, M; Marco-Contelles, J,期刊:European Journal of Medicinal Chemistry, 页码:6119-6130 , 文章类型: Article,,卷期:2011年46-12]
- The synthesis and pharmacological analyses of a number of furo[2,3-b]quinolin-4-amine, and pyrrolo [2,3-b]quinolin-4-amine derivatives are reported. Thus, we synthesized diversely substituted tacrine analogues 1-11 and 1...
|