- Analogs of pentamidine as potential anti-Pneumocystis chemotherapeutics
[作者:Maciejewska, D; Zabinski, J; Kazmierczak, P; Rezler, M; Krassowska-Swiebocka, B; Collins, MS; Cushion, MT,期刊:European Journal of Medicinal Chemistry, 页码:164-173 , 文章类型: Article,,卷期:2012年48-1]
- A series of 20 pentamidine analogs were prepared using 2 general Schemes that evaluated heteroatoms, sulfobenzene and alkanediamide groups in the aliphatic linker and methoxy substituents attached to the benzene rings fo...
- Synthesis of novel 1,3-diaryl pyrazole derivatives bearing rhodanine-3-fatty acid moieties as potential antibacterial agents
[作者:Xu, LL; Zheng, CJ; Sun, LP; Miao, J; Piao, HR,期刊:European Journal of Medicinal Chemistry, 页码:174-178 , 文章类型: Article,,卷期:2012年48-1]
- In the present study, a series of 1,3-diaryl pyrazole derivatives bearing rhodanine-3-fatty acid moieties were synthesized and their antimicrobial activities were tested against various Gram-positive and Gram-negative ba...
- Synthesis and antitumor evaluation of some new 1,3,4-oxadiazole-based heterocycles
[作者:Bondock, S; Adel, S; Etman, HA; Badria, FA,期刊:European Journal of Medicinal Chemistry, 页码:192-199 , 文章类型: Article,,卷期:2012年48-1]
- The synthetic strategies and characterization of some novel 1,3,4-oxadiazole derivatives carrying different pharmacophores and heterocyclic rings that are relevant to potential antitumor and cytotoxic activities are desc...
- Structure-based virtual screening for plant-derived SdiA-selective ligands as potential antivirulent agents against uropathogenic Escherichia coli
[作者:Ravichandiran, V; Shanmugam, K; Anupama, K; Thomas, S; Princy, A,期刊:European Journal of Medicinal Chemistry, 页码:200-205 , 文章类型: Article,,卷期:2012年48-1]
- The uropathogenic Escherichia colt pathogenecity is affected by quorum sensing transcriptional regulator SdiA. In this study, in vitro characterization of the active principles that could potentially antagonize with SdiA...
- A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation
[作者:Chiriano, G; De Simone, A; Mancini, F; Perez, DI; Cavalli, A; Bolognesi, ML; Legname, G; Martinez, A; Andrisano, V; Carloni, P; Roberti, M,期刊:European Journal of Medicinal Chemistry, 页码:206-213 , 文章类型: Article,,卷期:2012年48-1]
- In this work, we report a rational structure-based approach aimed at the discovery of new 2-aminoimidazoles as beta-secretase inhibitors. Taking advantage of a microwave-assisted synthetic protocol, a small library of de...
- Dibasic biphenyl H(3) receptor antagonists: Steric tolerance for a lipophilic side chain
[作者:Bordi, F; Rivara, S; Dallaturca, E; Carmi, C; Pala, D; Lodola, A; Vacondio, F; Flammini, L; Bertoni, S; Ballabeni, V; Barocelli, E; Mor, M,期刊:European Journal of Medicinal Chemistry, 页码:214-230 , 文章类型: Article,,卷期:2012年48-1]
- Within a series of histamine H(3)-antagonists characterized by a biphenyl core and two basic groups, we identified (S)-1-{[4'-((2-methylpyrrolidin-1-yl)methyl)biphenyl-4-yl]methyl}piperidine as a lead scaffold to introdu...
- Cytotoxic potential of novel 6,7-dimethoxyquinazolines
[作者:Yadav, MR; Grande, F; Chouhan, BS; Naik, PP; Giridhar, R; Garofalo, A; Neamati, N,期刊:European Journal of Medicinal Chemistry, 页码:231-243 , 文章类型: Article,,卷期:2012年48-1]
- Herein, we report the synthesis and cytotoxicity of a series of substituted 6,7-dimethoxyquinazoline derivatives. The cytotoxic activity of all synthesized compounds has been evaluated against HCT116p53(+/+) and HCT116p5...
- Synthesis and bioevaluation of novel 3,4,5-trimethoxybenzylbenzimidazole derivatives that inhibit Helicobacter pylori-induced pathogenesis in human gastric epithelial cells
[作者:Chang, CS; Liu, JF; Lin, HJ; Lin, CD; Tang, CH; Lu, DY; Sing, YT; Chen, LY; Kao, MC; Kuo, SC; Lai, CH,期刊:European Journal of Medicinal Chemistry, 页码:244-254 , 文章类型: Article,,卷期:2012年48-1]
- Helicobacter pylori infection is associated with gastritis, peptic ulcer, and even gastric malignancy. H. pylori's antibiotic resistance is the major obstacle preventing its eradication. A series of 3,4,5-trimethoxybenzy...
- Activity of novel quinoxaline-derived chalcones on in vitro glioma cell proliferation
[作者:Mielcke, TR; Mascarello, A; Filippi-Chiela, E; Zanin, RF; Lenz, G; Leal, PC; Chirardia, LD; Yunes, RA; Nunes, RJ; Battastini, AMO; Morrone, FB; Campos, MM,期刊:European Journal of Medicinal Chemistry, 页码:255-264 , 文章类型: Article,,卷期:2012年48-1]
- Gliomas are the most common and devastating tumors of the central nervous system (CNS). Many pieces of evidence point out the relevance of natural compounds for cancer therapy and prevention, including chalcones. In the ...
- Montmorillonite K-10 mediated green synthesis of cyano pyridines: Their evaluation as potential inhibitors of PDE4
[作者:Reddy, TR; Reddy, GR; Reddy, LS; Jammula, S; Lingappa, Y; Kapavarapu, R; Meda, CLT; Parsa, KVL; Pal, M,期刊:European Journal of Medicinal Chemistry, 页码:265-274 , 文章类型: Article,,卷期:2012年48-1]
- An efficient and green synthesis of functionalized cyano pyridines has been achieved via montmorillonite K-10 mediated multi-component reaction in a chemo- and regioselective manner. The four-component reaction of beta-k...
- Synthesis and evaluation of platelet aggregation inhibitory activity of some 3-phenyl-pyrroloquinazolinones
[作者:Ferlin, MG; Borgo, C; Deana, R,期刊:European Journal of Medicinal Chemistry, 页码:275-283 , 文章类型: Article,,卷期:2012年48-1]
- A series of 3-phenyl-2,7-dihydro-1H-pyrrolo[3,2-f]quinazolin-1-one derivatives (3-PPyQZ) was synthesized starting from 5-amino-indoles, via condensation with N-ethoxycarbonylthiobenzamides followed by thermal cyclization...
- Synthesis and biological assessment of novel 2-thiazolylhydrazones and computational analysis of their recognition by monoamine oxidase B
[作者:Distinto, S; Yanez, M; Alcaro, S; Cardia, MC; Gaspari, M; Sanna, ML; Meleddu, R; Ortuso, F; Kirchmair, J; Markt, P; Bolasco, A; Wolber, G; Secci, D; Maccioni, E,期刊:European Journal of Medicinal Chemistry, 页码:284-295 , 文章类型: Article,,卷期:2012年48-1]
- Monoamine oxidase B (MAO-B) is a promising target for the treatment of neurodegenerative disorders. We report the synthesis and the biological evaluation of halogenated derivatives of 1-aryliden-2-(4-phenylthiazol-2-yl)h...
- Synthesis and anti-protozoal activity of novel dihydropyrrolo[3,4-d][1,2,3]triazoles
[作者:Durust, Y; Karakus, H; Kaiser, M; Tasdemir, D,期刊:European Journal of Medicinal Chemistry, 页码:296-304 , 文章类型: Article,,卷期:2012年48-1]
- 1,2,4-Oxadiazole and 1,2,3-triazole containing heterocyclic compounds continue to gain interest in synthesis of chemical entities and exhibit various biological activities as anti-protozoal and anti-cancer agents. By usi...
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