- Regioselective hydrostannation of diarylalkynes directed by a labile ortho bromine atom: An easy access to stereodefined triarylolefins, hybrids of combretastatin A-4 and isocombretastatin A-4
[作者:Rasolofonjatovo, E; Provot, O; Hamze, A; Bignon, J; Thoret, S; Brion, JD; Alami, M,期刊:European Journal of Medicinal Chemistry, 页码:3617-3626 , 文章类型: Article,,卷期:2010年45-9]
- A series of triarylolefins bearing the combretastatin A-4 and the isocombretastatin A-4 cores were synthesized and evaluated. The cooperative ortho-effect of a labile bromine atom in the regioselective hydrostannation of...
- Synthesis and antibacterial activities of 6-O-methylerythromycin A 9-O-(3-aryl-2-propenyl) oxime ketolide, 2,3-enol ether, and alkylide analogues
[作者:Liang, JH; Dong, LJ; Wang, H; An, K; Li, XL; Yang, L; Yao, GW; Xu, YC,期刊:European Journal of Medicinal Chemistry, 页码:3627-3635 , 文章类型: Article,,卷期:2010年45-9]
- A facile and efficient route was presented to achieve 3-keto-clarithromycin 9-O-(3-aryl-E-2-propenyl) oxime derivatives 8, 2,3-dehydro-3-O-allyl-clarithromycin 9-O-(3-aryl-E-2-propenyl) oxime derivatives 11, and 3-O-ally...
- Effect of flavonoids on the A beta(25-35)-phospholipid bilayers interaction
[作者:Tedeschi, A; D'Errico, G; Lauro, MR; Sansone, F; Di Marino, S; D'Ursi, AM; Aquino, RP,期刊:European Journal of Medicinal Chemistry, 页码:3998-4003 , 文章类型: Article,,卷期:2010年45-9]
- Amyloid-beta peptide (A beta) is the major component of amyloid deposits found in the brain tissue of Alzheimer patients. The tendency of amyloid peptide to form amyloid plaques is known to be related to the features of ...
- Identification of potent virtual leads to design novel indoleamine 2,3-dioxygenase inhibitors: Pharmacophore modeling and molecular docking studies
[作者:John, S; Thangapandian, S; Sakkiah, S; Lee, KW,期刊:European Journal of Medicinal Chemistry, 页码:4004-4012 , 文章类型: Article,,卷期:2010年45-9]
- Indoleamine 2,3-dioxygenase, a heme-containing enzyme, is emerging as a vital target for the treatment of cancer, chronic viral infections, and other diseases. The aim of this study is to identify novel scaffolds and uti...
- Design, synthesis and biological evaluation of new (E)- and (Z)-1,2,3-triaryl-2-propen-1-ones as selective COX-2 inhibitors
[作者:Arfaie, S; Zarghi, A,期刊:European Journal of Medicinal Chemistry, 页码:4013-4017 , 文章类型: Article,,卷期:2010年45-9]
- A group of (E)-and (Z)-1,2,3-triaryl-2-propen-l-one derivatives possessing a methylsulfonyl COX-2 pharmacophore at the para position of the C-1 phenyl ring were synthesized and evaluated as selective COX-2 inhibitors. In...
- Synthesis and antibacterial activity of 3-O-carbamoyl derivatives of 6,11-di-O-methylerythromycin A: A novel class of acylides
[作者:Wu, ZY; Lu, Y; Luo, M; He, XR; Xiao, YL; Yang, J; Pan, YH; Qiu, GF; Guo, H; Hu, H; Zhou, DS; Hu, XM,期刊:European Journal of Medicinal Chemistry, 页码:3636-3644 , 文章类型: Article,,卷期:2010年45-9]
- A novel series of acylides, 3-O-carbamoyl derivatives of 6,11-di-O-methylerythromycin A, were synthesized and evaluated for their antibacterial activity. These compounds have significant antibacterial activity against Gr...
- Synthesis of substituted thieno[2,3-d]pyrimidine-2,4-dithiones and their S-glycoside analogues as potential antiviral and antibacterial agents
[作者:Hafez, HN; Hussein, HAR; El-Gazzar, ARBA,期刊:European Journal of Medicinal Chemistry, 页码:4026-4034 , 文章类型: Article,,卷期:2010年45-9]
- Previously, we synthesized and evaluated several thienopyrimidine derivatives containing heterocyclic ring substituents linked to the pyrimidine-2-thione nucleus at C-2 by a two- to four-atom spacer as potential anti-HIV...
- Design, synthesis and biological evaluation of L-dopa amide derivatives as potential prodrugs for the treatment of Parkinson's disease
[作者:Zhou, T; Hider, RC; Jenner, P; Campbell, B; Hobbs, CJ; Rose, S; Jairaj, M; Tayarani-Binazir, KA; Syme, A,期刊:European Journal of Medicinal Chemistry, 页码:4035-4042 , 文章类型: Article,,卷期:2010年45-9]
- A range of amide derivatives of L-dopa were synthesized and investigated for their pharmacological activity and their ability to be converted to L-dopa using the unilaterally 6-hydroxydopamine (6-OHDA)-lesioned rat, as a...
- Novel Tc-99m '4 + 1' peptide conjugates: Tuning the biodistribution by variation of coligands
[作者:Kunstler, JU; Seidel, G; Bergmann, R; Gniazdowska, E; Walther, M; Schiller, E; Decristoforo, C; Stephan, H; Haubner, R; Steinbach, J; Pietzsch, HJ,期刊:European Journal of Medicinal Chemistry, 页码:3645-3655 , 文章类型: Article,,卷期:2010年45-9]
- A sophisticated coligand strategy is presented for peptide-derived radioconjugates based on Tc-99m '4 + 1' mixed-ligand complexes. The new pharmacologically active coligands are assessed for Tc-99m-labeling of the RGD-pe...
- Carbonic anhydrase inhibitors. Regioselective synthesis of novel 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the human cytosolic isozymes I and II and transmembrane cancer-associated isozymes IX and XII
[作者:Brzozowski, Z; Slawinski, J; Innocenti, A; Supuran, CT,期刊:European Journal of Medicinal Chemistry, 页码:3656-3661 , 文章类型: Article,,卷期:2010年45-9]
- A series of 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamide (2-16) have been synthesized and investigated as inhibitors of four isoforms of zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1), that is the cytosolic ubi...
- Structural characterization and antibacterial activity against clinical isolates of Staphylococcus of N-phenylamide of monensin A and its 1:1 complexes with monovalent cations
[作者:Lowicki, D; Huczynski, A; Stefanska, J; Brzezinski, B,期刊:European Journal of Medicinal Chemistry, 页码:4050-4057 , 文章类型: Article,,卷期:2010年45-9]
- The ability of N-phenylamide of monensin A (M-AM1) to form complexes with Li+, Na+ and K+ cations is studied by ESI MS, H-1 and C-13 NMR, FT-IR spectroscopy and PM5 semi-empirical methods. ESI mass spectrometry indicates...
- 3-Formylchromones: Potential antiinflammatory agents
[作者:Khan, KM; Ambreen, N; Mughal, UR; Jalil, S; Perveen, S; Choudhary, MI,期刊:European Journal of Medicinal Chemistry, 页码:4058-4064 , 文章类型: Article,,卷期:2010年45-9]
- The synthesis and characterization of 3-formylchromone (1) and its derivatives 2-24 and evaluation of their potential antiinflammatory activities is reported here. These compounds were characterized by H-1 NMR, El MS, IR...
- Influence of bulky 3,3 '-diphenylalanine enantiomers replacing position 2 of AVP analogues on their conformations: NMR and molecular modeling studies
[作者:Sikorska, E; Kwiatkowska, A; Sobolewski, D; Slusarz, R; Slusarz, MJ,期刊:European Journal of Medicinal Chemistry, 页码:4065-4073 , 文章类型: Article,,卷期:2010年45-9]
- In this paper we use NMR spectroscopy and molecular modeling to examine four vasopressin analogues substituted with bulky 3,3'-diphenylalanine (Dpa) enantiomers: [Mpa(1),Dpa(2),Val(4),D-Arg(8)]VP (I), [Mpa(1),D-Dpa(2),Va...
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