- Synthesis and in vitro anti-Helicobacter pylori activity of N-[5-(5-nitro-2-heteroaryl)-1,3,4-thiadiazol-2-yl]thiomorpholines and related compounds
[作者:Mirzaei, J; Siavoshi, F; Emami, S; Safari, F; Khoshayand, MR; Shafiee, A; Foroumadi, A,期刊:European Journal of Medicinal Chemistry, 页码:1575-1580 , 文章类型: Article,,卷期:2008年43-8]
Synthesis and in vitro anti-Helicobacter pylori activity of N-[5-(5-nitro-2-heteroaryl)-1,3,4-thiadiazol-2-yl]thiomorpholines 5-7(a-c) and some related compounds 8a-c and 9a-c were described. The anti-H. pylori activi...
- In silico prediction of brain and CSF permeation of small molecules using PLS regression models
[作者:Bendels, S; Kansy, M; Wagner, B; Huwyler, J,期刊:European Journal of Medicinal Chemistry, 页码:1581-1592 , 文章类型: Article,,卷期:2008年43-8]
Computational partial least square (PLS) regression models were developed, which can be applied to predict central nervous system (CNS) penetration of drug-like organic molecules. For modeling, a dataset of 77 structu...
- Effects of 3-(4 '-geranyloxy-3 '-methoxyphenyl)-2-trans propenoic acid and its ester derivatives on biofilm formation by two oral pathogens, Porphyromonas gingivalis and Streptococcus mutans
[作者:Bodet, C; Epifano, F; Genovese, S; Curini, M; Grenier, D,期刊:European Journal of Medicinal Chemistry, 页码:1612-1620 , 文章类型: Article,,卷期:2008年43-8]
The aim of this study was to investigate the effect of 3-(4 '-geranyloxy-3 '-methoxyphenyl)-2-trans propenoic acid, active principle isolated from Acronychia baueri Schott, and its ester derivatives on biofilm formati...
- Structure-activity relationships for the inhibition of recombinant human cytochromes P450 by curcumin analogues
[作者:Appiah-Opong, R; de Esch, I; Commandeur, JNM; Andarini, M; Vermeulen, NPE,期刊:European Journal of Medicinal Chemistry, 页码:1621-1631 , 文章类型: Article,,卷期:2008年43-8]
Inhibition of cytochrome P450 (CYP) is a major cause of drug-drug interactions. In this work, inhibitory potentials of 33 curcumin analogues, i.e. 2,6-dibenzylidenecyclohexanone (A series), 2,5-dibenzylidenecyclopenta...
- Preparation and antibacterial activity of cyclic 2 ',3 '-carbamate derivatives of azithromycin
[作者:Heggelund, A; Romming, C; Undheim, K,期刊:European Journal of Medicinal Chemistry, 页码:1657-1664 , 文章类型: Article,,卷期:2008年43-8]
In a study of the importance of a basic amino function in erythromycin derived antibiotics, N '-demethylazithromycin 2 ',3 '-carbamate-11, 12-carbonate has been prepared in six steps from (9E)-erythromycin A 9-oxime. ...
- 1,8-naphthyridines VII. New substituted 5-amino[1,2,4] triazolo [4,3-a][1,8]naphthyridine-6-carboxamides and their isosteric analogues, exhibiting notable anti-inflammatory and/or analgesic activities, but no acute gastrolesivity
[作者:Roma, G; Grossi, G; Di Braccio, M; Piras, D; Ballabeni, V; Tognolini, M; Bertoni, S; Barocelli, E,期刊:European Journal of Medicinal Chemistry, 页码:1665-1680 , 文章类型: Article,,卷期:2008年43-8]
The [1,2,4]triazolo[4,3-a][1,8]naphthyridine-6-carboxamide derivatives 5-amino (2) or 5-alkoxy (3) substituted and the 5-amino[1,2,4] triazolo[4,3-a]quinoline-4-carboxamide derivatives (4), designed to obtain new effe...
- Synthesis, characterization, antioxidant activity and DNA-binding studies of two rare earth(III) complexes with naringenin-2-hydroxy benzoyl hydrazone ligand
[作者:Li, TR; Yang, ZY; Wang, BD; Qin, DD,期刊:European Journal of Medicinal Chemistry, 页码:1688-1695 , 文章类型: Article,,卷期:2008年43-8]
Two novel rare earth complexes, Y(III) complex (1) and Eu(III) complex (2), with naringenin-2-hydroxy benzoyl hydrazone ligand were synthesized and characterized. The interaction of the two metal complexes and the fre...
- Synthesis, binding properties and receptor docking of 4-halo-6-[2-(4-arylpiperazin-1-yl)ethyl]-1H-benzimidazoles, mixed ligands of D-2 and 5-HT1A receptors
[作者:Andric, D; Roglic, G; Sukalovic, V; Soskic, V; Kostic-Rajacic, S,期刊:European Journal of Medicinal Chemistry, 页码:1696-1705 , 文章类型: Article,,卷期:2008年43-8]
In this publication we are describing synthesis, binding properties, and receptor docking of 4-halo-6-[2-(4-arylpiperazin-1-yl)ethyl]-1H-benzimidazoles, a new compounds with potential antipsychotics properties. Affini...
- Synthesis and anti-inflammatory evaluation of methylene bridged benzofuranyl imidazo[2,1-b][1,3,4]thiadiazoles
[作者:Jadhav, VB; Kulkarni, MV; Rasal, VP; Biradar, SS; Vinay, MD,期刊:European Journal of Medicinal Chemistry, 页码:1721-1729 , 文章类型: Article,,卷期:2008年43-8]
A series of 6-substituted and 5,6-disubstituted 2-(6-methyl-benzofuran-3-ylmethyl)-imidazo[2,1-b] [ 1,3,4]thiadiazoles have been synthesized. The new compounds have been tested for their in vivo analgesic, anti-inflam...
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