Showing papers in "European Journal of Medicinal Chemistry in 2005"

TL;DR: Design of a second generation ofHDACs was based upon data affording potent HDACs such as LAQ824 and PDX101 currently under phase I clinical trials, and two of them, MS-275 and CI-994, have reached phase II and I clinical Trials, respectively.

TL;DR: 4-(4-Hydroxy-benzylidene-imino)phenyl)-morpholine (7) was found to be the most potent antimicrobial activity with MIC of 25, 19, 21, 16, 29, 20 and 40 microg/ml against S. aureus, S. epidermidis, B. cereus, M. luteus, E. albicans and A. niger, respectively.

TL;DR: It is demonstrated that 1-3, and 7 have anti-inflammatory effects and 5, 6, and 12 are potential anti- inflammation and cancer chemopreventive agents.

TL;DR: Ursolic acid and 2alpha-hydroxyursolic acid isolated from apple peels were found to show growth inhibitory activity against four tumor cell lines, HL-60, BGC, Bel-7402 and Hela.

TL;DR: Two substituted 1,2, 3-triazoles 4 and 6 have been synthesized by the 1,3-dipolar cycloaddition reaction of 4-azido-8-(trifluoromethyl)quinoline 2 with ethyl acetoacetate and acetylacetone, respectively and screened for their antimicrobial activity.

TL;DR: New thiazole derivatives of triazoles were synthesized and evaluated for antifungal and antibacterial activity and showed that some of the compounds have very strong antIfungal activity.

TL;DR: The ligand L has been synthesized by the condensation reaction of 2-mercaptobenzimidazole and diethyloxalate and the results reveal that the complex 1 is highly active against the bacterial strains and also inhibits fungal growth.

TL;DR: In an effort to establish new candidates with improved antineoplastic, anti-HIV-1 and antimicrobial activities, the synthesis and in vitro biological evaluation of various series of 2-substituted benzoxazoles are reported.

TL;DR: Under suitable conditions PAMAM dendrimers can be highly effective used to enhance the solubility of NSAIDs.

TL;DR: From the results, novel compounds, 5c and 5g, exhibited considerably more potent biological activity than that of the reference compounds, pioglitazone and rosig litazone, respectively.

TL;DR: The inhibition of AChE and butyrylcholinesterase (BChE) were determined: compounds 13, 15a, 17, and 20 are moderate or strong inhibitors of ChE, the latter two compounds show a 10-fold higher affinity to BChE.

TL;DR: Several new pyrazolo[3,4-d]pyridazin derivatives were prepared by the reaction of two [corrected] 1H-pyrazole-3-carboxylic acids and various hydrazines and had the highest antimicrobial activities against Gram-negative, Gram-positive bacteria and fungi.

TL;DR: Spiro derivatives of oxindole and isoxazole-5-one were synthesized by using Michael addition reaction, highlighting the regioselective approach towards the synthesis of Michael diadduct followed by condensation of Michaeldiadduct.

TL;DR: The results showed that compounds 45-46 and 55-57, having 3,4-dichloro substituted phenyl at the position C-2, of N-bulky alkyl substituted benzimidazolecarboxamidines exhibited the greatest activity with MIC values of 1.56-0.39 microg/ml.

TL;DR: The synthesis of four novel compounds, including hydrazones (2), (3) and (7) exist in two conformers as synperiplanar and antiperiPlanar, and Structural assignment, stereochemistry and biological assays are discussed.

TL;DR: It is demonstrated that amino group is an effective substitute for the hydroxyl group for antioxidant property and produced a dramatic inhibition of lipid peroxidation.

TL;DR: Under suitable conditions PAMAM dendrimers can be highly effective used to enhance the solubility of ketoprofen.

TL;DR: A novel, ecofriendly, one pot solvent free method for the synthesis of 4-aryl-7,7-dimethyl-1,2,3,4,5,6,7,8-octahydroquinazoline-2-one/thione-5-one derivatives is described which devoids the use of any organic solvents and auxiliaries.

TL;DR: Comparison of the cytotoxic effects of the three newly synthesized lanthanum complexes against the acute myeloid leukemia derived HL-60 and the chronic myeloids leukemia (CML)-derived BV-173 and the ability of this complex to trigger programmed cell death is evaluated.

TL;DR: The data suggested that the antitumor potencies of beta-carboline derivatives were enhanced by the introduction of benzyl substituent into the position-2, the acute toxicity of Beta- carboline derivatives reduced dramatically by the introducing of an appropriate substituents into the positions-3 and 9.

TL;DR: The 3D models of both CB1 and CB2 human receptors have been established by homology modeling using as template the X-ray structure of bovine Rhodopsin a G-protein-coupled receptor (GPCR) to model the receptor-ligand complexes.

TL;DR: The cyclisation to 4-hydroxy coumarin 6 was found to be reducing the anti-inflammatory and analgesic activity in this series and these newly synthesized compounds were found to produce less toxicity and less ulcerogenic effects.

TL;DR: (benzofuran-2-yl)(3-phenyl-3-methyl cyclobutyl)-O-benzylketoxime 6a showed good antimicrobial effect against C. albicans ATCC 10231 and was found the most active derivative against S. aureus ATCC 6538.

TL;DR: A series of substituted 2-polyfluoroalkyl and 2-nitrobenzylsulphanyl benzimidazoles was synthesized and showed appreciable antimycobacterial activity, particularly 5,6-dichloro-2-nonafluorobutylbenzimidrazole (2h).

TL;DR: The triazolothiadiazine analogues 6a-e were obtained via a multistep synthesis sequences beginning with the hydroxybenzophenones 1a- e and tested against variety of fungal and bacterial strains in comparison to fluconazole and chloramphenicol, respectively.

TL;DR: QSAR analysis of new antibacterial benzenesulfonamidefluoroquinolones coming from derivatization of N4-piperazinyl of ciprofloxacin were studied, showing a linear correlation of the activity with electronic and steric parameters and reinforces previous biological findings about the presence of new interactions with target topoisomerases.

TL;DR: The results revealed that these complexes are effective chemicals in inhibiting amoebal growth, with compound 5 (having -N(CH3)(C6H5) substituent at N4) and complexes 1a-5a being more effective than the commercial antiamoebic drug, metronidazole, based on IC50 values.

TL;DR: Compounds 2a, 2b, 2c, 4c and 4f proved to exert cardiotonic activity comparable to that of milrinone using spontaneously beating atria model from reserpine-treated guinea pigs and proved to be non-toxic and well tolerated by mice up to 250 mg kg (-1) orally and up to 125 mg kg(-1) through parenteral route.

TL;DR: Nine new (+/-)-8-alkyl-5,7-dihydroxy-4-(4-hydroxyphenyl)-3,4- dihydrocoumarins have been synthesized from 2,4,6-trimethoxybenzaldehyde via a short, efficient, and regioselective pathway.

TL;DR: A new series of 2,6-dibenzylamino-3,5-dicyanopyridines synthesized and evaluated for their in vitro anticancer activity toward cell lines of nine different types of human cancer demonstrated remarkable antic cancer activity against most of the tested subpanel tumor cell lines.