Showing papers in "European Journal of Medicinal Chemistry in 2004"

TL;DR: The study showed that the compounds inhibited the induction of gastric mucosal lesions and it can be suggested from the results that their protective effects may be related to inhibition of lipid peroxidation in the Gastric mucosa.

TL;DR: A series of hydrazones synthesized from various cholesterol derivatives were evaluated for their in vitro antimicrobial properties against human pathogens and the best results have been obtained with tosylhydrazone cholesterol derivatives 8 and 9.

TL;DR: Acetic acid ethyl esters containing 5-oxo-[1,2,4]triazole ring (2) were synthesized by the condensation of compounds 1a-f with ethyl bromoacetate in basic media and compounds 7a,c,d,f were obtained.

TL;DR: Structural-activity relationships (SAR) studies revealed that benzothiazole ring system enhanced the antimicrobial activity against Staphylococcus aureus and electron withdrawing groups at position 5 of the benzazoles increased the activity against C. albicans.

TL;DR: The quantitative models relating the structural features of cinnamic acid derivatives I, II and III and their antimicrobial activity showed that Gram negative Escherichia coli and Candida albicans (fungus) were the most sensitive microorganisms.

TL;DR: Some pyridazinone derivatives showed appreciable activity and the antihypertensive activities of the compounds were examined both in vitro and in vivo.

TL;DR: The location of the methyl group at the C-3 of compounds 12 and 14 has been demonstrated to be a key structural element of antifungal potency.

TL;DR: A series of 3- and 5-methylthiophene-2-carboxaldehyde alpha-(N)-heterocyclichydrazones were synthesized and submitted to an in vitro investigation of their anticancer, anti-HIV and antimicrobial activities, where some of the newly synthesized compounds were found to possess antiproliferative properties.

TL;DR: The most active compound, 3-[1-acetyl-5-(p-hydroxyphenyl)-2-pyrazolin-3-yl]indole (7) was found to be most potent, which has shown higher percent of inhibition of oedema, lower ulcerogenic liability and acute toxicity than the standard drug phenylbutazone.

TL;DR: Four tetrazolo[1,5-a]quinoline derivatives were proved to be as active as indomethacin in animal models of inflammation and antimicrobial activities.

TL;DR: 5-(4-[2-[N-methyl-(5-phenyl-pyridin-2-yl)amino]ethoxy]benzyl)thiazolidine-2,4-dione (6d) was selected as a candidate for further pharmacological studies.

TL;DR: It is shown that logarithms of PS-products, log PS, can satisfactorily be correlated with the five Abraham descriptors for 30 neutral compounds, and molecular size leads to an increase in permeation rate, and dipolarity/polarizability, hydrogen bond acidity and hydrogen bond basicity all decrease the rate of permeation.

TL;DR: The Tuberculosis Antimicrobial Acquisition and Coordinating Facility has provided anti-mycobacterial data concerning inhibition activity of 12 compounds.

TL;DR: Some 2-[(benzazole-2-yl)thioacetylamino]thiazole derivatives (III) were synthesized by reacting 4-methyl-2-(chloroacetyamino)thiazoles derivatives (I) with benzazol- 2-thiole (II) in acetone in the presence of K(2)CO(3).

TL;DR: The pharmacophore, which contains two hydrogen bond acceptors (lipid) and two hydrophobic (aromatic) features, was found to map well onto many well-known antimalarial drug classes including quinolines, chalcones, rhodamine dyes, Pfmrk cyclin dependent kinase inhibitors, malarial FabH inhibitors, and plasmepsin inhibitors.

TL;DR: (1,3-Benzothiazol-2-yl) amino-9-(10H)-acridinone derivatives were synthesized via a procedure based on the Ullman reaction and were assessed for their in vitro antileishmanial and anti-HIV activities.

TL;DR: Examination of structure-activity-relationships at P2 receptors of a series of NF449 analogues found it to be the most potent and selective P2X(1) antagonist known.

TL;DR: Synthesis of some new 3-aryl/hetryl-5,7-dimethyl-1,2,4-triazolo[4,3-a]pyrimidines (3a-k) has been accomplished by the oxidation of 4,6-dimethy-2- pyrimidinylhydrazones of various aldehydes with iodobenzene diacetate in dichloromethane.

TL;DR: Out of the 12 compounds synthesized, compound 5[beta-(phenothiazinyl-10-yl)ethyl]-1-(benzoyl)-1,2,3,4-tetrazole showed promising anti-inflammatory activity.

TL;DR: These compounds exhibited in vitro antitumour activity with moderate to excellent growth inhibition against a panel of 60 cell lines of leukemia, non-small cell lung cancer melanoma, ovarian cancer, prostate cancer and breast cancer.

TL;DR: These compounds were converted to 5-(2-substituted-1,3-thiazol-5-yl)-2-alkoxybenzamides and 5-N-(subStituted aryl)-1, 3-th Diazol- 5-yl)2-alksoxy benzamides by reacting with n-alkylbromides (7a-b) in presence of a base.

TL;DR: Some novel benzoxazolylethoxypiperidones have been synthesized and their antibacterial activity against streptococcus faecalis, bacillus subtilis, escherichia coli, staphylococcus aureus aand pseudomonas aeruginosa and antifungal activity against Candida-6 and Aspergillus niger were evaluated.

TL;DR: The optimised conditions for synthesis and purification of PEG-Ara-C products with a low amount of remaining free drug are reported, and aminoadipic acid was a suitable bicarboxylic amino acid to overcome the steric hindrance between the vicinal Ara-C molecules in the dendrimeric structure.

TL;DR: A new series of 23 6,7-difluoro-3-methyl-2-phenylthio/phenylsulfonyl/phenYLsulfinyl/benzylamino/phenylamino-quinoxaline 1,4-dioxides variously substituted in the phenyl moiety, was synthesized and submitted to in vitro evaluation for anti-mycobacterial, anti-trichomonas, anti

TL;DR: FSB was found to stain amyloid plaques and neurofibrillary tangles of AD brains with greater fluorescence intensity and a lower level of background signals compared to BSB, indicating that FSB can be an excellent fluorescent compound to label human amyloids lesions with high sensitivity and specificity.

TL;DR: Physiological nature of flavonoids reveals biotechnological source of new trypsin inhibitors as antipancreatitis, anticancer and anti-inflammation drugs.

TL;DR: The investigated compound showed anticonvulsive activity and potent antinociceptive action.

TL;DR: The observation of significant anti-tuberculosis activity in some of these analogues is described, and the discovery of novel ring-substituted-1H-imidazole-4-carboxylic acid ethyl esters as a new class of anti-Tuberculosis agents is described.

TL;DR: All the tested compounds highly inhibited the soybean lipoxygenase, whereas compounds 12, 17 and 19(II) highly compete with DMSO for (*)OH.

TL;DR: 6-chloro-2-styryl-3-(pyrimidin-2yl)-4(3H)-quinazolinone inhibited the growth of human MCF7 breast carcinoma cells and Burkitt lymphoma CA46 cells, consistent with its mechanism of action resulting from its inhibitory effect on tubulin assembly.