Showing papers in "European Journal of Medicinal Chemistry in 2003"

TL;DR: A modification of the parallel artificial membrane permeation assay (PAMPA), developed with 30 structurally diverse commercial drugs and validated with 14 Wyeth Research compounds, has the advantages of predicting passive blood-brain barrier penetration with high success, high throughput, low cost, and reproducibility.

TL;DR: Fullerene is able to fit inside the hydrophobic cavity of HIV proteases, inhibiting the access of substrates to the catalytic site of the enzyme, and can be used as radical scavenger and singlet oxygen in high quantum yields.

TL;DR: A series of 3-substituted 4-[5-(4-methoxy-2-nitrophenyl)-2-furfurylidene] amino-5-mercapto-1,2,4-triazoles synthesized were screened for their anticancer activity against a panel of 60 cell lines derived from seven cancer types namely, lung, colon, melanoma, renal, ovarian, CNS and leukemia.

TL;DR: Extensive pre-clinical studies indicated that NHE inhibitors afford substantial protection in different animal models of myocardial ischemia (MI) and reperfusion, but the results of clinical trials involving eniporide and cariporides were mixed.

TL;DR: In this review, COX and 5-LOX pathways are first described in order to highlight the therapeutic interest of designing such compounds.

TL;DR: 2,6-Dimethyl-N'-(2-hydroxyphenylmethylidene)imidazo (3c) showed the most favorable cytotoxicity and demonstrated the most marked effects in the National Cancer Institute's 60 human tumor cell line in vitro screen on an ovarian cancer cell line.

TL;DR: Seven compounds, namely 7a-c, 9, 11, 13 and 14, exhibited potential and broad spectrum antitumor activity against most of the tested subpanel tumour cell lines (GI50<100 microM) and particular effectiveness on the leukaemia subpanel at both the GI50 and TGI levels.

TL;DR: A series of arylthioureas, aromatic aldehyde thiosemicarbazones, and 5-aryl-2-furfuraldehyde thIosemicarazones were condensed with 2,4-dichloro-5-fluorophenacyl bromide to yield respective arylaminothiazoles, aryLidene/5- Daryl-2 -furfurylidene hydrazinothia

TL;DR: 1-(5'-Nitro-2-furyl)-5-methyl-1,2,4-triazolo[4,3-a]quinoline (6e) was associated with substantially higher antibacterial activity than some commercial antibiotics against Salmonella typhi at MIC i.e. 10 microg mL(-1).

TL;DR: The synthesised compounds were found to provide 12-34% inhibition of mycobacterial growth of M. tuberculosis H37 Rv in the primary screen and determined by maximal electroshock (MES) and subcutaneous metrazole tests in mice and rats following the procedures of antiepileptic drug development (ADD) program of the National Institutes of Health.

TL;DR: Compounds 9a and 12a are the most distinctive derivatives identified in the present study because of their remarkable in vivo and in vitro anti-inflammatory activity in addition to their pronounced antibacterial activities comparable to ampicillin against Gram positive and -negative bacteria.

TL;DR: The antibacterial data revealed that compounds 7a-c had strong and better activity against tested Gram-positive organisms than the reference quinolones such as ciprofloxacin, norfloxacsin and enoxacIn, however, all three compounds were nearly inactive against Gram-negative bacteria.

TL;DR: Two series of N-[5-(2-furanyl)-2-methyl-4-oxo-4H-thieno[2,3-d]pyrimidin-3-yl]-carboxamide series have shown significant antibacterial and antimycobacterial activity against all the microbial strains used, when tested in vitro.

TL;DR: Several compounds exhibit stronger antiproliferative activities than the natural metabolite with IC(50) values in the nanomolar range and some analogues, especially those possessing azaindole moieties, are much more selective than rebeccamycin toward the tumour cell lines tested.

TL;DR: Using regression analysis QSAR, a relationship between biological activity and the physicochemical properties of the test compounds is found and their cytotoxic effect increases with an increase of the hydrophobic parameters in the region of the substituents at the 2-, 3- and 4-positions of the benzopyrone skeleton of 4-6.

TL;DR: Four-(Bromomethyl) coumarins 1, 2, 3 and 4 have been reacted with vanillins, 2 and 2A to obtain the corresponding ethers 3 and 5 and the aryloxymethyl coumarin with p-formyl group was found to be most active.

TL;DR: New choline-like quaternary ammonium chlorides derivatives of deanol esters exhibited strong activity and wide anti-bacterial spectra, similar to the activity of benzalkonium chloride.

TL;DR: The potency, selectivity and low cytotoxicity of 2-acetyl-3-methylquinoxaline 1,4-di-N-oxide derivatives make them valid leads for synthesizing new compounds that possess better activity.

TL;DR: In this study, alpha-diazo-beta-oxoaldehyde compounds were condensed with different amines to yield 4-acyl-1H-1,2,3-triazole derivatives, which were investigated for their inhibition activities against tuberculosis.

TL;DR: Among the different heterocyclic rings, the N-substituted indole ring is shown to be more conducive to both the activities than any other ring, however, a 5-membered ring is indicated to be less effective than a 9- or 10- Membered ring for activity B.

TL;DR: 3-[[(6-Chloro-3-phenyl-4(3H)-quinazolinone-2-yl)mercaptoacetyl]hydrazono]-5-fluoro-1H- 2-indolinone 5o showed the most favourable cytotoxicity against a renal cancer cell line UO-31.

TL;DR: A series of 1,4,6-trisubstituted pyrazolo[3,4-d]pyrimidines 15-19, 30-38 capable of selectively inhibiting CDK2 activity were synthesized by derivatization at C-4, C-6 and N-1 with various amines and lower alkyl groups.

TL;DR: The result shows that the extent of absorption in these two species is similar and it is suggested that the absorption in rats could be used as an alternative method to human absorption in pre-clinical oral absorption studies.

TL;DR: A series of 2,6-bis(arylidene)cycloalkanones and related compounds containing one or two substituents at the four position of the cyclohexyl ring were shown to display cytotoxic activity towards murine P388 and L1210 cells as well as human Molt 4/C8 and CEM T-lymphocytes.

TL;DR: New antiprotozoals active against Philasterides dicentrarchi, the causative agent of scuticociliatosis in farmed turbot and Black Sea bass-bream, have been synthesised and tested.

TL;DR: Pharmacokinetic evaluation of compound 1e in rats using LC/MS analysis unequivocally provides evidence that this compound is converted into the decarboxylated analogue 3a in the brain and the urine.

TL;DR: The aim is to prepare the introduction of the association of vitamins C and K(3) into human clinics as a new, non-toxic adjuvant cancer therapy and increase knowledge in the mechanisms underlying cancer cells death by CK( 3) may ameliorate the techniques of their in vivo administration.

TL;DR: Four Pt(II) complexes with 2-H/ or-methyl/or-aminomethylbenzimidazole or 1,2-dimethylbenzicazole ligands as "non-leaving groups" were synthesized and their antiproliferative properties were tested against the human MCF-7 breast cancer cell line.

TL;DR: A series of 2',5'-dihydroxychalcones were synthesized and evaluated for cytotoxicity against tumor cell lines and human umbilical venous endothelial cells (HUVEC) and several compounds were shown to have marked cytotoxic selectivity towards HUVECs.

TL;DR: For decades neuroreceptor research has focused on the development of NMDA glycine-site antagonists, after Johnson and Ascher found out in 1987 about the co-agonistic character of this achiral amino acid at the NMDA receptor.