17 research outputs found
Synthesis and antimicrobial activity of hydroxy-isophthalaldehyde acid derivatives.
No full text4-hydroxy-isophthalaldehyde acid (1), its alkyl esters (methyl, ethyl, propyl and butyl) and alkyl ethers (propyl, butyl, pentyl and esyl), as well as 6-hydroxy-isophthalaldehyde acid (2) ita alkyl esters (methyl and ethyl), 4-hydroxy-5-iodo-isophthalaldehyde acid (3) and its methyl ester were synthesized and characterized. Antimicrobial and antifungal activity was tested and the LD50 of the most active compound 4 was determined
Synthesis and pharmacological activity of 2-(substituted phenyl)-3-{2 or 3-[(4-substituted phenyl-4-hydroxy)piperidino]ethyl or propyl}-1,3-thiazolidin-4-ones.
No full textDiurno MV, Mazzoni O, Capasso F, Izzo AA, Bolognese A. Synthesis andpharmacological activity of 2-(substituted phenyl)-3-[2 or 3-[(4-substituted phenyl-4-hydroxy)piperidino]ethyl or propyl]-1,3-thiazolidin-4-ones.
No full textGOMEZ-MONTERREY I. M., CAMPIGLIA P., MAZZONI O., NOVELLINO E., DIURNO M. V. (2001). Cycloaddition reactions of thiazolidine derivatives. An approach to the synthesis of new functionalized heterocyclic systems. TETRAHEDRON LETTERS. vol. 42, pp. 5755-5757 ISSN: 0040-4039.
No full textAntidiarrhoeal activity of new thiazolidinones related to loperamide.
No full textA series of thiazolidinones related to loperamide was synthesized and evaluated for antidiarrhoeal activity in mice, using the castor oil test. Of five compounds tested, antidiarrhoeal activity was found only for 2-(p-nitrophenyl)-3-¿3-[(4-(p-chlorophenyl)-4-hydroxy)piperidino]ethyl¿- 1,3-thiazolidin-4-one. The compound was less active than loperamide (ED50 values = 48.7 (24.8-95.6) and 0.91 (0.24-3.40) mg kg-1 respectively), but was also less toxic (LD50 values = 745.9 (545.2-929.8) and 108.9 (85.5-138.7) mg kg-1, respectively). Its antidiarrhoeal activity was counteracted by naloxone. Our results support the hypothesis that this compound, like loperamide, is an opiate-receptor agonist
Binding site of loperamide: automated docking of loperamide in human mi - and delta -opioid receptors.
No full textSynthesis of new pyrido[4,3-g and 3,4-g]quinoline-5,10-dione and dihydro thieno[[2,3-g and 3,2-g]quinoline-4,9-dione derivatives and perliminary evaluation of cytotoxic activity
No full textNew benzo[g]isoquinoline-5,10-diones and dihydrothieno [2,3-b]naphtho-4,9-dione derivatives
No full textNovel antitumoral agents with quinonic structure were synthesized and evaluated for their in vitro cytotoxic activities. This study examines the cytotoxic activities of several aryl benzo[g]isoquinoline-5,10-dione derivatives and a number of aminoacyl dihydrothieno[2,3-b]naphtho-4.9-dione (DTNQ) derivatives containing amino acids in position 3 of the ring system. Compound 6 showed remarkable cytotoxic activity at submicromolar concentration not only against several human leukaemia and solid tumour cell lines, but also toward sensitive and resistant human cell lines
A novel approach to the synthesis of diaza-bridged heterocycle derivatives
No full textA novel synthetic route of diaza-bridged heterocycles based on natural 3,9-diazabicyclo[3.3.1]non-6-ene scaffold has been accomplished. The synthetic approach consists of a Pictet-Spengler condensation of the l-Dopa-OMe with an appropriate aldehyde, Fmoc-Aa-H, followed by intramolecular lactamization. This approach generated two configurationally distinct products (cis and trans-isomers), increasing the stereochemical diversity of these compounds
