1027244-50-3Relevant academic research and scientific papers
Chalcones: A valid scaffold for monoamine oxidases inhibitors
Chimenti, Franco,Fioravanti, Rossella,Bolasco, Adriana,Chimenti, Paola,Secci, Daniela,Rossi, Francesca,Yá?ez, Matilde,Orallo, Francisco,Ortuso, Francesco,Alcaro, Stefano
experimental part, p. 2818 - 2824 (2010/01/16)
A large series of substituted chalcones have been synthesized and tested in vitro for their ability to inhibit human monoamine oxidases A and B (hMAO-A and hMAO-B). While all the compounds showed hMAO-B selective activity in the micro- and nanomolar ranges, the best results were obtained in the presence of chlorine and hydroxyl or methoxyl substituents. To better understand the enzyme-inhibitor interaction and to explain the selectivity of the most active compounds toward hMAO-B, molecular modeling studies were carried out on new, high resolution, hMAO-B crystallographic structures. For the only compound that also showed activity against hMAO-A as well as low selectivity, the molecular modeling study was also performed on the hMAO-A crystallographic structure. The docking technique provided new insight on the inhibition mechanism and the rational drug design of more potent/selective hMAO inhibitors based on the chalcone scaffold.
Synthesis and in vitro selective anti-Helicobacter pylori activity of pyrazoline derivatives
Chimenti,Bizzarri,Manna,Bolasco,Secci,Chimenti,Granese,Rivanera,Lilli,Scaltrito,Brenciaglia
, p. 603 - 607 (2007/10/03)
In order to develop new anti-Helicobacter pylori agents, a series of N1-substituted 3,5-diphenyl pyrazolines P1-P13 was prepared and evaluated for their antibacterial activity. All synthesized compounds showed little or no activity against different species of Gram-positive and Gram-negative bacteria of clinical relevance and against various strains of pathogenic fungi. The same derivatives exhibited a significant degree of activity against a range of H. pylori strains, including those resistant to the reference compound metronidazole. Among the prepared compounds those with an N1-acetyl group and a 4-methoxy substituent in the 5-phenyl ring showed the best activity against H. pylori metronidazole resistant strains in the 1-4 μg/mL MIC range.
Synthesis and Selective Inhibitory Activity of 1-Acetyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole Derivatives against Monoamine Oxidase
Chimenti, Franco,Bolasco, Adriana,Manna, Fedele,Secci, Daniela,Chimenti, Paola,Befani, Olivia,Turini, Paola,Giovannini, Valentina,Mondovì, Bruno,Cirilli, Roberto,La Torre, Francesco
, p. 2071 - 2074 (2007/10/03)
A novel series of 1-acetyl-3-(4-hydroxy- and 2,4-dihydroxyphenyl)-5-phenyl-4,5-dihydro-(1H)-pyrazole derivatives 1 - 12 have been synthesized and investigated for the ability to selectively inhibit the activity of the A and B isoforms of monoamine oxidase
Synthesis and activity of a new series of chalcones as aldose reductase inhibitors
Severi, Fabio,Benvenuti, Stefania,Costantino, Luca,Vampa, Gabriella,Melegari, Michele,Antolini, Luciano
, p. 859 - 866 (2007/10/03)
A new series of chalcone derivatives has been synthesized and tested in vitro in order to assess their ability to inhibit aldose reductase enzyme (ALR2) and their specificity towards the target enzyme with respect to other oxidoreductases, such as aldehyde reductase, sorbitol dehydrogenase, and glutathione reductase. All the compounds display affinity for ALR2. The X-ray crystal structure of 1-(2,4-dihydroxyphenyl)-3-(2-methoxyphenyl)propen-1-one was determined.
