154407-02-0Relevant academic research and scientific papers
Synthesis, antimycobacterial evaluation and pharmacophore modeling of analogues of the natural product formononetin
Mutai, Peggoty,Pavadai, Elumalai,Wiid, Ian,Ngwane, Andile,Baker, Bienyameen,Chibale, Kelly
, p. 2510 - 2513 (2015/06/02)
Abstract The synthesis and antimycobacterial activity of formononetin analogues is hereby reported. Formononetin and its analogue 11E showed 88% and 95% growth inhibition, respectively, against the H37Rv strain of Mycobacterium tuberculosis. Pharmacophore modeling studies indicated that the presence of a hydroxyl group in formononetin and its analogues, is crucial for maintaining activity.
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 of some pyrazole derivatives and preliminary investigation of their affinity binding to P-glycoprotein
Manna, Fedele,Chimenti, Franco,Fioravanti, Rossella,Bolasco, Adriana,Secci, Daniela,Chimenti, Paola,Ferlini, Cristiano,Scambia, Giovanni
, p. 4632 - 4635 (2007/10/03)
A series of substituted pyrazolines were synthesized and evaluated for their anticancer activity and for their ability to inhibit P-glycoprotein- mediated multidrug resistance by direct binding to a purified protein domain containing an ATP-binding site and a modulator interacting region. Compounds 2a and e have been found to bind to P-glycoprotein with greater affinity.
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.
