77605-58-4Relevant academic research and scientific papers
Light-Driven Carboxylation of o-Alkylphenyl Ketones with CO2
Masuda, Yusuke,Ishida, Naoki,Murakami, Masahiro
, p. 14063 - 14066 (2015/11/25)
o-Alkylphenyl ketones undergo a C-C bond forming carboxylation reaction with CO2 simply upon irradiation with UV light or even solar light. The reaction presents a clean process exploiting light energy as the driving force for carboxylation of organic molecules with CO2.
1-aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: Novel AMPA receptor antagonists
Chimirri, Alba,De Sarro, Giovambattista,De Sarro, Angela,Gitto, Rosaria,Grasso, Silvana,Quartarone, Silvana,Zappalà, Maria,Giusti, Piero,Libri, Vincenzo,Constanti, Andrew,Chapman, Astrid G.
, p. 1258 - 1269 (2007/10/03)
Our previous publication (Eur. J. Pharmacol. 1995, 294, 411-422) reported preliminary chemical and biological studies of some 2,3- benzodiazepines, analogues of 1-(4-aminophenyl)-4-methyl-7,8- (methylenedioxy)-5H-2,3-benzodiazepine (1, GYKI 52466), which have been shown to possess significant anticonvulsant activity. This paper describes the synthesis of new 1-aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones and the evaluation of their anticonvulsant effects. The observed findings extend the structure-activity relationships previously suggested for this class of anticonvulsants. The seizures were evoked both by means of auditory stimulation in DBA/2 mice and by pentylenetetrazole or maximal electroshock in Swiss mice. 1-(4'-Aminophenyl)- (38) and 1-(3'-aminophenyl)-3,5-dihydro- 7,8-dimethoxy-4H-2,3-benzodiazepin-4-one (39), the most active compounds of the series, proved to be more potent than 1 in all tests employed. In particular, the ED50 values against tonus evoked by auditory stimulation were 12.6 μmol/kg for derivative 38, 18.3 μmol/kg for 39, and 25.3 μmol/kg for 1. Higher doses were necessary to block tonic extension induced both by maximal electroshock and by pentylenetetrazole. In addition these compounds exhibited anticonvulsant properties that were longer lasting than those of compound 1 and were less toxic. The novel 2,3-benzodiazepines were also investigated for a possible correlation between their anticonvulsant activities against convulsions induced by 2-amino-3-(3-hydroxy-5- methylisoxazol-4-yl)propionic acid (AMPA) and their affinities for benzodiazepine receptors (BZR). The 2,3-benzodiazepines did not affect the binding of [3H]flumazenil to BZR, and conversely, their anticonvulsant effects were not reversed by flumazenil. On the other hand the 2,3- benzodiazepines antagonized seizures induced by AMPA and aniracetam in agreement with an involvement of the AMPA receptor. In addition, both the derivative 38 and the compound 1 markedly reduced the AMPA receptor-mediated membrane currents in guinea-pig olfactory cortical neurons in vitro in a noncompetitive manner. The derivatives 25 and 38-40 failed to displace specific ligands from N-methyl-D-aspartate (NMDA), AMPA/kainate, or metabotropic glutamate receptors.
2-Benzopyran-3-ones Stabilised by Alkoxy Substituents
Bradshaw, David P.,Jones, David W.,Tideswell, John
, p. 169 - 173 (2007/10/02)
In contrast to the corresponding compounds lacking alkoxy substituents, the 2-benzopyran-3-ones 5, 6, 7 and 9 are stable and easily isolated.In contrast to the 6-methoxy derivative 7, the 7-methoxy isomer 8 cannot be isolated; the stabilising effect of th
2-(Arylmethyl)arylacetic Acids as Potential Antiinflammatory Agents
Brancaccio, Giovanni,Larizza, Angelo,Lettieri, Guglielmo,Monforte, Pietro
, p. 998 - 1000 (2007/10/02)
The title compounds 2 have been synthesized and tested for antiinflammatory activity.The synthetic method, consisting of the chemical sequence 3-aryl-1H-indenes (4) 2-(aroyl)arylacetic acids (5) 2, appears to be of value because of its simplicity
