671207-58-2Relevant academic research and scientific papers
Asymmetric construction of quaternary α-nitro amides by palladium-catalyzed C(sp3)-H arylation
Kong, Wei-Xin,Xie, Shi-Jing,Cao, Chen-Yao-Zi,Zhang, Chao-Wei,Wang, Chuanyong,Duan, Wei-Liang
supporting information, p. 2292 - 2295 (2020/03/04)
Pd-Catalyzed enantioselective C(sp3)-H arylation of N-(o-Br-aryl) anilides has been disclosed, and quaternary α-nitro amides were constructed with up to 98% ee. The presence of the nitro group on the substrate enables the progress of the reaction and the ready transformation of the product to optically active quaternary amino acid derivatives.
Benzoazepine derivative as potent antagonists of the glycine binding site associated to the NMDA receptor
Di Fabio, Romano,Micheli, Fabrizio,Baraldi, Davide,Bertani, Barbara,Conti, Nadia,Dal Forno, Giovanna,Feriani, Aldo,Donati, Daniele,Marchioro, Carla,Messeri, Tommaso,Missio, Andrea,Pasquarello, Alessandra,Pentassuglia, Giorgio,Pizzi, Domenica A.,Provera, Stefano,Quaglia, Anna M.,Sabbatini, Fabio M.
, p. 723 - 738 (2007/10/03)
A series of benzoazepine derivatives, bearing suitable substituents at the C-3 position, was designed and evaluated by superimposition with the pharmacophore model of the glycine binding site. To fully explore the SAR of this class of compounds and to allow the preparation of new different compounds at the C-3 position, appropriate synthetic routes were set up. The benzoazepines were evaluated in terms of in vitro affinity using [ 3H]glycine binding assay and in vivo potency by inhibition of convulsions induced by N-methyl-D-aspartate (NMDA) in mice. This further analysis confirmed the preliminary results previously reported and that compound 27 is the most promising compound (Ki=32 nM, ED50=0.09 mg/kg, i.v.) in this series. Significant neuroprotective effect was observed after both pre- and post-ischaemia administration in the MCAo model. In particular, after post-ischaemia administration, it was found to be still effective when the administration was delayed up to 6 h after occlusion of the middle cerebral artery.
