64594-44-1Relevant articles and documents
Synthesis and anticonvulsant activity of some 4-nitro-N-phenylbenzamides
Bailleux, V.,Vallee, L.,Nuyts, J. P.,Hamoir, G.,Poupaert, J. H.,et al.
, p. 439 - 444 (1995)
A short series of 4-nitro-N-phenylbenzamides was synthesized and evaluated for anticonvulsant properties and neurotoxicity.In mice dosed intraperitoneally, three of the four 4-nitro-N-phenylbenzamides were efficient in the maximal electroshock-induced sei
Five-membered heteroaromatic ring fused-pyrimidine derivatives: Design, synthesis, and hedgehog signaling pathway inhibition study
Zhang, Liandi,Xin, Minhang,Shen, Han,Wen, Jun,Tang, Feng,Tu, Chongxing,Zhao, Xinge,Wei, Ping
supporting information, p. 3486 - 3492 (2014/07/22)
A series of novel five-membered heteroaromatic ring fused-pyrimidine derivatives including purines, pyrrolo[2,3-d]pyrimidines, pyrrolo[3,2-d] pyrimidines, thieno[2,3-d]pyrimidines, thieno[3,2-d]pyrimidines and furo[3,2-d]pyrimidines have been identified to be potent inhibitors of hedgehog signaling pathway. The synthesis and SAR of these compounds are described. Among this new series of hedgehog signaling pathway inhibitors, most compounds exhibited significant inhibitory activity compared to vismodegib, indicating that the five-membered heteroaromatic ring fused-pyrimidines stand out as encouraging scaffolds among the currently reported structural skeletons for hedgehog signaling pathway inhibitors, deserving more exploration and further investigation.
Design, anticonvulsive and neurotoxic properties of retrobenzamides / N- (nitrophenyl)benzamides and N-(aminophenyl)benzamides
Bourhim, Mustapha,Poupaert, Jacques H.,Stables, James P.,Vallee, Louis,Vamecq, Joseph
, p. 81 - 87 (2007/10/03)
Design, anticonvulsant properties in maximal electroshock-reduced seizures [MES] and seizures reduced by subcutaneous administration of pentetrazole (scPtz), and neurotoxicity of retrobenzamides (N- (nitrophenyl)benzamides and N-(aminophenyl) benzamides are reported. These data are further compared with those on carbamazepine, phenytoin, ameltolide and other reference compounds. Studies on retrobenzamides in mice dosed intraperitoneally point out a good anticonvulsant potential in the MES test for the amino derivatives (N-(aminophenyl)benzamides) and moderate activity for corresponding 'nitro' derivatives. In rats dosed orally, aminoretrobenzamides were, however, less active in the MES test than in mice dosed intraperitoneally. Differences between experimental animal species and administration routes lead to hypothesize rapid metabolization of compounds, reduced intestinal resorption and increased removal from body. The presence of a methyl substitution on the N-phenyl moiety of aminoretrobenzamides attenuated these discrepancies between mice and rats. Present results indicate that pharmacological values - including the dose offering anticonvulsant protection in 50 % of tested animals (ED50) and protective indices - obtained on some retrobenzamides may compete with phenytoin and carbamazepine values. By contrast with phenytoin, some retrobenzamides further exhibit activity in the scPtz test.
