33329-27-0Relevant articles and documents
Quinoline derivative, and preparation method and uses thereof
-
Paragraph 0310; 0312-0313, (2018/11/04)
The invention relates to a quinoline derivative, and a composition including the derivative, and also relates to a preparation method of the derivative, and uses of the derivative in the prevention ortreatment of harmful fungi and the killing of pests.
Synthesis and?biological activity of?6H-isoindolo[2,1-a]indol-6-ones, analogues of?batracylin, and?related compounds
Guillaumel, Jean,Léonce, Stéphane,Pierré, Alain,Renard, Pierre,Pfeiffer, Bruno,Arimondo, Paola B.,Monneret, Claude
, p. 379 - 386 (2007/10/03)
Closely related to batracylin, 6H-isoindolo[2,1-a]indol-6-ones including 2-nitro- 13a, 2-amino- 14, and 2-diethylaminopropionamide derivative 16 as well as D-ring substituted 13b, 13c or A-ring substituted 13d and 20 analogues, were synthesised and evaluated against L1210 leukaemia. Subsequent treatment of 13b and 13c with N,N-diethylethylenediamine at 180?°C, led to compounds 17a and 17b arising from an unexpected opening of the pyrrolidinone ring and amidification of the keto group. Under the same conditions, the dichloro derivative 13d led to the monoalkyl compound 20 which was the most cytotoxic of the series.
Synthesis and anticonvulsant and neurotoxic properties of substituted N- phenyl derivatives of the phthalimide pharmacophore
Vamecq, Joseph,Bac, Pierre,Herrenknecht, Christine,Maurois, Pierre,Delcourt, Philippe,Stables, James P.
, p. 1311 - 1319 (2007/10/03)
A series of compounds including 4-amino (1), 3-amino (2), 4-nitro (3), 2-methyl-3-amino (4), 2-methyl-3-nitro (5), 2-methyl-4-amino (6), 2-methyl-4- nitro (7), 2-methyl-5-amino (8), 2-methyl-5-nitro (9), 2-methyl-6-amino (10), 2-methyl-6-mitro (11), 2,6-dimethyl (12), 2-methyl-3-carboxy (13), 2- methoxycarbonyl (14), 2-methyl-4-methoxy (15), 2,4-dimethoxy (16), 2-chloro- 4-amino (17), and 2-chloro-4-nitro (18) N-phenyl substituents of phthalimide were evaluated along with N-[3-methyl-(2-pyridinyl)]phthalimide (19), N-(3- amino-2-methylphenyl)succinimide (20), and phenytoin for anticonvulsant and neurotoxic properties. Initial screening in the intraperitoneal (ip) maximal electroshock-induced seizure (MES) test and the subcutaneous pentylenetetrazol-induced seizure (scPtz) test in mice led to the selection of 1, 2, 4, 10, 12, 17, and 19 for oral MES evaluation in rats. The resultant ED50 values for 4, 10, 17, and phenytoin were 8.0, 28.3, 5.7 and 29.8 mg/kg, respectively. In the batrachotoxin affinity assay, IC50 values for 17 and phenytoin were 0.15 and 0.93 μM, respectively, and in the recently validated magnesium deficiency-dependent audiogenic seizure test, ED50 values of 5.2 and 23 mg/kg were obtained for 17 and phenytoin, respectively. Electrophysiology studies on compound 17 point out its ability to (i) potentiate GABA-evoked current responses with a failure to directly activate the GABAA receptor and (ii) to affect, at 100 μM excitatory non NMDA, but not NMDA, receptors with a 25% block of kainate-evoked response. Electrophysiology measurements on voltagegated sodium channels in N1E-115 neuroblastoma cells confirm voltage-dependent block of these channels by compound 17. In view of its interaction with multiple ion channels, one would predict that compound 17 might be active in a wide range of seizure models.
2-[(Aminophenyl and amidophenyl)amino]-1-azacycloalkanes having antidiarrheal activity
-
, (2008/06/13)
This invention relates to the novel use of certain aromatic substituted amidines as antidiarrheals.