36467-52-4Relevant articles and documents
Method for preparing mosapride intermediate
-
Paragraph 0006; 0035-0038, (2019/08/30)
The invention provides a method for preparing a mosapride intermediate, and concretely relates to a method for preparing a key mosapride intermediate 2-ethoxy-4-amino-chlorobenzoic acid. The method ischaracterized in that the intermediate is prepared from sodium 4-aminosalicylate by four steps of N-carbethoxyphthalimide acylation, ethyl bromide bisethylation, N-chlorosuccinimide chlorination andalcoholic hydrazine hydrate solution deprotection and hydrolysis. The method which improves the synthesis process of the intermediate greatly improves the yield of the intermediate, shortens the reaction time and effectively reduces the production cost.
Docking, synthesis, and pharmacological evaluation of isoindoline derivatives as anticonvulsant agents
Davood, Asghar,Amini, Mohsen,Azimidoost, Leila,Rahmatpour, Somaieh,Nikbakht, Ali,Iman, Maryam,Shafaroodi, Hamed,Ansari, Abdollah
, p. 3177 - 3184 (2013/07/19)
Eleven analogs of N-arylisoindoline pharmacophore were synthesized and evaluated for their anticonvulsant activities. The in vivo screening data acquired indicate that all the analogs have the ability to protect against pentylenetetrazole-induced seizure. Compounds 2, 6, and 11 elevated clonic seizure thresholds at 30 min which were more active than reference drug phenytoin, and compounds 2, 7, and 11 showed marked anticonvulsant activity on tonic seizure. The most potent compounds were 2 and 11 which had comparative activity to the phenytoin. Using a model of the open pore of the Na channel, we have docked all compounds. Docking studies have revealed that these compounds interacted mainly with residues II-S6 of NaV1.2 by making hydrogen bonds and have additional hydrophobic interactions with other domains in the channel's inner pore.
