91377-59-2Relevant academic research and scientific papers
Design, synthesis and protection against pentylenetetrazole-induced seizure of N-aryl derivatives of the phthalimide pharmacophore
Davood, Asghar,Nematollahi, Alireza,Shafaroodi, Hamed,Shirazi, Mehrshad,Amini, Mohsen,Iman, Maryam
, p. 953 - 963,11 (2012)
A series of compounds including N-aryl substituents of phthalimide and 4-nitrophthalimide were synthesized and evaluated for their anticonvulsant properties. The in vivo screening data suggest that all the analogs have the ability to protect against pentylenetetrazole-induced seizures. These compounds exerted their maximal effects 30 min after administration. The most potent compound in both, tonic and clonic seizure was 1-naphthyl derivative (comp. 6), which was more active than the reference drug known as Phenytoin. Using an open pore model of the Na channel, these anticonvulsants were docked in the active site and examined in relation to the residues identified by mutagenesis as important for their binding energies. Docking studies revealed that all compounds (1-13) interacted mainly with residues II-S6 of NaV1.2 by making hydrogen bonds and additional hydrophobic interactions with domain I and II in the channel's inner pore.
Synthesis and anticancer evaluation of novel isoxazole/pyrazole derivatives
Abu Bakr, Sherifa M.,Abd El-Karim, Somaia S.,Said, Medhat M.,Youns, Mahmoud M.
, p. 1387 - 1399 (2016/04/26)
The key intermediate 3-amino-5-methylisoxazole (1) was allowed to react with phthalic anhydride and/or maleic anhydride under different conditions to produce different isoxazole products. Schiff bases 9a-c obtained via the reaction of 1 with different aldehydes were condensed with thioglycolic acid to afford the corresponding thiazolidin-4-one derivatives 10a, b. Furthermore, condensation of the Schiff bases 9a, c with various secondary amines produced the corresponding 5-substituted pyrazole derivatives 11a-d, respectively. The anticancer activity of some of the newly synthesized compounds was evaluated against Panc-1 and Caco-2 cell lines using doxorubicin as a standard drug. Most of the tested derivatives exhibited high cytotoxic potency against Panc-1 carcinoma cell lines, but moderate to weak activity was obtained against Caco-2 cell lines.
