68765-23-1Relevant academic research and scientific papers
Design, synthesis, and molecular docking study of benzothiazolotriazine derivatives for anticonvulsant potential
Firdaus, Jannat Ul,Habib, Anwar,Siddiqui, Nadeem,Alam, Ozair,Naim, Mohd. Javed,Partap, Sangh,Sahu, Meeta
, (2018)
A series of newer benzothiazolotriazine derivatives (4a–k) was designed, synthesized, and characterized as anticonvulsant agents against the two classically used MES and scPTZ animal models. The synthesized derivatives were tested in vivo in both the animal models, followed by a neurotoxicity study by the rotarod method. Compound 4e, 8-chloro-4-(2-chlorocyclohexa-1,5-dien-1-yl)-2-((4-methoxybenzyl)thio)-10aH-benzo[4,5]thiazolo[3,2a][1,3,5]triazine was found most promising among the series in both the animal models, with no neurotoxicity. From this it may be confirmed that the presence of a methoxy (OCH3) group at the lipophilic aryl ring was showing high anticonvulsant potency. In the molecular modeling study, compound 4e (docking score = ?8.70) showed important hydrogen bond interaction with the amino acids LYS 329, SER 137, GLY 136 and π–π interactions with PHE 189 at the active site of GABA-AT. These derivatives can be further explored for the development of newer/novel anticonvulsant agents.
N-{[(6-Substituted-1,3-benzothiazole-2-yl)amino]carbonothioyl}-2/4-substituted benzamides: Synthesis and pharmacological evaluation
Rana, Arpana,Siddiqui, Nadeem,Khan, Suroor A.,Ehtaishamul Haque, Syed,Bhat, Mashooq A.
, p. 1114 - 1122 (2008/09/21)
A series of 1,3-benzothiazol-2-yl benzamides (11-30) were prepared in satisfactory yield and evaluated for their anticonvulsant, neurotoxicity, CNS depressant study and other toxicity studies. All the synthesized compounds were in good agreement with elemental and spectral data. Majority of the compounds were active in MES and scPTZ screen and showed the decrease in the immobility time. None of the compounds had shown neurotoxicity or liver toxicity.
