On February 29, 2020, Shafie, Arefeh; Mohammadi-Khanaposhtani, Maryam; Asadi, Mehdi; Rahimi, Nastaran; Ranjbar, Parviz Rashidi; Ghasemi, Jahan B.; Larijani, Bagher; Mahdavi, Mohammad; Shafaroodi, Hamed; Dehpour, Ahmad Reza published an article.Synthetic Route of 89-77-0 The title of the article was Novel fused 1,2,3-triazolo-benzodiazepine derivatives as potent anticonvulsant agents: design, synthesis, in vivo, and in silico evaluations. And the article contained the following:
A novel series of 1,2,3-triazolo-benzodiazepine derivatives 6a-o has been synthesized and evaluated in vivo for their anticonvulsant activities using by pentylenetetrazole (PTZ)- and maximal electroshock (MES)-induced seizures in mice. The synthetic approach started with diazotizing 2-aminobenzoic acids 1 to produce 2-azidobenzoic acids 2. Next, reaction of the latter compounds with propargylamine 3, benzaldehyde 4, and isocyanides 5 led to the formation of the title compounds 6a-o, in good yields. All the synthesized compounds exhibited high anticonvulsant activity in the PTZ test, comparable to or better than the standard drug diazepam. Among the tested compounds, N-(tert-butyl)-2-(9-chloro-6-oxo-4H-[1,2,3]triazolo[1,5-a][1,4]benzodiazepin-5(6H)-yl)-2-(3-bromophenyl)acetamide 6h was the most potent compound in this assay. Moreover, compounds 6i and 6k showed excellent activity in MES test. Loss of the anticonvulsant effect of compound 6h in the presence of flumazenil in the PTZ test and appropriate interaction of this compound in the active site of benzodiazepine (BZD)-binding site of GABAA receptor confirm involvement of BZD receptors in the anticonvulsant activity of compound 6h. The experimental process involved the reaction of 2-Amino-4-chlorobenzoic acid(cas: 89-77-0).Synthetic Route of 89-77-0
The Article related to triazolo benzodiazepine anticonvulsant agent seizure, 1,2,3-triazolo-benzodiazepine, anticonvulsant, docking study, seizure, Pharmacology: Effects Of Antimicrobials and Parasiticides and other aspects.Synthetic Route of 89-77-0
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