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Synthesis and anticonvulsant activities of 5-(2-Chlorophenyl)-7H-pyrido[4,3-f][1,2,4]triazolo[4,3-a][1,4]diazepines

✍ Scribed by Charles Y. Fiakpui; Oludotun A. Phillips; K. S. Keshava Murthy; Edward E. Knaus

Publisher
Journal of Heterocyclic Chemistry
Year
1999
Tongue
English
Weight
305 KB
Volume
36
Category
Article
ISSN
0022-152X

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✦ Synopsis

Abstract

A group of 5‐(2‐chlorophenyl)‐10‐(substituted)‐7__H__‐pyrido[4,3‐f][1,2,4]triazolo[4,3‐a][1,4]diazepines 7a‐c were synthesized by the acid catalyzed reaction of 5‐(2‐chlorophenyl)‐2‐hydrazino‐3__H__‐pyrido[3,4‐e]‐[1,4]diazepine (6) with either trimethyl orthoformate, triethyl orthoacetate or triethyl orthobenzoate, respectively. 5‐(2‐Chlorophenyl)‐7__H__‐pyrido[4,3‐f][1,2,4]triazolo[4,3‐a][1,4]diazepine (7a) and 5‐(2‐chlo‐rophenyl)‐10‐methyl‐7__H__‐pyrido[4,3‐f][1,2,4]triazolo[4,3‐a][1,4]diazepine (7b) exhibited good anticonvulsant activity in the subcutaneous metrazol anticonvulsant screen which serves as a model for absence (petit mal) epilepsy.

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## Abstract ^14^C‐Labelled (S)‐(+)‐6‐(2‐chlorophenyl)‐3‐cyclopropanecarbonyl‐8,11‐dimethyl‐2,3,4,5‐ tetrahydro‐8H‐pyrido[4′,3′:4,5]thieno[3,2‐f][1,2,4]triazolo[4,3‐a][1,4] diazepine (^14^C‐E6123), a platelet activating factor receptor antagonist for studying the pharmacokinetic profile of E6123, wa