Synthesis and Evaluation of 5 ‐(o‐Tolyl)‐1H‐tetrazole Derivatives as Potent Anticonvulsant Agents

A series of 5‐(o‐tolyl)‐1H‐tetrazole derivatives were synthesized and evaluated for their anticonvulsant activities. 1‐(2‐Methylbenzyl)‐5‐(o‐tolyl)‐1H‐tetrazole (3h) showed important anticonvulsant activity against the MES‐induced seizures, as well as lower neurotoxicity with an ED50 value of 12.7 mg/kg and a TD50 value of over 500 mg/kg after intraperitoneal injection into mice, providing 3h with a high protective index (TD50/ED50) of over 39.4. The achieved results prove that the distinctive compounds could be valuable as a model for future development, adaptation, and investigation to construct more active analogues. In a series of 5‐(o‐tolyl)‐1H‐tetrazole derivatives, 1‐(2‐methylbenzyl)‐5‐(o‐tolyl)‐1H‐tetrazole (3h) showed significant anticonvulsant activity against MES‐induced seizures and lower neurotoxicity after intraperitoneal injection into mice, providing 3h with a high protective index (TD50/ED50) of over 39.4. Some compounds could be valuable as a model to construct more active analogues.
Source: Archiv der Pharmazie - Category: Drugs & Pharmacology Authors: Tags: Full Paper Source Type: research