Related Experiment Video
Updated: May 18, 2026

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
Design, Synthesis of 6-Substituted-pyrido[3,2-d]pyridazine Derivatives with Anticonvulsant Activity
Zheng-Qi Dong1, Xiao-Mei Liu, Cheng-Xi Wei
1Institute of Medicinal Plant Development,Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100193, China. weichengxi1224@yahoo.com.cn.
Abstract:
The aim of the present paper was to find new compounds with stronger anticonvulsant activity and lower neurotoxicity, a novel series of 6-substituted-pyrido[3,2-d]pyridazine derivatives was synthesized using furo[3,4-b]pyridine-5,7-dione as the starting material. Their anticonvulsant activities were evaluated by the maximal electroshock test (MES) and their neurotoxicity was measured by the rotarod test. The results of these tests demonstrated that N-m-chlorophenyl-[1,2,4]triazolo- [4,3-b]-pyrido[3,2-d]pyridazin-6-amine (3) was the most potent anticonvulsant, with ED50 value of 13.6 mg/kg and protective index (PI = TD50 / ED50) values of 7.2 in the MES test. Compound N-m-chlorophenyltetriazolo[5,1-b]-pyrido[3,2-d]pyridazin-6-amine (19), exhibited a little weaker activity than compound 3 in controlling the seizure induced by MES test at the dose of 15.9 mg/kg, but it possessed lower neurotoxicity with PI value of 13.4, which was safer than marketed drug carbamazepine.
Related Concept Videos
Nucleophilic Aromatic Substitution of Aryldiazonium Salts: Aromatic SN1
In the Sandmeyer reaction, for example, the diazonio group is replaced by a chloro, bromo, or cyano...
Diazonium Group Substitution with Halogens and Cyanide: Sandmeyer and Schiemann Reactions
Structure-Activity Relationships and Drug Design
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...
Diazonium Group Substitution: –OH and –H
Chemotherapy-Induced Nausea and Vomiting: Dopamine Receptor Antagonists
Phenothiazines, such as prochlorperazine...
Aryldiazonium Salts to Azo Dyes: Diazo Coupling

