Zhi-Gang Sun

Bio: Zhi-Gang Sun is an academic researcher from Yanbian University. The author has contributed to research in topics: Phthalazine & Primary (chemistry). The author has an hindex of 3, co-authored 5 publications receiving 26 citations.

Synthesis and primary anticonvulsant activity evaluation of 6-alkyoxyl-tetrazolo[5,1-a]phthalazine derivatives

Abstract: A new series of 6-alkyoxyl-tetrazolo[5,l- a ] phthalazine derivatives (4 a-4 o) were synthesized as potential anticonvulsant agents. Anticonvulsant activity was evaluated by the maximal electroshock (MES) test. Neurotoxicity was evaluated by the rotarod neurotoxicity test. The pharmacological results showed that 6-(4-chlorophenyoxyl) - tetrazolo [5,1- a ] phthalazine (4 m) was the most potent agent, with a median effective dose (ED 50 ) of 6.8 mg/kg and a median neurotoxic dose (TD 50 ) of 456.4 mg/kg. The protective index (PI = TD50/ED50) for compound 4 m was 67.1, which was significantly higher than that for the reference drug carbamazepine (PI = 6.4).

Synthesis and Antiinflammatory Activity Evaluation of Some Novel 6-Alkoxy (Phenoxy)-[1,2,4]triazolo[3,4-a]phthalazine-3-amine Derivatives.

Abstract: Title compounds (VI) (21 examples) are synthesized starting from phthalic anhydride (I) using the cyclization reaction of phthalazinylhydrazine (II) with cyanogen bromide as the key step.

Synthesis and Primary Anticonvulsant Activity Evaluation of 6-Alkyoxyl-tetrazolo[5,1-a]phthalazine Derivatives.

Abstract: Title compounds (V), synthesized starting from dichlorophthalazine (I), are found to exhibit anticonvulsant activity.

Tetrazolium Compounds: Synthesis and Applications in Medicine

Abstract: Tetrazoles represent a class of five-membered heterocyclic compounds with polynitrogen electron-rich planar structural features. This special structure makes tetrazole derivatives useful drugs, explosives, and other functional materials with a wide range of applications in many fields of medicine, agriculture, material science, etc. Based on our research works on azoles and other references in recent years, this review covers reported work on the synthesis and biological activities of tetrazole derivatives.

Recent developments on triazole nucleus in anticonvulsant compounds: a review

Abstract: Epilepsy is one of the common diseases seriously threatening life and health of human. More than 50 million people are suffering from this condition and anticonvulsant agents are the main treatment. However, side effects and intolerance, and a lack of efficacy limit the application of the current anticonvulsant agents. The search for new anticonvulsant agents with higher efficacy and lower toxicity continues to be the focus and task in medicinal chemistry. Numbers of triazole derivatives as clinical drugs or candidates have been frequently employed for the treatment of various types of diseases, which have proved the importance of this heterocyclic nucleus in drug design and discovery. Recently many endeavours were made to involve the triazole into the anticonvulsants design, which have brought lots of active compounds. This work is an attempt to systematically review the research of triazole derivatives in the design and development of anticonvulsant agents during the past two decades.

Additive-Driven Rhodium-Catalyzed [4+1]/[4+2] Annulations of N-Arylphthalazine-1,4-dione with α-Diazo Carbonyl Compounds

Abstract: A Rh(III)-catalyzed strategy involving the [4+1] annulation of 2-arylphthalazine-1,4-diones with α-diazo carbonyl compounds was developed, accessing a series of unprecedented hydroxy-dihydroindazolo-fused phthalazines in good to excellent yields. By varying the additive, phthalazino-fused cinnolines were synthesized under Rh-catalyzed conditions via [4+2] annulation between the same starting materials. Notably, such two strategies showed a good functional group tolerance and high atom efficiency.