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Chun-Bo Zhang

Bio: Chun-Bo Zhang is an academic researcher from Yanbian University. The author has contributed to research in topics: Quinazoline. The author has an hindex of 2, co-authored 2 publications receiving 24 citations.
Topics: Quinazoline

Papers
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Journal ArticleDOI
TL;DR: A series of novel 6-alkyoxyl [1,2,4]triazolo[1,5-a]quinazoline derivatives were synthesized in this article, and the anticonvulsant activity of all the target compounds 4a-4s, characterized by IR, 1H-NMR and MS, were evaluated using Maximal electroshock test.
Abstract: A series of novel 6-alkyoxyl[1,2,4]triazolo[1,5-a]quinazoline derivatives were synthesized in this study. The anticonvulsant activity of all the target compounds 4a–4s, characterized by IR, 1H-NMR and MS, were evaluated using Maximal electroshock test. The pharmacological results showed that some of the compounds displayed positive anticonvulsant activity. Among them, 6-(benzyloxy)-[1,2,4]triazolo[1,5-a]quinazoline (4a) was the most active compound with an ED50 value of 78.9 mg/kg and a PI value of 9.0.

16 citations


Cited by
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Journal ArticleDOI
TL;DR: 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.
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.

79 citations

Journal ArticleDOI
TL;DR: In this paper, Fourier transform infrared (FT-IR) spectroscopy in the region 400-4000 cm−1, proton and carbon-13 NMR chemical shifts and UV-Vis.

21 citations

Journal ArticleDOI
TL;DR: Quantitative assessment of the compounds after intraperitoneal administration in mice showed that the most active compound was 5-[3-(trifluoromethyl)phenoxy]thieno[1,2,4]triazolo[4,3-c]pyrimidine (5o), which was more effective in the MES and scPTZ tests than the well-known anticonvulsant drugs carbamazepine and ethosuximide.
Abstract: This work concerns the design and synthesis of novel, substituted 5-alkoxythieno[2,3-e][1,2,4]triazolo[4,3-c]pyrimidine derivatives 5a–p prepared from 3-amino-2-thiophenecarboxylic acid methyl ester. The final compounds were screened for their in vivo anticonvulsant activity using maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) tests. Neurotoxicity (NT) was tested using a rotarod test. The structure-anticonvulsant activity relationship analysis revealed that the most effective structural motif involves a substituted phenol, especially when substituted with a single chlorine, fluorine or trifluoromethyl group (at the meta-position), or two chlorine atoms. These molecules possessed high activity according to the MES and scPTZ models. Quantitative assessment of the compounds after intraperitoneal administration in mice showed that the most active compound was 5-[3-(trifluoromethyl)phenoxy]thieno[2,3-e] [1,2,4]triazolo[4,3-c]pyrimidine (5o) with ED50 values of 11.5 mg/kg (MES) and 58.9 mg/kg (scPTZ). Furthermore, compound 5o was more effective in the MES and scPTZ tests than the well-known anticonvulsant drugs carbamazepine and ethosuximide.

17 citations

Journal ArticleDOI
TL;DR: Aromatic α-aminoazaheterocycles are the focus of significant investigations and exploration by researchers owing to their key role in diverse biological and physiological processes as mentioned in this paper, and therefore, the synthesis of a structurally diverse range of their derivatives through simple and convenient methods represents a vital field of synthetic organic chemistry.
Abstract: Aromatic α-aminoazaheterocycles are the focus of significant investigations and exploration by researchers owing to their key role in diverse biological and physiological processes. The existence of their derivatives in numerous drugs and alkaloids is due to their heterocyclic nitrogenous nature. Therefore, the synthesis of a structurally diverse range of their derivatives through simple and convenient methods represents a vital field of synthetic organic chemistry. Multicomponent reactions (MCRs) provide a platform to introduce desirable structure diversity and complexity into a molecule in a single operation with a significant reduction in the use of harmful organic waste, and hence have attracted particular attention as an excellent tool to access these derivatives. This review covers the advances made from 2010 to the beginning of 2020 in terms of the utilization of α-aminoazaheterocycles as synthetic precursors in MCRs.

14 citations