BIOMAT Database Logo BIOMAT Database Logo

Synthesis and anticonvulsant activity of 1-formamide-triazolo[4,3-a]quinoline derivatives. 2010

Cheng-Xi Wei, and Xian-Qing Deng, and Kyu-Yun Chai, and Zhi-Gang Sun, and Zhe-Shan Quan
Institute of Neurosurgery, Inner Mongolia University for Nationalities, Tongliao, China.

Using 6-hydroxy-3,4-dihydro-2(1H)-quinolone as the starting material, a series of 1-formamide-triazolo[4, 3-a]quinoline derivatives (6a-6n) was synthesized, the anticonvulsant effect and neurotoxicity of the compounds was calculated with maximal electroshock test and rotarod tests with intraperitoneally injected in KunMing mice. The results demonstrated that compound 7-(hexyloxy)-4,5-dihydro-[1,2,4] triazolo[4,3-a]quinoline-1-carboxamide (6d) was the most active one and also had the lowest toxicity. In the anti-maximal electroshock potency test, it showed median effective dose (ED(50)) of 30.1 mg/kg, median toxicity dose (TD(50)) of 286 mg/kg, and the protective index of 9.5 which is greater than the reference drug carbamazepine with the protective index value of 6.0.

UI MeSH Term Description Entries
D008297 Male Males
D008815 Mice, Inbred Strains Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations, or by parent x offspring matings carried out with certain restrictions. All animals within an inbred strain trace back to a common ancestor in the twentieth generation. Inbred Mouse Strains,Inbred Strain of Mice,Inbred Strain of Mouse,Inbred Strains of Mice,Mouse, Inbred Strain,Inbred Mouse Strain,Mouse Inbred Strain,Mouse Inbred Strains,Mouse Strain, Inbred,Mouse Strains, Inbred,Strain, Inbred Mouse,Strains, Inbred Mouse
D011804 Quinolines
D002220 Carbamazepine A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties. Amizepine,Carbamazepine Acetate,Carbamazepine Anhydrous,Carbamazepine Dihydrate,Carbamazepine Hydrochloride,Carbamazepine L-Tartrate (4:1),Carbamazepine Phosphate,Carbamazepine Sulfate (2:1),Carbazepin,Epitol,Finlepsin,Neurotol,Tegretol
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D004353 Drug Evaluation, Preclinical Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications. Drug Screening,Evaluation Studies, Drug, Pre-Clinical,Drug Evaluation Studies, Preclinical,Drug Evaluations, Preclinical,Evaluation Studies, Drug, Preclinical,Evaluation, Preclinical Drug,Evaluations, Preclinical Drug,Medicinal Plants Testing, Preclinical,Preclinical Drug Evaluation,Preclinical Drug Evaluations,Drug Screenings,Screening, Drug,Screenings, Drug
D005260 Female Females
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000927 Anticonvulsants Drugs used to prevent SEIZURES or reduce their severity. Anticonvulsant,Anticonvulsant Drug,Anticonvulsive Agent,Anticonvulsive Drug,Antiepileptic,Antiepileptic Agent,Antiepileptic Agents,Antiepileptic Drug,Anticonvulsant Drugs,Anticonvulsive Agents,Anticonvulsive Drugs,Antiepileptic Drugs,Antiepileptics,Agent, Anticonvulsive,Agent, Antiepileptic,Agents, Anticonvulsive,Agents, Antiepileptic,Drug, Anticonvulsant,Drug, Anticonvulsive,Drug, Antiepileptic,Drugs, Anticonvulsant,Drugs, Anticonvulsive,Drugs, Antiepileptic
D015394 Molecular Structure The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds. Structure, Molecular,Molecular Structures,Structures, Molecular

Related Publications

Cheng-Xi Wei, and Xian-Qing Deng, and Kyu-Yun Chai, and Zhi-Gang Sun, and Zhe-Shan Quan
Design and synthesis of 5-alkoxy-[1,2,4]triazolo[4,3-a]quinoline derivatives with anticonvulsant activity.
March 2009, European journal of medicinal chemistry,
Cheng-Xi Wei, and Xian-Qing Deng, and Kyu-Yun Chai, and Zhi-Gang Sun, and Zhe-Shan Quan
Synthesis and anticonvulsant activity of 1-substituted-7-benzyloxy-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline.
July 2005, Biological & pharmaceutical bulletin,
Cheng-Xi Wei, and Xian-Qing Deng, and Kyu-Yun Chai, and Zhi-Gang Sun, and Zhe-Shan Quan
Synthesis and anticonvulsant activity of 8-alkoxy-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-1-one derivatives.
April 2011, European journal of medicinal chemistry,
Cheng-Xi Wei, and Xian-Qing Deng, and Kyu-Yun Chai, and Zhi-Gang Sun, and Zhe-Shan Quan
Synthesis and studies on the anticonvulsant activity of 5-alkoxy-[1,2,4]triazolo[4,3-a]pyridine derivatives.
August 2012, Arzneimittel-Forschung,
Cheng-Xi Wei, and Xian-Qing Deng, and Kyu-Yun Chai, and Zhi-Gang Sun, and Zhe-Shan Quan
Design, synthesis and anticonvulsant activity evaluation of 7-substituted-[1,2,4]-triazolo[4,3-f]pyrimidine derivatives.
November 2012, Medicinal chemistry (Shariqah (United Arab Emirates)),
Cheng-Xi Wei, and Xian-Qing Deng, and Kyu-Yun Chai, and Zhi-Gang Sun, and Zhe-Shan Quan
Synthesis and anticonvulsant activity of 5-phenyl-[1,2,4]-triazolo[4,3-a]quinolines.
December 2008, Archiv der Pharmazie,
Cheng-Xi Wei, and Xian-Qing Deng, and Kyu-Yun Chai, and Zhi-Gang Sun, and Zhe-Shan Quan
Synthesis and Antibacterial Activity of Novel Triazolo[4,3-a]pyrazine Derivatives.
November 2023, Molecules (Basel, Switzerland),
Cheng-Xi Wei, and Xian-Qing Deng, and Kyu-Yun Chai, and Zhi-Gang Sun, and Zhe-Shan Quan
8-Amino-3-benzyl-1,2,4-triazolo[4,3-a]pyrazines. Synthesis and anticonvulsant activity.
September 1995, Journal of medicinal chemistry,
Cheng-Xi Wei, and Xian-Qing Deng, and Kyu-Yun Chai, and Zhi-Gang Sun, and Zhe-Shan Quan
Synthesis and Anticonvulsant Activity Evaluation of 4-Phenyl-[1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one and Its Derivatives.
August 2015, Archiv der Pharmazie,
Cheng-Xi Wei, and Xian-Qing Deng, and Kyu-Yun Chai, and Zhi-Gang Sun, and Zhe-Shan Quan
Synthesis and anticonvulsant activity of 7-alkoxyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines.
November 2005, Bioorganic & medicinal chemistry letters,
Copied contents to your clipboard!