A class of oral N-[(1S,3S)-1-methyl-1,2,3,4-tetrahydro-beta-carboline-3-carbonyl]- N '-(amino-acid-acyl)hydrazine: Discovery, synthesis, in vitro anti-platelet aggregation/in vivo anti-thrombotic evaluation and 3D QSAR analysis

作者：Yao, Kun; Zhao, Ming^*; Zhang, Xiaoyi; Wang, Yuji; Li, Li; Zheng, Meiqing; Peng, Shiqi

来源：European Journal of Medicinal Chemistry, 2011, 46(8): 3237-3249.

DOI：10.1016/j.ejmech.2011.04.037

• Tetrahydro-beta-carboline
• Anti-platelet aggregation
• Anti-thrombotic activity
• Conformation analysis
• 3D QSAR

The in vivo anti-thrombotic activities of amino acid modified tetrahydro-beta-carbolines depended upon the proximity of the side chain of the amino acid residue to the carboline-cycle. Based on this proximity the computerized screening of various tetrahydro-beta-carboline derivatives was performed and N-[(1S,3S)-1-methyl-1,2,3,4-tetrahydro-beta-carboline-3-carbonyl]-N'-(amino-acid-acyl)hydrazines were explored having large proximity. The in vivo anti-thrombotic assays explored that at a dose of 10 nmol/kg eighteen novel N-[(1S,3S)-1-methyl-1,2,3,4-tetrahydro-beta-carboline-3-carbonyl [-N'-(amino-acid-acyl)hydrazines were orally efficacious.

• 出版日期2011-8
• 单位首都医科大学