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一类口服 N-[(1S,3S)-1-甲基-1,2,3,4-四氢-β-咔啉-3-羰基]-N'-(氨基酸酰基)酰肼：发现、合成、体外抗血小板聚集/体内抗血栓形成评价及 3D QSAR 分析。

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

机构信息

College of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, PR China.

出版信息

Eur J Med Chem. 2011 Aug;46(8):3237-49. doi: 10.1016/j.ejmech.2011.04.037. Epub 2011 Apr 29.

DOI:10.1016/j.ejmech.2011.04.037
PMID:21571404
Abstract

The in vivo anti-thrombotic activities of amino acid modified tetrahydro-β-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-β-carboline derivatives was performed and N-[(1S,3S)-1-methyl-1,2,3,4-tetrahydro-β-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-β-carboline-3-carbonyl]-N'-(amino-acid-acyl)hydrazines were orally efficacious.

摘要

氨基酸修饰的四氢-β-咔啉的体内抗血栓活性取决于氨基酸残基的侧链与咔啉环的接近程度。基于这种接近程度，对各种四氢-β-咔啉衍生物进行了计算机筛选，并探索了具有较大接近程度的 N-[(1S,3S)-1-甲基-1,2,3,4-四氢-β-咔啉-3-羰基]-N'-(氨基酸酰基)腙。体内抗血栓试验表明，在 10 nmol/kg 的剂量下，18 种新型 N-[(1S,3S)-1-甲基-1,2,3,4-四氢-β-咔啉-3-羰基]-N'-(氨基酸酰基)腙具有口服疗效。

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