945650-85-1Relevant academic research and scientific papers
A class of 3 S -2-aminoacyltetrahydro-β-carboline-3-carboxylic acids: Their facile synthesis, inhibition for platelet activation, and high in vivo anti-thrombotic potency
Liu, Jiawang,Jiang, Xueyun,Zhao, Ming,Zhang, Xiaoyi,Zheng, Meiqing,Peng, Li,Peng, Shiqi
experimental part, p. 3106 - 3116 (2010/09/05)
3S-Tetrahydro-β-carboline-3-carboxylic acid (TCCA) effectively inhibits ADP-induced platelet activation. This paper used TCCA as a lead, modified its 2-position with amino acids, and provided 20 novel 3S-2-aminoacyl-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acids (5a-t). With the in vitro assay, it was demonstrated that this modification diminished the IC50 values from 701 nM of TCCA to 10 nM of 5a-t. With the in vivo assay, it was demonstrated that this modification reduced the efficacious dose from 5.0 μmol/kg of TCCA to 0.1 μmol/kg of 5a-t. Comparing the Cerius2 based conformation of them with that of their analogues, the 3-position modified TCCA, it was suggested that the comparatively unfolded conformation was one of the important factors of enhancing the in vivo antithrombotic potency.
