Synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing a cleavable moiety with anti-platelet activity was written by Yang, Xiao-Zhi;Yang, Wen-Hui;Xu, Yun-Gen;Diao, Xiao-Juan;He, Guang-Wei;Gong, Guo-Qing. And the article was included in European Journal of Medicinal Chemistry in 2012.Formula: C8H12N2O This article mentions the following:
A novel series of prodrugs I(R = tBu, hexyl, pentyl, iPr, Et, Bn, Me) consisting of dabigatran and 2-hydroxymethyl-3,5,6-trimethylpyrazine (HTMP) were synthesized. The pharmacol. results show that all of them possess the effect of anti-platelet aggregation induced by thrombin in vitro. Moreover, one of those compounds, I(R = hexyl) (ED50 = 2.1 ± 1.3 mg/kg) shows more potent activity for inhibiting thrombosis in vivo than that of dabigatran etexilate (ED50 = 4.4 ± 2.2 mg/kg). In the experiment, the researchers used many compounds, for example, (3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3Formula: C8H12N2O).
(3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3) belongs to pyrazine derivatives. Pyrazine derivatives have antitumor, antibiotic, anticonvulsant, antituberculous and diuretic effects as well as kinase, enzymatic and potent tubulin and FtsZ polymerization inhibitory activities. A number of pyrazine-based derivatives were used as dyes or fluorescent probes.Formula: C8H12N2O