Design, synthesis and biological evaluation of thrombin inhibitors with 1,2,3,4-tetrahydrobenzo[4,5]imidazo[1,2-a]pyrazine nucleus was written by Chen, Dongxing;Shi, Jinyu;Chen, Qiufang;Zhang, Rui;Gong, Guoqing;Xu, Yungen;Zhu, Qihua. And the article was included in Gaodeng Xuexiao Huaxue Xuebao in 2017.HPLC of Formula: 75907-74-3 This article mentions the following:
Compound 1, a new thrombin inhibitor with 1,2,3,4-tetrahydrobenzo[4,5]imidazo[1,2-a]pyrazine nucleus, was selected as lead compound, and fourteen carbamate derivatives derivatives were designed and prepared Furthermore, a twin drug (11) was synthesized by coupling compound 1 with 2-hydroxymethyl-3,5,6-trimethylpyrazine (HTMP). The structures of all the target compounds were confirmed by 1H-NMR, 13C-NMR and HRMS. Preliminary biol. activity test results indicated that all of the tested compounds exhibited a certain degree of inhibitory effect on thrombin-induced platelet aggregation, among which compound 4b [IC50 = (0.11鍗?.08) 娓璵ol/L] showed better anti-platelet aggregation activity than dabigatran etexilate [IC50 = (0.60鍗?.05) 娓璵ol/L]. The in vitro exptl. results in rat venous thrombosis model demonstrated compound 4b could significantly reduce thrombosis in a dose-response manner. Compound 11, which showed weak inhibitory effect on thrombin-induced platelet aggregation, also displayed comparable inhibitory effect on rat venous thrombosis with dabigatran etexilate. The study pointed out that the enhanced potency of compound 11 may be the synergetic effect on HTMP and compound 1 which were generated by hydrolysis in vivo. In the experiment, the researchers used many compounds, for example, (3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3HPLC of Formula: 75907-74-3).
(3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3) belongs to pyrazine derivatives. Pyrazine is an N-heterocyclic moiety, and it can be easily prepared from ethylenediamine and 1,2-diketone, 浼?hydroxyketone, 浼?methyl ketone. A number of pyrazine-based derivatives were used as dyes or fluorescent probes.HPLC of Formula: 75907-74-3