The design and synthesis of thrombin inhibitors: analogues of MD805 containing non-polar surrogates for arginine at the P1 position was written by Baettig, U.;Brown, L.;Brundish, D.;Dell, C.;Furzer, A.;Garman, S.;Janus, D.;Kane, P. D.;Smith, G.;Walker, C. V.;Cockcroft, X.;Ambler, J.;Mitchelson, A.;Talbot, M. D.;Tweed, M.;Wills, N.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2000.Electric Literature of C4H5N3O This article mentions the following:
A series of monocyclic and bicyclic amino acids have been synthesized and incorporated into thrombin inhibitors based on CGH728, an analog of the Mitsubishi compound MD805. Benzthiazolylalanine (Bta) was a good non-polar substitute for arginine at the P1 position, yielding compounds with low nanomolar potency and good selectivity for thrombin. In the experiment, the researchers used many compounds, for example, 5-Aminopyrimidin-4(3H)-one (cas: 69785-94-0Electric Literature of C4H5N3O).
5-Aminopyrimidin-4(3H)-one (cas: 69785-94-0) belongs to pyrimidine derivatives. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. A Cu-catalyzed and 4-HO-TEMPO-mediated [3 + 3] annulation of commercially available amidines with saturated ketones enables an efficient and facile synthesis of structurally important pyrimidines via a cascade reaction of oxidative dehydrogenation/annulation/oxidative aromatization.Electric Literature of C4H5N3O
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia