Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors was written by Han, Yongxin;Giroux, Andre;Colucci, John;Bayly, Christopher I.;Mckay, Daniel J.;Roy, Sophie;Xanthoudakis, Steve;Vaillancourt, John;Rasper, Dita M.;Tam, John;Tawa, Paul;Nicholson, Donald W.;Zamboni, Robert J.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2005.COA of Formula: C4H6N2S This article mentions the following:
The iterative process for the discovery of a series of pyrazinone mono-amides as potent, selective and reversible non-peptide caspase-3 inhibitors (e.g., M826 and M867) is reported. The studied compounds were prepared according to modified literature procedure from ethylaminobutyrate hydrochloride via intermediate acids (e. g., I), which were synthesized using Dess-Martin periodinane oxidation Treating of coupled to the resin in the presence of Hunig’s base intermediate acids I with 90% TFA in water gave the desired inhibitors (e. g. II). These compounds were screened directly, without further purification, against four representative recombinant human caspases, as well as in the NT2 cell against camptothecin induced apoptosis. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1COA of Formula: C4H6N2S).
Thiazol-2-ylmethanamine (cas: 55661-33-1) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.COA of Formula: C4H6N2S
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica