Design, synthesis and antitrypanosomal activity of heteroaryl-based 1,2,4-triazole and 1,3,4-oxadiazole derivatives was written by Shaykoon, Montaser Sh.;Marzouk, Adel A.;Soltan, Osama M.;Wanas, Amira S.;Radwan, Mohamed M.;Gouda, Ahmed M.;Youssif, Bahaa G. M.;Abdel-Aziz, Mohamed. And the article was included in Bioorganic Chemistry in 2020.Application of 6924-68-1 This article mentions the following:
Two series of novel 1,2,4-triazol-3-yl-thioacetamides I [X = O, NOH; R = 4-pyridyl, 2-pyrazinyl] and 5-pyrazin-2-yl-3H-[1,3,4]oxadiazole-2-thiones II [R1 = 4-Me, 2-F, 3,4,5-tri-MeO, etc.] were synthesized. The prepared compounds I and II were identified using 1H NMR, 13C NMR and elemental anal. The synthesized compounds I and II [R1 = 2-F, 4-F, 4-Me, 2-MeO, 4-MeO] were evaluated with α-difluoromethylornithine (DFMO) as a control drug for their in-vitro antitrypanosomal activity against Trypanosoma brucei. Results showed that compound I [X = O, R = 4-pyridyl (III)] was the most active compound in general and also more potent than control DFMO. Compound III was 8 folds more potent than the reference with IC50 of 0.79μM and IC90 of 1.35μM, resp. compared to DFMO (IC50 = 6.10μM and IC90 of 8.66μM). The tested compounds showed moderate cytotoxicity with selectivity indexes ranging from 12 to 102 against L6 cells. Docking study was performed into ten of T. brucei enzymes which have been identified as potential/valid targets for most of the antitrypanosomal agents. The results of the docking study revealed high binding scores toward many of the selected enzymes. A good correlation was observed only between log (IC50) of antitrypanosomal activity of the new compounds and their calculated Ki values against TryR enzyme (R2 = 0.726). Compound III, the most active as antitrypanosomal agents exhibited similar binding orientation and interaction to those of WP6 against TryR enzyme. However, in a next round of work, a complementary studies will be carried out to clarify the mechanism of action of these compounds In the experiment, the researchers used many compounds, for example, Ethyl pyrazine-2-carboxylate (cas: 6924-68-1Application of 6924-68-1).
Ethyl pyrazine-2-carboxylate (cas: 6924-68-1) belongs to pyrazine derivatives. Pyrazines are part of several biologically active polycyclic compounds; examples are quinoxalines, phenazines; and the bio-luminescent natural products pteridines, flavins, and their derivatives. Substituted pyrazines have been found as subunits of multiple synthetically constructed therapeutic agents, as well as several natural products.Application of 6924-68-1