Ohba, Mai; Oka, Tomoichiro; Ando, Takayuki; Arahata, Saori; Ikegaya, Asaka; Takagi, Hirotaka; Ogo, Naohisa; Owada, Kazuhiro; Kawamori, Fumihiko; Wang, Qiuhong; Saif, Linda J.; Asai, Akira published the artcile< Discovery and synthesis of heterocyclic carboxamide derivatives as potent anti-norovirus agents>, Application of C5H2Cl2O2S, the main research area is heterocyclic carboxamide preparation SAR antiviral.
In this study, synthesis, anti-norovirus activity, and structure-activity relationship (SAR) of a series of heterocyclic carboxamide derivatives I (R3 = 2-thienyl, 2-furyl, 2-thiazolyl, etc.; R4 = H, 6-Cl, 4-Br, etc.) has been described. Heterocyclic carboxamide I (R3 = 5-bromo-thiophen-2-yl; R4 = 6-F) (50% effective concentration (EC50)= 37 μM) was identified using the cytopathic effect reduction assay by the author’s screening campaign. Initial SAR studies suggested the importance of halogen substituents on the heterocyclic scaffold and identified 3,5-di-bromo-thiophene derivative (EC50 = 24 μM) and 4,6-di-benzothiazole derivative (EC50 = 5.6 μM) as more potent inhibitors than I (R3 = 5-bromo-thiophen-2-yl; R4 = 6-F). Moreover, their hybrid compound, 3,5-di-bromo-thiophen-4,6-di-fluoro-benzothiazole, showed the most potent anti-norovirus activity with a EC50 value of 0.53 μM. Further investigation suggested that the hybrid compound might inhibit intracellular viral replication or the late stage of viral infection.
Chemical & Pharmaceutical Bulletin published new progress about Antiviral agents. 31166-29-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C5H2Cl2O2S, Application of C5H2Cl2O2S.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics