ABSTRACT
12-N-Benzenesulfonyl-11-matrinic acid derivatives are a new class of anti-CVB3 compounds, but the mechanism of action is still unknown. Therein, two kinds of molecule probes were designed and constructed in this study, including matrinic amines that might be applied to the BIAcore fishing technique and biotin-tagged matrinic derivatives, which could be applied in the biotin affinity chromatography. Moreover, their anti-CVB3 activities were evaluated. Among them, 10a displayed a good activity with an IC50 value of 0.8 μmol·L-1. This active molecule probe provides a key chemical tool for exploration of the anti-CVB3 mechanism of this type of compounds.
ABSTRACT
12-N-m-Cyanobenzenesulfonyl matrinic butyl methyl ether is a potent anti-coxsackievirus B3(CVB3) agent bearing a novel structure skeleton. Taking this compound as a lead, totally 15 novel target compounds have been synthesized and evaluated for the anti-CVB3 activities using CPE method. Structureactivity relationship (SAR) demonstrated that the shorten-length of 11-side chain was not helpful for keeping the good anti-virus activity. Among the newly synthesized compounds, compound c1 displayed a good anti-CVB3 activity with the IC50 of 7.1 μmol·L-1 and SI of 35.5, similar to that of the lead. The SAR results provided useful information for further optimization of these compounds in the molecular structure.