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Novel N‑Benzenesulfonyl Sophocarpinol Derivatives as Coxsackie B Virus Inhibitors
journal contribution
posted on 2015-02-12, 00:00 authored by Sheng Tang, Lanying Kong, Yinghong Li, Jiandong Jiang, Limei Gao, Xinyue Cheng, Linlin Ma, Xin Zhang, Yuhuan Li, Danqing SongNovel N-benzenesulfonyl sophocarpinic acid/ester
and sophocarpinol derivatives were synthesized and evaluated for their
antienteroviral activities against coxsackievirus type B3 (CVB3) from
sophocarpine (1), a natural medicine isolated from Chinese
herb. Structure–activity relationship (SAR) analysis revealed
that the double bond and its geometrical configuration and position
at the C-11 attachment did not greatly affect the potency. Among these
derivatives, sophocarpinol 24d exerted the promising activities against not only CVB3
but also CVB1, CVB2, CVB5, and CVB6 with IC50 ranging from
0.62 to 3.63 μM (SI from 46 to 275), indicating a broad-spectrum
antienteroviral characteristic. The SAR results provided the powerful
information for further strategic optimization and development of
a novel scaffold of broad-spectrum antiviral candidates against enteroviruses.