Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 6, Issue 2, Pages 183-186Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml500525s
Keywords
Sophocarpine; sophocarpinol; structure-activity relationship; enteroviruse; coxsakievirus type B3
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Funding
- National Natural Science Foundation of China [81321004, 81402799]
- Beijing Natural Science Foundation [7142107]
- 863 Youth Project [SS2015AA020910]
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Novel 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, CVBS, and CVB6 with IC50 ranging from 0.62 to 3.63 mu M (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.
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