Synthesis and antifungal activity of β-amino alcohol derivatives of sclareol

Twenty-four β-amino alcohol derivatives of sclareol were synthesized and evaluated for their in vitro antifungal activity using the mycelia growth inhibitory rate method. The structure-activity relationship indicated that the nature and position of the substituent on the phenyl ring had an effect on the activity. Generally, the result showed that the m-substituted isomers exhibited better activity than their corresponding o/p-substituted isomers. Compared with the other derivatives, compounds 2a-2c containing fluoro group proved to have excellent fungicidal activities against Fusarium graminearum with EC₅₀ values of 3.79, 3.35, and 4.66 μg/mL, respectively.