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<i>Grindelia ventanensis</i> (Asteraceae) is an endemic species growing wild in Argentina. In this work, we studied the dichloromethane extract of this plant for their antioxidant activity and cholinesterase inhibition. This extract was fractionated using column chromatography and HPLC. Six diterpenoids were isolated and identified using RMN and MS analyses. The 13-methyl-17-oxo-labda-7,13-diene-15-oic acid elicited the best results in both bioassays, with IC₅₀ = 11.04 µM in the AChE inhibition test and an antioxidant activity comparable to trolox, the reference antioxidant (IC₅₀ = 7.13 µM). Significant bioactivity was also observed for the rest of the isolated compounds.