Abstract A series of stereochemically defined analogues of (2S, 3R, 4S)-4-hydroxyisoleucine and related α-hydroxy acids have been prepared by multi-step routes from D-glucose, whereas ketolization between TBDMS-protected hydroxypropanone and ethyl isocyanoacetate led to racemic analogues. Bioassays showed that of eight newly synthesized compounds, two of them presented an interesting statistical trend to increase ...