Structure-activity relationship (SAR) studies of the natural pesticida
l peptide, tentoxin, are described in the context of similarity betwee
n pharmaceutical and agricultural methods of developing biologically a
ctive peptidomimetics. Essential residue substitutions that confer bio
logical activity through predictable conformational changes in the pep
tide backbone and side chain functionalities are discussed. A combinat
ion of molecular modelling studies and the biological activity of natu
ral, synthetic and photochemically transformed analogs of tentoxin is
utilized to further the understanding of structural and conformational
requirements for biological activity.