The development of a new approach for the generation of a novel type of put
ative insect control agents based on backbone cyclic peptidomimetic antagon
ists of insect-neuropeptides is reported. The approach, termed the backbone
cyclic neuropeptide based on antagonist (BBC-NBA) was applied to the insec
t pyrokinin/pheromone biosynthesis activating neuropeptide (PBAN) family as
a model, and led to the discovery of a potent linear lead antagonist and s
everal highly potent, metabolically stable BBC peptidomimetic antagonists,
devoid of agonistic activity, which inhibited in vivo PBAN-mediated activit
ies in moths. (C) 2000 Elsevier Science Ltd. All rights reserved.