Enkephalins mimetics design

F ure 3.28. Peptidomimetics that have been designed based on iterative introduction of constraints into parent peptide and hypotheses concerning receptor-bound conformation. Enkephalin mimetic (388), RGD platelet GPIIb/IIIa receptor antagonists (384,385), thyrohberin [TRH (387)], and somatostatin (383,389).For an overview of recent approaches to peptidomimetic design, see the review by Bursavich and Rich (382). 

Compounds 32 and 33 (Scheme 13), reported in the 1980s,1t79,80 were designed as mimetics of the pentapeptide Met-enkephalin. Both compounds had very poor biological activity, which could be attributable to a number of features. 

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