M. Falorni et al., New oxazole-based conformationally restricted peptidomimetics: Design and synthesis of pseudopeptides, EUR J ORG C, (18), 2000, pp. 3217-3222
A general synthesis of a new class of optically active amino acids containi
ng an oxazole moiety is described along with a strategy for their insertion
into a peptidomimetic chain. A modified portion of endothelin-1 is prepare
d as a potential receptor antagonist. The procedure presented is based on r
eadily available materials and can be performed in multigram quantities.