1228804-21-4Relevant articles and documents
Analogues of both Leu- and Met-enkephalin containing a constrained dipeptide isostere prepared from a Baylis-Hillman adduct
Galeazzi, Roberta,Martelli, Gianluca,Marcucci, Eleonora,Orena, Mario,Rinaldi, Samuele,Lattanzi, Roberta,Negri, Lucia
, p. 1057 - 1065 (2010)
An efficient route was developed for the synthesis of the Fmoc-protected dipeptide 4, isostere of Gly-Gly containing an α-methylene β-amino acid; the conformationally restricted analogues of Leu-enkephalin, 3a, and Met-enkephalin, 3b, respectively, were prepared by changing 4 for Gly 2-Gly3 in the native compounds 3a and 3b whose biological activities were significantly lower than the parent compounds.