207725-70-0Relevant articles and documents
A Constrained Diketopiperazine as a New Scaffold for the Synthesis of Peptidomimetics
Pons, Jean-Francois,Fauchere, Jean-Luc,Lamaty, Frederic,Molla, Annie,Lazaro, Rene
, p. 853 - 859 (2007/10/03)
As a new scaffold for peptidomimetic synthesis, a highly constrained bifunctional diketopiperazine, 4, has been prepared by smooth N-alkylation with tert-butyl bromoacetate. As a first application, we describe herein the synthesis of new peptidomimetics of the Arg-Gly-Asp (RGD) sequence. The product 30, which shows a selective platelet-aggregation inhibiting activity, can be used as a lead for the preparation of more potent products.