TEMPLATE-FIXED &bgr;-HAIRPIN PEPTIDOMIMETIC WITH CXCR4 ANTAGONIZING ACTIVITY

摘要

PROBLEM TO BE SOLVED: To provide template-fixed &bgr;-hairpin peptidomimetics having CXCR4 activity which comprise a template-fixed chain of 12, 14 or 18 α-amino acid residues which are Gly, NMeGly, Pro or Pip or certain types depending on the positions of the residues in the chain.SOLUTION: Template-fixed &bgr;-hairpin peptidomimetics are represented by formula (I) (wherein Z is a template-fixed chain of 12, 14 or 18 α-amino acid residues) and include salts thereof. They have CXCR4 antagonizing properties and can be used for preventing HIV infections in healthy individuals or for slowing or halting viral progression in infected patients or for treating immuno suppression or during apheresis collections of peripheral blood stem cells. These &bgr;-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution-phase synthetic strategy.