O

R1 = OH or Acyl sulfonamide

Fig. 2.10 Recent macrocyclic tripeptide inhibitors.

R1 = OH or Acyl sulfonamide

Fig. 2.10 Recent macrocyclic tripeptide inhibitors.

work comprised substitution of the P2 proline as well as modification of the P1 residue (Table 2.5) [138-143]. These studies culminated in the development of VX-950, a a-keto-amide, which is currently undergoing clinical testing [144]. The compound binds slowly and reversibly to the protease. It

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