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[DOI] [PMC free article] [PubMed] [Google Scholar] 9.Crdova A., Mielgo-Ayuso J., Fernandez-Lazaro C., Caballero-Garca A., Roche E., Fernndez-Lzaro D

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The structure of the IRAP ( vide infra ( The metathesis reaction was applied to obtain a series of macrocyclic compounds, devoid of the reactive disulfide function and with the potential to become oral bioavailable and more metabolically stable ( 28 exhibited a Ki value of 4.1 nM and the corresponding analogue with a saturated double bond, compound 29 , a Ki value of 25 nM, demonstrating that a proper constrain of flexibility of the ring system, alternatively an electron density in the center of the lipophilic bridge between amino acid residues in positions 1 and 3 is favorable for affinity to IRAP (Figure 7)