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yaoguiyang木蟲 (小有名氣)
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[求助]
求助構(gòu)效關(guān)系的翻譯
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An essential feature of Cyp inhibitors designed to be used as antiviral agents is that the immunosuppressive activity due to CN inhibition is reduced or removed. This has been most effectively achieved by modification of the side chain of the [MeLeu]4 residue, which is involved in a tight ‘a(chǎn)romatic sandwich’ with CN residues Trp352 and Phe356 (Fig. 4). Surprisingly, moving one methyl group at the [MeLeu]4 residue to give [MeIle]4CsA (NIM-811), was found to remove immunosuppressive activity, while retaining the same affinity for CypA as CsA itself.58 This ability to reduce immunosuppressive activity by making small chemical changes at [MeLeu]4 was further demonstrated by [MeVal]4CsA59 and [40-HOMeLeu]4CsA55a,59,60 which show >2500-fold and >100-fold loss of immunosuppressive activity, respectively. The [BMT]1 residue characteristic of the cyclosporins is unique in that in the cyclophilin-bound conformation, this group extends from the cyclophilin binding interface to a region very near the calcineurin-binding region (Figure 2). Early work had suggested that P1-modified cyclosporins can retain cyclophilin binding affinity without maintaining the immunosuppressive activity of 1.73,117 In particular, the Merck group highlighted the cyclophilin binding activity of [CH(OH)CH(CH3)- CH2SCH3]1-CsA, which has 178% of the cyclophilin binding activity of 1 but only 10% of the immunosuppressive potency.74 Aurinia has reported that extension of the BMT group of the cyclosporins and addition of a D-Ala group in the P3 position provides a series of nonimmunosuppressive cyclophilin analogue molecules such as 14 (Figure 9).118 This molecule has more than 14-fold greater inhibition of cyclophilin A isomerase activity relative to 1. Furthermore, while specific assay methodology was not provided, it was asserted that this example has only 3% of the immunosuppressive activity of 1. Although the structure has not been revealed, in July 2013 it was reported that Aurinia had identified a lead candidate and was in the process of fully evaluating the scope of the anti-HCV activity of this analogue. |
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