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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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Traditionally, the immunosuppressive potential of cyclosporin derivatives was tested in isolated T-cell assays. In this context, the immunosuppressive activity of cyclosporins largely correlates with the ability of cyclophilin A−cyclosporin complexes to inhibit the activity of calcineurin. However, as described above, cyclophilins appear to be involved in other immune response processes such as innate immunity and inflammation. In order to explore the potential of cyclophilin inhibitors to act as inhibitors of leukocyte trafficking by inhibiting extracellular cyclophilins, a series of impermeable cyclosporins were prepared.83 The benzimidazole derivative 15 (Figure 9) was determined to have a similar affinity to cyclophilin A as 1 in an in vitro proline isomerase binding assay. A cellular cyclophilin binding assay developed using a fluorescently labeled cyclophilin derivative revealed that 15 is at least 50-fold less permeable than 1. As expected, despite its significant restriction to the extracellular space, 15 inhibits leukocyte migration toward cyclophilin A. This inhibitor also reduces leukocyte activation in a mouse model of allergic contact hypersensitivity. Although detailed data are not available, in a patent filing Scynexis explored the potential for alkylation at P5 to influence the immunosuppressive activity and antiviral potency of 1.119 Earlier, chemists at Sandoz had demonstrated that alkylation of the free NH at this position can influence the conformation and immunsuppressive activity of cyclosporin derivatives.120 Compound 16 (Figure 10) was prepared via alkylation of [(D)- MeAla]3-CsA with dimethylallyl bromide. This analogue was reported to bind to cyclophilins A and D with good (<60 nM) potency and to have an EC50 in the replicon assay of less than 200 nM. Furthermore, in a standard stimulated T-cell assay, 12 was found to be at least a 40-fold less potent inhibitor of IL-2 release than 1. |
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yaoguiyang
木蟲 (小有名氣)
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2樓2014-11-30 11:06:32
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