Design and synthesis of novel FKBP inhibitors

…, S Julin, J DiBrino, R Spencer, R Williams

文献索引：Hauske; Dorff; Julin; DiBrino; Spencer; Williams Journal of Medicinal Chemistry, 1992 , vol. 35, # 23 p. 4284 - 4296

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被引用次数: 98

摘要

Small molecule FKBP inhibitors were prepared with inhibitory activity ranging from micromolar to nanomolar. The design of these inhibitors derives from a structural analysis of the substrates for FKBP and cyclophilin. As a consequence of this analysis two key observations were made, namely:(1) amino ketone moieties are suitable as FKBP recognition elements at the P1-P1'site and (2) the P3/-P4/site will accept a trans-olefin as ...