Design, synthesis and inhibition activity of a novel cyclic enediyne amino acid conjugates against MPtpA

[摘要]：In course of studies towards the discovery of selective inhibitors of MPtpA, a novel cyclic endiyne malonamic acid has been designed and synthesized. The synthesis involves a crucial intramolecular Knoevenagel reaction. The compound displayed a reversible non-competitive inhibition against MPtpA with inhibition constant K-i of 22.5 mu M. The enediyne acts as a recognition framework in inducing the inhibition and not as a reactive functional moiety. This was confirmed by comparing the inhibiting activity with that of the corresponding saturated cyclic non-enediyne analogue. (C) 2011 Elsevier Ltd. All rights reserved.

[全文传递流程]：

一般上传文献全文的时限在1个工作日内