1311293-10-3Relevant academic research and scientific papers
Design, synthesis and inhibition activity of a novel cyclic enediyne amino acid conjugates against MPtpA
Chandra, Koushik,Dutta, Debajyoti,Mitra, Analava,Das, Amit K.,Basak, Amit
, p. 3274 - 3279 (2011)
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 Ki of 22.5 μM. 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.
