Chandra, Koushik ; Dutta, Debajyoti ; Mitra, Analava ; Das, Amit K. ; Basak, Amit (2011) Design, synthesis and inhibition activity of a novel cyclic enediyne amino acid conjugates against MPtpA Bioorganic & Medicinal Chemistry, 19 (10). pp. 3274-3279. ISSN 0968-0896
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Official URL: http://doi.org/10.1016/J.Bmc.2011.03.024
Related URL: http://dx.doi.org/10.1016/J.Bmc.2011.03.024
Abstract
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.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to Elsevier Science. |
| Keywords: | Inhibition; Enediyne; Amino acid; Conjugate; MPtpA; Knoevenagel |
| ID Code: | 129878 |
| Deposited On: | 05 Dec 2022 05:26 |
| Last Modified: | 05 Dec 2022 05:26 |
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