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|Title:||Diverted total synthesis of falcitidin acyl tetrapeptides as new antimalarial leads|
|Authors:||Kotturi, S.R. |
|Source:||Kotturi, S.R., Somanadhan, B., Ch'Ng, J.-H., Tan, K.S.-W., Butler, M.S., Lear, M.J. (2014-03-12). Diverted total synthesis of falcitidin acyl tetrapeptides as new antimalarial leads. Tetrahedron Letters 55 (11) : 1949-1951. ScholarBank@NUS Repository. https://doi.org/10.1016/j.tetlet.2014.02.008|
|Abstract:||We report not only the convergent total synthesis of falcitidin, a natural inhibitor of falcipain-2 from myxobacterium Chitinophaga, but also its diversification into a new antimalarial class of N-acyl tetrapeptides (Acyl-His-Ile-Val-Pro-NH2). Despite the lack of whole-cell activity of falcitidin itself, our study led to the identification of a trifluoromethyl (CF3) analogue displaying sub-micromolar IC50 activity against Plasmodium falciparum 3D7 in a standard blood-cell assay, but only when N-tritylated on its histidine (imidazole) residue. © 2014 Elsevier Ltd. All rights reserved.|
|Source Title:||Tetrahedron Letters|
|Appears in Collections:||Staff Publications|
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