Please use this identifier to cite or link to this item: https://doi.org/10.1016/j.tetlet.2014.02.008
Title: Diverted total synthesis of falcitidin acyl tetrapeptides as new antimalarial leads
Authors: Kotturi, S.R. 
Somanadhan, B.
Ch'Ng, J.-H.
Tan, K.S.-W.
Butler, M.S.
Lear, M.J. 
Keywords: Antimalarial agents
Falcitidin
Natural products
Tetrapeptide
Trifluoromethyl
Issue Date: 12-Mar-2014
Citation: 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
URI: http://scholarbank.nus.edu.sg/handle/10635/93627
ISSN: 00404039
DOI: 10.1016/j.tetlet.2014.02.008
Appears in Collections:Staff Publications

Show full item record
Files in This Item:
There are no files associated with this item.

SCOPUSTM   
Citations

3
checked on Sep 22, 2018

WEB OF SCIENCETM
Citations

3
checked on Sep 11, 2018

Page view(s)

21
checked on May 11, 2018

Google ScholarTM

Check

Altmetric


Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.