Title
Structural and biological evaluation of some loloatin C analogues
Author
Tuin, A.W.
Grotenbreg, G.M.
Spalburg, E.
de Neeling, A.J.
Mars-Groenendijk, R.H.
Noort, D.
van der Marel, G.A.
Overkleeft, H.S.
Overhand, M.
TNO Defensie en Veiligheid
Publication year
2009
Abstract
Loloatin C is a cyclic cationic antimicrobial peptide which is active against Gram positive as well as certain Gram negative bacteria. Unfortunately, it is equally potent against human erythrocytes. To probe the structure-activity relationship of this promising antibiotic peptide, amino acid substitution and/or incorporation of a constraint sugar amino acid dipeptide isoster has been applied. Six new derivatives have been synthesized using SPPS and their solution structure investigated using NMR studies. Finally, the antimicrobial and the hemolytic activities have been determined. © 2009 Elsevier Ltd. All rights reserved.
Subject
Chemistry
Cationic antimicrobial peptide
Loloatin C
Structure-activity relationship
Sugar amino acid
To reference this document use:
http://resolver.tudelft.nl/uuid:3afd55d3-4d0b-49a5-a1e1-3129422a8a94
DOI
https://doi.org/10.1016/j.bmc.2009.07.049
TNO identifier
183955
ISSN
0968-0896
Source
Bioorganic and Medicinal Chemistry, 17 (17), 6233-6240
Document type
article