Products/Services Used | Details | Operation |
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Proteins, Expression, Isolation and Analysis | Chloromethylated Merrifield resin and TFMSA were from Fluka, HATU from GenScript (Piscataway, NJ), and HBTU from Matrix Innova- tion (Montreal, Quebec). | Get A Quote |
A series of gramicidin S (GS) analogues have been synthesized where the Phe (i + 1) and Pro (i + 2) residues of the beta-turn have been swapped while the respective chiralities (D-, L-) at each position are preserved, and Phe is replaced by surrogates with aromatic side chains of diverse size, orientation, and flexibility. Although most analogues preserve the beta-sheet structure, as assessed by NMR, their antibiotic activities turn out to be highly dependent on the bulkiness and spatial arrangement of the aromatic side chain. Significant increases in microbicidal potency against both Gram-positive and Gram-negative pathogens are observed for several analogues, resulting in improved therapeutic profiles. Data i... More