New analogs of temporin-LK1 as inhibitors of multidrug-resistant (MDR) bacterial pathogens

作者：Shah Zafar Ali; Farooq Saba; Ali Syed Abid; Hameed Abdul; Choudhary M Iqbal; Shaheen Farzana^*

来源：Synthetic Communications, 2018, 48(10): 1172-1182.

DOI：10.1080/00397911.2018.1437450

• Antibacterial peptides
• MDR bacterial strains
• Pseudomonas aeruginosa
• Staphylococcus aureus
• temporin-LK1

The peptide temporin-LK1 (1) was obtained from the skin secretion of frog Limnonectes kuhlii (Ranidae). It is a unique antimicrobial peptide with 17 residues, including four L-phenylalanines and single glycine. Mass spectrometry and Edmand degradation were used for the determination of sequence of amino acids in temporin-LK 1 (1), and confirmed by cDNA cloning. We report here the synthesis and structural studies of temporin-LK1 (1) and its analogs 2-4. Peptides 2-4 were prepared by substitution of achiral glycine residue of temporin-LK1 (1) with D-alanine, L-phenylglycine, and L-naphthylalanine, respectively. Peptides 1-4 were evaluated against multidrug-resistant (MDR) strains of Staphylococcus aureus and Pseudomonas aeruginosa. Analog 2 was found active against all MDR strains of S. aureus and P. aeruginosa at a much lower dose than the clinically used antibiotics.
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• 出版日期2018