- A combined solid- and solution-phase approach provides convenient access to analogues of the calcium-dependent lipopeptide antibiotics
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The calcium-dependent lipopeptide antibiotics represent a promising new class of antimicrobials for use in combating drug-resistant bacteria. At present, daptomycin is the only such lipopeptide used clinically and displays potent antimicrobial activity against a number of pathogenic Gram-positive bacteria. Given the increasing need for new antibiotics, practical synthetic access to unnatural analogues of daptomycin and related antimicrobial lipopeptides is of value. We here report an efficient synthetic route combining solid- and solution-phase techniques that allows for the rapid preparation of daptomycin analogues. Using this approach, four such analogues, including two enantiomeric variants, were synthesized and their antimicrobial activities and hydrolytic stabilities evaluated.
- Hart, Peter 'T,Kleijn, Laurens H. J.,De Bruin, Gerjan,Oppedijk, Sabine F.,Kemmink, Johan,Martin, Nathaniel I.
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p. 913 - 918
(2014/02/14)
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- Synthesis of 'difficult' peptides free of aspartimide and related products, using peptoid methodology
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We developed an efficient, cost effective strategy for Fmoc-based solid phase synthesis of 'difficult' peptides and/or peptides containing Asp/Asn-Gly sequences, free of aspartimide and related products, using a peptoid methodology for the preparation of N-substituted glycines.
- Zahariev, Sotir,Guarnaccia, Corrado,Pongor, Csaba I.,Quaroni, Luca,?ema?ar, Ma?a,Pongor, Sándor
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p. 4121 - 4124
(2007/10/03)
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