Argifin; efficient solid phase total synthesis and evalution of analogues of acyclic peptide

An effective solid phase synthesis of Argifin, providing subsequent access to effective synthesis of analogues, was developed in 13% overall yield, as well as elucidating structure–activity relationships. The novel acyclic peptide 18b, prepared from a synthetic intermediate of Argifin, was found to...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2009-04, Vol.17 (7), p.2751-2758
Hauptverfasser: Sunazuka, Toshiaki, Sugawara, Akihiro, Iguchi, Kanami, Hirose, Tomoyasu, Nagai, Kenichiro, Noguchi, Yoshihiko, Saito, Yoshifumi, Yamamoto, Tsuyoshi, Ui, Hideaki, Gouda, Hiroaki, Shiomi, Kazuro, Watanabe, Takeshi, Ōmura, Satoshi
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Sprache:eng
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Zusammenfassung:An effective solid phase synthesis of Argifin, providing subsequent access to effective synthesis of analogues, was developed in 13% overall yield, as well as elucidating structure–activity relationships. The novel acyclic peptide 18b, prepared from a synthetic intermediate of Argifin, was found to be 70 times more potent as an inhibitor of Serratia marcescens chitinases B than Argifin itself
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2009.02.047