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An efficient and practical method for solid-phase synthesis of tripeptide-bearing glycopeptide antibiotics: combinatorial parallel synthesis of carboxamide derivatives of chloroorienticin B
Authors:Yasukata Tatsuro  Shindo Hirohisa  Yoshida Osamu  Sumino Yukihito  Munekage Tadashi  Narukawa Yukitoshi  Nishitani Yasuhiro
Institution:Discovery Research Laboratories, Shionogi & Co., Ltd., Sagisu 5-12-4, Fukushima-ku, Osaka 553-0002, Japan. tatsuro.yasukata@shionogi.co.jp
Abstract:An efficient and practical method was established for solid-phase parallel synthesis of the peptide-bearing carboxamide derivatives of chloroorienticin B, and over 80 compounds were synthesized simultaneously. Among the derivatives prepared, compounds having both tryptophan and tyrosine residues (1-3) were found to possess potent antibacterial activity against VRE.
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