Method for synthesizing cyclic peptide

Abstract

Abstract PURPOSE:To obtain a new cyclic peptide useful as an antifungal agent, having low toxicity and strongly sterilizing action on various pathogenic fungi by synthesizing a straight-chain peptide having specific amino acid sequence and subjecting the straight-chain peptide to ring-closure reaction. CONSTITUTION:A method for successively linking an N-methyl-alpha-amino acid, an alpha-hydroxy acid, an alpha-amino acid, a cyclic amino acid, etc., is performed to give an O-protection type or nonprotection type straight-chain peptide of formula I [X1 is 2-hydroxy-3-methylpentanoic acid (Hmp), 2-hydroxy-3- methylbutanoic acid (Hmb) or 2,4-dihydroxy-3-methylpentanoic acid (Dhmp); X3 is Phe, etc.; X4 is MePhe, Mealy, MeTyr, etc.; X5 is Pro, etc.; X6 is Leu, Val, Glu, etc.; X7 is Medal, MeLeu, Hmb, etc.; X8 is Leu, Nva, etc.; X9 is betaHOMeVal, MeThr, etc.], which is subjected to ring closure to give a cyclic peptide of formula II.

Inventors

• 👤 Toru Kurome
• 👤 徹 黒目
• 👤 Kazutada Takesako
• 👤 一任 竹迫
• 👤 Ikunoshin Katou
• 👤 郁之進 加藤
• 👤 Kaoru Inami
• 👤 薫 稲見
• 👤 Tetsuo Shiba
• 👤 哲夫 芝

Bibliographic Details