220808-33-3Relevant academic research and scientific papers
PROCESS FOR MAKING BIARYL-BRIDGED CYCLIC PEPTIDES
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Page/Page column 100; 101, (2021/06/04)
The invention provides a method of preparing a biaryl-bridged cyclic peptide compound of Formula (I), where R1, R2, R3, R4, R5, R8, R7, R8, R9, R10, R11, R12, n and m are as defined in the specification. The biaryl-bridged cyclic peptides of Formula (I) are used in the preparation of pharmaceutically active substances, such as, for example, arylomycin and arylomycin analogues.
Synthesis of Biaryl-Bridged Cyclic Peptides via Catalytic Oxidative Cross-Coupling Reactions
Ben-Lulu, Mor,Gaster, Eden,Libman, Anna,Pappo, Doron
supporting information, p. 4835 - 4839 (2020/02/11)
Biaryl-bridged cyclic peptides comprise an intriguing class of structurally diverse natural products with significant biological activity. Especially noteworthy are the antibiotics arylomycin and its synthetic analogue G0775, which exhibits potent activity against Gram-negative bacteria. Herein, we present a simple, flexible, and reliable strategy based on activating-group-assisted catalytic oxidative coupling for assembling biaryl-bridged cyclic peptides from natural amino acids. The synthetic approach was utilized for preparing a number of natural and unnatural biaryl-bridged cyclic peptides, including arylomycin/G0775 and RP 66453 cyclic cores.
Discovery of novel motilin antagonists: Conversion of tetrapeptide leads to orally available peptidomimetics
Taka, Naoki,Matsuoka, Hiroharu,Sato, Tsutomu,Yoshino, Hitoshi,Imaoka, Ikuhiro,Sato, Haruhiko,Kotake, Ken-ichiro,Kumagai, Yoshikazu,Kamei, Kenshi,Ozaki, Ken-ichi,Higashida, Atsuko,Kuroki, Toshio
scheme or table, p. 3426 - 3429 (2010/02/28)
We successfully discovered peptidomimetic motilin antagonists (17c and 17d) through the improvement of physicochemical properties of a tetrapeptide antagonist (2). Furthermore, with oral administration and based on motilin antagonistic activity, both comp
