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Total Synthesis and Antibacterial Study of Cyclohexapeptides Desotamide B, Wollamide B and Their Analogs
Author(s) -
Chen YiXing,
Liu Chao,
Liu Nan,
Wu Ye,
Zhao QingJie,
Hu HongGang,
Li Xiang,
Zou Yan
Publication year - 2018
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.201700414
Subject(s) - chemistry , total synthesis , antibacterial peptide , natural product , peptide , antibacterial activity , peptide synthesis , antibiotics , cyclic peptide , bacteria , combinatorial chemistry , stereochemistry , gram , solid phase synthesis , biochemistry , biology , genetics
As natural‐product‐derived antibiotics, desotamides A – D and wollamides exhibit growth inhibitory activity against Gram ‐posivite bacteria ( IC 50 0.6 – 7 μ m ) and are noncytotoxic to mammalian cells ( IC 50 > 30 μ m ). Herein we firstly report the total synthesis of above two cyclohexapeptides as well as a series of structural variants through solid phase peptide synthesis, of which 3 displayed a 2‐fold increase of antibacterial activity when compared with the original peptide 1 . This strategy may offer good improvements for the synthesis of other cyclic peptides.