Citation: YANG Jin, MA Qiseng, ZHONG Ying, ZHU Longbao, GE Fei, TAO Yugui, SONG Ping. Solid-Phase Synthesis of Cyclohexapeptide Thermoactinoamide A and Its Antibacterial Activity[J]. Chinese Journal of Applied Chemistry, ;2019, 36(6): 677-682. doi: 10.11944/j.issn.1000-0518.2019.06.180364 shu

Solid-Phase Synthesis of Cyclohexapeptide Thermoactinoamide A and Its Antibacterial Activity

School of Biochemical Engineering, Anhui Polytechnic University, Wuhu, Anhui 241000, China

Corresponding author: ZHU Longbao, swgctaoyg@126.com
Received Date: 13 November 2018
Revised Date: 19 December 2018
Accepted Date: 30 January 2019

Fund Project: the Natural Sciences Foundation of Anhui Province Universities KJ2017A123the Anhui Polytechnic University Youth Talent Program 2016BJRC006Supported by the Natural Sciences Foundation of Anhui Province Universities(No.KJ2017A123), the Anhui Polytechnic University Youth Talent Program(No.2016BJRC006)

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A natural antibacterial cyclic peptide thermoactinoamide A was synthesized by solid-liquid phase two-step method. First, based on fluorenylmethoxycarbonyl(Fmoc) solid phase synthesis, the linear peptide was obtained in 84% yield by optimizing the addition of N, N'-diisopropylethylamine(DIPEA). Then the linear peptide was converted to thermoactinoamide A in 51% yield(43% yield total) through optimizing the cyclization conditions. Antibacterial activity test results show that minimum inhibitory concentration of cyclic thermoactinoamide A for Staphylococcus aureus is 32 μg/mL. In summary, an effectively synthetic strategy was developed for further applications of cyclic peptide thermoactinoamide A on analyzing the structure-activity relationship and improving the bioactivity.
- thermoactinoamide A,
- solid-phase synthesis,
- cyclic peptide,
- antibacterial activity
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