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TDPBP Derivative Aiding Liquid-Phase Synthesis Strategy and ACE Inhibitory Structure-activity Relationship of Anti-SARS Octapeptide

preprint
submitted on 17.08.2020 and posted on 18.08.2020 by Haidi Li, Jin Ren, Zixin Zhang, Junyou Li, Ninghui Chang, Chuanguang Qin
The tri(4'-diphenylphosphonyloxylbenzoyl phenyl) phosphate (TDPBP) derivatives were designed and developed as C-terminal supports to aid the greener and highefficient liquid-phase peptide synthesis (LPPS) without the need of unrecyclable resin and chromatographic separation, whereby the anti-SARS octapeptide (2) (AVLQSGFR) was synthesized with TDPBP-OH support via Fmoc chemistry and support-aided precipitation (SAP) technology. Furthermore, the ACE inhibition and the inhibitory structure-activity relationship (SAR) between the synthetic C-terminal amidated derivate (1), anti-SARS octapeptide (2) and its alanine-scanning sequence analogues (3) to (9) were systematically studied by HPLC analysis and 3D-QSAR via molecular docking.

History

Email Address of Submitting Author

qinchg@nwpu.edu.cn

Institution

Northwestern Polytechnical University

Country

China

ORCID For Submitting Author

0000-0003-4849-0187

Declaration of Conflict of Interest

No competing financial interests

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