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TDPBP Derivative Aiding Liquid-Phase Synthesis Strategy and ACE Inhibitory Structure-activity Relationship of Anti-SARS Octapeptide
preprintsubmitted on 17.08.2020, 17:34 and posted on 18.08.2020, 13:18 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.