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submitted on 17.08.2020 and posted on 18.08.2020by 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.