Total Synthesis of Cyclosenegalin A

Abstract A Pro‐Gly‐typed cyclopeptide, cyclosenegalin A, was firstly isolated from Annona senegalensis and Annona scleroderma. In this study, we reported synthesis the cycloheptapeptide with a combination of solid‐ and solution‐phase synthetic methods. This study also compared the effectiveness of β...

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Main Authors: Anderson Arnold Aloanis, Prof. Tati Herlina, Dr. Ari Hardianto, Prof. Rani Maharani
Format: Article
Language:English
Published: Wiley-VCH 2024-12-01
Series:ChemistryOpen
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Online Access:https://doi.org/10.1002/open.202400175
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author Anderson Arnold Aloanis
Prof. Tati Herlina
Dr. Ari Hardianto
Prof. Rani Maharani
author_facet Anderson Arnold Aloanis
Prof. Tati Herlina
Dr. Ari Hardianto
Prof. Rani Maharani
author_sort Anderson Arnold Aloanis
collection DOAJ
description Abstract A Pro‐Gly‐typed cyclopeptide, cyclosenegalin A, was firstly isolated from Annona senegalensis and Annona scleroderma. In this study, we reported synthesis the cycloheptapeptide with a combination of solid‐ and solution‐phase synthetic methods. This study also compared the effectiveness of β‐turn inducer type I and II in cyclosenegalin A to facilitate the cyclization process. The synthesis of cyclosenegalin A were prepared using two different sequences of linear peptides for cyclization. First sequence employed β‐turn type I inducer (Ser‐Ala‐Val‐Thr) as turning point and second sequence employed β‐turn type II inducer (Thr‐Pro‐Gly‐Leu). The successful cyclization was obtained using the linear sequence of NH2‐Ala‐Val‐Thr‐Pro‐Gly‐Leu‐Ser‐OH with β‐turn type II. The final product was obtained in 8.2 % yield with PyBOP/DIEA act as coupling agent. The synthetic cyclosenegalin A were characterized with HR‐ToFMS, 1H NMR, 13C NMR, HSQC, HMBC, TOCSY, and ROESY. The synthetic product was also evaluated for its antimicrobial activity.
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spelling doaj-art-78988d367a0a4ccb89a90b85e85ee5aa2025-08-20T02:20:51ZengWiley-VCHChemistryOpen2191-13632024-12-011312n/an/a10.1002/open.202400175Total Synthesis of Cyclosenegalin AAnderson Arnold Aloanis0Prof. Tati Herlina1Dr. Ari Hardianto2Prof. Rani Maharani3Department Chemistry Universitas Negeri Manado Minahasa 95619Department Chemistry Universitas Padjadjaran Jatinangor 45363Department Chemistry Universitas Padjadjaran Jatinangor 45363Department Chemistry Universitas Padjadjaran Jatinangor 45363Abstract A Pro‐Gly‐typed cyclopeptide, cyclosenegalin A, was firstly isolated from Annona senegalensis and Annona scleroderma. In this study, we reported synthesis the cycloheptapeptide with a combination of solid‐ and solution‐phase synthetic methods. This study also compared the effectiveness of β‐turn inducer type I and II in cyclosenegalin A to facilitate the cyclization process. The synthesis of cyclosenegalin A were prepared using two different sequences of linear peptides for cyclization. First sequence employed β‐turn type I inducer (Ser‐Ala‐Val‐Thr) as turning point and second sequence employed β‐turn type II inducer (Thr‐Pro‐Gly‐Leu). The successful cyclization was obtained using the linear sequence of NH2‐Ala‐Val‐Thr‐Pro‐Gly‐Leu‐Ser‐OH with β‐turn type II. The final product was obtained in 8.2 % yield with PyBOP/DIEA act as coupling agent. The synthetic cyclosenegalin A were characterized with HR‐ToFMS, 1H NMR, 13C NMR, HSQC, HMBC, TOCSY, and ROESY. The synthetic product was also evaluated for its antimicrobial activity.https://doi.org/10.1002/open.202400175Beta-turnCyclopeptideSolid-phase synthesisSolution-phase synthesisTotal synthesis
spellingShingle Anderson Arnold Aloanis
Prof. Tati Herlina
Dr. Ari Hardianto
Prof. Rani Maharani
Total Synthesis of Cyclosenegalin A
ChemistryOpen
Beta-turn
Cyclopeptide
Solid-phase synthesis
Solution-phase synthesis
Total synthesis
title Total Synthesis of Cyclosenegalin A
title_full Total Synthesis of Cyclosenegalin A
title_fullStr Total Synthesis of Cyclosenegalin A
title_full_unstemmed Total Synthesis of Cyclosenegalin A
title_short Total Synthesis of Cyclosenegalin A
title_sort total synthesis of cyclosenegalin a
topic Beta-turn
Cyclopeptide
Solid-phase synthesis
Solution-phase synthesis
Total synthesis
url https://doi.org/10.1002/open.202400175
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AT drarihardianto totalsynthesisofcyclosenegalina
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