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作为抗菌剂的阿比西尼亚霉素C截短衍生物的合成与生物学评价

Synthesis and biological evaluation of truncated derivatives of abyssomicin C as antibacterial agents.

作者信息

Monjas Leticia, Fodran Peter, Kollback Johanna, Cassani Carlo, Olsson Thomas, Genheden Maja, Larsson D G Joakim, Wallentin Carl-Johan

机构信息

Department of Chemistry and Molecular Biology, University of Gothenburg, Kemigården 4, 412 96, Gothenburg, Sweden.

Centre for Antibiotic Resistance Research (CARe), University of Gothenburg, Gothenburg, Sweden.

出版信息

Beilstein J Org Chem. 2019 Jul 2;15:1468-1474. doi: 10.3762/bjoc.15.147. eCollection 2019.

DOI:10.3762/bjoc.15.147
PMID:31354863
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6633193/
Abstract

The synthesis and antibacterial activity of two new highly truncated derivatives of the natural product abyssomicin C are reported. This work outlines the limits of structural truncation of the natural product and consequently provides insights for further structure-activity relationship studies towards novel antibiotics targeting 4-amino-4-deoxychorismate (ADC) synthase. Specifically, it is demonstrated that the synthetically challenging bicyclic motif is essential for activity towards methicillin-resistant (MRSA).

摘要

报道了天然产物阿比西尼亚霉素C的两种新型高度截短衍生物的合成及其抗菌活性。这项工作概述了天然产物结构截短的限度，从而为针对4-氨基-4-脱氧分支酸（ADC）合酶的新型抗生素的进一步构效关系研究提供了见解。具体而言，已证明具有合成挑战性的双环基序对于对耐甲氧西林金黄色葡萄球菌（MRSA）的活性至关重要。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e1e9/6633193/3862e907869e/Beilstein_J_Org_Chem-15-1468-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e1e9/6633193/b967321a3aee/Beilstein_J_Org_Chem-15-1468-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e1e9/6633193/6dc3cf05d18a/Beilstein_J_Org_Chem-15-1468-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e1e9/6633193/2fd3344ca9c3/Beilstein_J_Org_Chem-15-1468-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e1e9/6633193/b0df47781f72/Beilstein_J_Org_Chem-15-1468-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e1e9/6633193/53af2df45ee2/Beilstein_J_Org_Chem-15-1468-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e1e9/6633193/3862e907869e/Beilstein_J_Org_Chem-15-1468-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e1e9/6633193/b967321a3aee/Beilstein_J_Org_Chem-15-1468-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e1e9/6633193/6dc3cf05d18a/Beilstein_J_Org_Chem-15-1468-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e1e9/6633193/2fd3344ca9c3/Beilstein_J_Org_Chem-15-1468-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e1e9/6633193/b0df47781f72/Beilstein_J_Org_Chem-15-1468-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e1e9/6633193/53af2df45ee2/Beilstein_J_Org_Chem-15-1468-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e1e9/6633193/3862e907869e/Beilstein_J_Org_Chem-15-1468-g007.jpg

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