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多杂环肽模拟物：寡环胍的平行固相合成及其对结核分枝杆菌 DNA 回旋酶的抑制活性。

Polyheterocyclic peptidomimetics: Parallel solid phase synthesis of oligo cyclic guanidines and their inhibition activity against Mycobacterium tuberculosis DNA gyrase.

机构信息

Center for Translational Science, Florida International University, 11350 SW Village Parkway, Port Saint Lucie, FL 34987, USA.

Department of Chemistry & Biochemistry, Florida International University, 11200 SW 8th Street, Miami, FL 33199, USA.

出版信息

Bioorg Med Chem Lett. 2023 Sep 1;93:129439. doi: 10.1016/j.bmcl.2023.129439. Epub 2023 Aug 8.

DOI:10.1016/j.bmcl.2023.129439
PMID:37557925
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10993493/
Abstract

Polyheterocycles are one of the most desired synthetic targets due to their numerous and valuable applications in various fields. We report the design and the parallel synthesis of novel linear oligocyclic guanidine peptidomimetics from predesigned reduced polyamides. A screening of these compounds identified active Mycobacterium tuberculosis DNA gyrase inhibitors which do not inhibit human DNA topoisomerase IIα and topoisomerase I.

摘要

多杂环化合物因其在各个领域的广泛应用而成为最受关注的合成目标之一。我们设计并平行合成了新型线性寡环胍肽模拟物，这些模拟物是由预先设计的还原聚酰胺衍生而来的。对这些化合物进行筛选，鉴定出了新型结核分枝杆菌 DNA 拓扑异构酶抑制剂，它们不抑制人源 DNA 拓扑异构酶 IIα 和拓扑异构酶 I。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2288/10993493/41987d595c59/nihms-1923598-f0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2288/10993493/3a18db22aed5/nihms-1923598-f0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2288/10993493/2e6c914014f1/nihms-1923598-f0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2288/10993493/55a3af9874b5/nihms-1923598-f0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2288/10993493/7e21e706ee63/nihms-1923598-f0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2288/10993493/41987d595c59/nihms-1923598-f0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2288/10993493/3a18db22aed5/nihms-1923598-f0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2288/10993493/2e6c914014f1/nihms-1923598-f0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2288/10993493/55a3af9874b5/nihms-1923598-f0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2288/10993493/7e21e706ee63/nihms-1923598-f0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2288/10993493/41987d595c59/nihms-1923598-f0006.jpg

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