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三嗪:药物发现和生物缀合的优势结构。

s-Triazine: A Privileged Structure for Drug Discovery and Bioconjugation.

机构信息

Peptide Science Laboratory, School of Chemistry and Physics, University of KwaZulu-Natal, Durban 4001, South Africa.

KwaZulu-Natal Research Innovation and Sequencing Platform (KRISP), School of Laboratory Medicine and Medical Sciences, College of Health Sciences, University of KwaZulu-Natal, Durban 4041, South Africa.

出版信息

Molecules. 2021 Feb 6;26(4):864. doi: 10.3390/molecules26040864.

DOI:10.3390/molecules26040864
PMID:33562072
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7914932/
Abstract

This review provides an overview of the broad applicability of s-triazine. Our many years working with this intriguing moiety allow us to discuss its wide activity spectrum (inhibition against MAO-A and -B, anticancer/antiproliferative and antimicrobial activity, antibacterial activity against MDR clinical isolates, antileishmanial agent, and use as drug nano delivery system). Most of the compounds addressed in our studies and those performed by other groups contain only -substitution. Exploiting the concept of orthogonal chemoselectivity, first described by our group, we have successfully incorporated different nucleophiles in different orders into s-triazine core for application in peptides/proteins at a temperature compatible with biological systems.

摘要

这篇综述概述了三嗪的广泛适用性。我们多年来一直致力于研究这一有趣的部分,因此能够讨论其广泛的活性谱(对 MAO-A 和 -B 的抑制作用、抗癌/抗增殖和抗菌活性、对 MDR 临床分离株的抗菌活性、抗利什曼原虫药物以及用作药物纳米传递系统)。我们研究过的大多数化合物和其他小组研究的化合物都只包含 -取代。利用我们小组首次描述的正交化学选择性概念,我们成功地按不同顺序将不同亲核试剂引入三嗪核心,以在与生物系统兼容的温度下应用于肽/蛋白质。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/43fa/7914932/0e6f53948cf5/molecules-26-00864-sch008.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/43fa/7914932/4294221b31d6/molecules-26-00864-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/43fa/7914932/85151b195827/molecules-26-00864-g003.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/43fa/7914932/67b686d8229b/molecules-26-00864-sch003.jpg
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