Behnsen Antonia, Hertrampf Gesa, Vojnović Sandra, Nikodinović-Runić Jasmina, Gulder Tobias A M
Chair of Technical Biochemistry, Technical University of Dresden Bergstraße 66 01069 Dresden Germany
Institute of Molecular Genetics and Genetic Engineering, University of Belgrade Vojvoded Stepe 444a Belgrade 11000 Serbia
RSC Adv. 2024 Nov 5;14(47):35215-35219. doi: 10.1039/d4ra05941g. eCollection 2024 Oct 29.
The rapid emergence of antibiotic resistance in recent years poses a substantial global health threat. Thus, the discovery of potent novel antibiotics is of utmost importance. One such compound class with promising antibiotic potential are the myxocoumarins from MYX-030, which exhibit exceptional antibiotic activities against several Gram-positive pathogens, including MRSA. Interestingly, the synthetic chromene dione precursors lacking the alkyl side chain also display promising antibiotic potential. Within this work, a focused library of chromene diones resembling the myxocoumarin A core structure was synthesized to explore structure-activity relationships. We were able to identify derivatives equipotent to the natural product but devoid of the alkyl chain and the nitro substituent to significantly facilitate synthetic access.
近年来抗生素耐药性的迅速出现对全球健康构成了重大威胁。因此,发现强效新型抗生素至关重要。一类具有潜在抗生素潜力的化合物是来自MYX - 030的粘质香豆素,它们对包括耐甲氧西林金黄色葡萄球菌(MRSA)在内的几种革兰氏阳性病原体表现出优异的抗生素活性。有趣的是,缺乏烷基侧链的合成色烯二酮前体也显示出有前景的抗生素潜力。在这项工作中,合成了一个类似于粘质香豆素A核心结构的色烯二酮聚焦文库,以探索构效关系。我们能够鉴定出与天然产物等效但没有烷基链和硝基取代基的衍生物,从而显著促进合成途径。