Synthesis and antibiotic potential of myxocoumarin-inspired chromene dione analogs

Abstract

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 Stigmatella aurantiaca 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.