Fascaplysin derivatives binding to DNA via unique cationic five-ring coplanar backbone showed potent antimicrobial/antibiofilm activity against MRSA in vitro and in vivo

Derivatization of Marine‐Derived Fascaplysin via Highly Regioselective Suzuki‐Miyaura Coupling Contributing to the Enhanced Antibacterial Activity

“…Interestingly, compared with published amide series of fascaplysin derivatives (Table 3), [11] the results showed that derivatives synthesized by coupling reaction have a wider range of excellent antibacterial activity, especially against Gram-negative E coli (ATCC 25922). In this study, the most active compound 17 d was 32 times more active against E coli (ATCC 25922) than the naphthylamide fascaplysin derivative (MIC 1.56 vs 50 μg/mL).…”

“…[27] We have found that amide-functionalized fascaplysin derivatievs exhibit excellent antibacterial activity. [11] Therefore, the biological activity of these newly synthesized compounds in this work was preliminarily evaluated by minimum inhibitory concentration (MIC). The solvent dimethyl sulfoxide (DMSO) was used as the negative control, besides, vancomycin and colistin were worked as positive controls for Gram-positive bacteria MRSA (ATCC 43300) and Gram-negative bacteria Escherichia coli (ATCC 25922), respectively.…”

“…[9] In addition, lately, we also found that 9methylfascaplysin could be used in the treatment of ischemic stroke, [10] while amide-modified fascaplysin derivatives showed potency against MRSA. [11] All these results reveal that the unique backbone of fascaplysin plays a key role in their bioactivities and structural modification at the C6 position of βcarboline A ring would impose powerful influence on the biological properties. Motivated by these achievements, we initiate study of the synthesis and bioactivity exploration of new fascaplysin derivatives, which could own strong potent bioactivities and suitable physicochemical properties.…”

Quaternary ammonia compounds in disinfectant products: evaluating the potential for promoting antibiotic resistance and disrupting wastewater treatment plant performance

“…75 Meanwhile, a newly synthesized mono-cationic QAC has been found to bind with DNA to block the synthesis of enzyme and receptor, and inhibit the migration of genomic DNA. 76,77…”

“…75 Meanwhile, a newly synthesized mono-cationic QAC has been found to bind with DNA to block the synthesis of enzyme and receptor, and inhibit the migration of genomic DNA. 76,77 2.2 Tolerance and resistance to QACs Generally speaking, tolerance is the capacity of microorganisms to survive a transient exposure to antibiotics or disinfectants without a change in the mini MIC. 78 Understanding when microorganisms are more tolerant to QACs could mean that a greater exposure time to QACs, rather than a greater concentration of QACs, is required to produce the same extent of disinfection.…”