6790-21-2Relevant articles and documents
ANTIBACTERIAL AGENTS AGAINST DRUG-RESISTANT STAPHYLOCOCCUS AUREUS OR VANCOMYCIN-RESISTANT ENTEROCOCCUS AND ANTIFUNGAL AGENTS COMPRISING STEPHANITIS SVENSONI-DERIVED POLYKETIDE OR SYNTHETIC ANALOGS THEREOF
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Paragraph 0043; 0045-0042, (2020/10/27)
PROBLEM TO BE SOLVED: To provide antibacterial or antifungal agents comprising a naturally occurring substance or synthetic analogs thereof having high antibacterial activity against methicillin-resistant Staphylococcus aureus or vancomycin-resistant Ente
Structure-activity relationships and optimization of acyclic acylphloroglucinol analogues as novel antimicrobial agents
Tan, Haibo,Liu, Hongxin,Zhao, Liyun,Yuan, Yao,Li, Bailin,Jiang, Yueming,Gong, Liang,Qiu, Shengxiang
supporting information, p. 492 - 499 (2016/10/04)
Methicillin-resistant Staphylococcus aureus (MRSA) poses a serious threat to global public health, because it exhibits resistance to existing antibiotics and therefore high rates of morbidity and mortality. In this study, twenty-one natural product-based acylphloroglucinol congeners were synthesized, which possessed different side chains. Antibacterial screening against MRSA strains revealed that acyl moiety tailoring is a prerequisite for the antibacterial activity. Moreover, the lipophilicity, rather than the magnitude of the hydrophobic acyl tail dominates variability in activity potency. Compound 11j was identified as a promising lead for the generation of new anti-MRSA drug development. It was discovered by optimization of the side chain length in light of the potency, the breadth of the antibacterial spectrum, the rate of bactericidal action, as well as the membrane selectivity. Compound 11j exerted profound in?vitro antibacterial activity against the MRSA strain (JCSC 2172), and its MIC was 3-4 orders of magnitude lower than that of vancomycin. A preliminary mode of action study of compound 11j at the biophysical and morphology levels disclosed that the mechanism underlying its anti-MRSA activity included membrane depolarization and, to a lesser extent, membrane disruption and cell lysis.
Simplified YM-26734 inhibitors of secreted phospholipase A2 group IIA
Oslund, Rob C.,Cermak, Nathan,Verlinde, Christophe L.M.J.,Gelb, Michael H.
supporting information; experimental part, p. 5415 - 5419 (2009/05/30)
Simplified analogs of YM-26734, a known inhibitor of secreted phospholipase A2 (sPLA2) group IIA, were synthesized and found to also display potent inhibition at low nanomolar concentrations. Analogs were based on the didodecanoylphl
