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␤ 2 -Glycoprotein I ( ␤ 2 -GPI) is a major antigen for anticardiolipin antibodies (aCL, Abs) present in patients with antiphospholipid syndrome. We recently reported that ␤ 2 -GPI specifically binds to oxidized LDL (oxLDL) and that the ␤ 2 -GPI's major ligand, oxLig-1 is 7-ketocholesteryl-9-carboxynonanoate (Kobayashi, K., E. Matsuura, Q. P.

A structure-guided molecular design approach was used to optimize quercetin diacylglycoside analogues that inhibit bacterial DNA gyrase and topoisomerase IV and show potent antibacterial activity against a wide spectrum of relevant pathogens responsible for hospital- and community-acquired infections. In this paper, such novel 3,7-diacylquercetin, quercetin 6''-acylgalactoside, and quercetin 2'',6''-diacylgalactoside analogues of lead compound 1 were prepared to assess their target specificities and preferences in bacteria. The significant enzymatic inhibition of both Escherichia coli DNA gyrase and Staphylococcus aureus topoIV suggest that these compounds are dual inhibitors. Most of the investigated compounds exhibited pronounced inhibition with MIC values ranging from 0.13 to 128 μg/mL toward the growth of multidrug-resistant Gram-positive methicillin-resistant S. aureus, methicillin sensitive S. aureus, vancomycin-resistant enterococci (VRE), vancomycin intermediate S. aureus, and Streptococcus pneumoniae bacterial strains. Structure-activity relationship studies revealed that the acyl moiety was absolutely essential for activity against Gram-positive organisms. The most active compound 5i was 512-fold more potent than vancomycin and 16-32-fold more potent than 1 against VRE strains. It also has realistic in situ intestinal absorption in rats and showed very low acute toxicity in mice. So far, this compound can be regarded as a leading antibacterial agent.

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Aminopropyl silica gels were modified with two porphyrin derivatives and five phthalocyanine derivatives. The modified silica gels were evaluated for the usefulness as high-performance liquid chromatography stationary phases for the separation of π-electron-rich polyaromatic hydrocarbons (PAHs) such as naphthalene and phenanthrene. As a result of the modification, the aminopropyl silica gels acquired a function of π–π electron interaction with PAHs. In particular, the aminopropyl silica gel modified with copper phthalocyanine (Cu-PCS) showed the strongest π–π electron interaction with PAHs. It was the most suited as a stationary phase for the separations of PAHs among the modified silica gels tested. The Cu-PCS column could be utilized for the separation of π-electron-rich compounds including medicines, mutagens, and pollutants.