- Structure-Activity Relationship and Anticancer Profile of Second-Generation Anti-MRSA Synthetic Retinoids
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We previously reported the antibacterial activity of CD437, a known antitumor compound. It proved to be a potent antimicrobial agent effective against both growing and persister cells of methicillin-resistant Staphylococcus aureus (MRSA). Herein, we report the synthesis of a panel of analogs and their effect on both MRSA and cancer cells. The hydrophobic group of the parent compound was varied in steric bulk, and lipid-mimicking analogs were tested. Biological assessment confirmed that the adamantane moiety is the most effective substitution for antibacterial activity, and some preferential action in cancer over MRSA was achieved.
- Cheng, Ana V.,Kim, Wooseong,Escobar, Iliana E.,Mylonakis, Eleftherios,Wuest, William M.
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supporting information
p. 393 - 397
(2020/03/31)
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- A novel mesoporous hydrogen-bonded organic framework with high porosity and stability
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A highly stable hydrogen-bonded organic framework, HOF-14, has been successfully constructed and structurally characterized. It possesses a permanent three dimensional (3D) porous structure. The activated HOF-14 has a high BET surface area of 2573 m2 g-1 and a record large pore volume of 1.36 cm3 g-1 among HOF materials. In addition, HOF-14 also exhibits high chemical and thermal stability and is capable of highly selective separation of light hydrocarbons under ambient conditions.
- Wang, Bin,Lv, Xiu-Liang,Lv, Jie,Ma, Li,Lin, Rui-Biao,Cui, Hui,Zhang, Jian,Zhang, Zhangjing,Xiang, Shengchang,Chen, Banglin
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supporting information
p. 66 - 69
(2019/12/25)
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- N - heterocyclic compound, intermediate, preparation method, pharmaceutical composition and application (by machine translation)
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The invention discloses a N - heterocyclic compound, intermediate, preparation method, pharmaceutical composition and application. The invention of SHP2 N - heterocyclic compound to have high selectivity, can effectively inhibit the cell in the SHP2 downstream signal path ERK phosphorylation level, to tumor cells has very good inhibition activity, it has broad drug development prospects; its preparation method is simple, mild reaction conditions, high yield and purity, after treatment is simple, environmental protection, and is favorable for industrial production. (by machine translation)
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- BIARYL DERIVATIVE AS GPR120 AGONIST
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The present invention relates to a biaryl derivative expressed by the chemical formula 1, a method for producing the biaryl derivative, a pharmaceutical composition comprising same, and use of same, the biaryl derivative expressed by the chemical formula 1, as a GPR120 agonist, promoting GLP-1 generation in the gastro-intestinal tract, reducing insulin resistance in the liver, muscles and the like from anti-inflammatory activity in the macrophage, pancreatic cells and the like, and allowing effective use in prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.
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Paragraph 0065; 0314
(2017/11/17)
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- NAPHTHYLAMIDE COMPOUND, PREPARATION METHOD AND USE THEREOF
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The present invention relates to a naphthylamide compound of the structure as represented by formula (I), medicinal salts, prodrugs and hydrates or solvates thereof, and also relates to a method of preparing the compounds, pharmaceutical compositions comp
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Paragraph 0025; 0122
(2017/01/09)
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- HETEROCYCLIC PROLINAMIDE DERIVATIVES
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This invention is directed to novel heterocyclic prolinamide derivatives of Formula (I), and pharmaceutically acceptable salts, solvates, solvates of the salt and prodrugs thereof, useful in the prevention (e.g., delaying the onset of or reducing the risk of developing) and treatment (e.g., controlling, alleviating, or slowing the progression of) of age-related macular degeneration (AMD) and related diseases of the eye. These diseases include dry-AMD, wet-AMD, geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells. The invention disclosed herein is further directed to methods of prevention, slowing the progress of, and treatment of dry-AMD, wet-AMD, and geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells, comprising: administration of a therapeutically effective amount of compound of the invention. The compounds of the invention are inhibitors of HTRAl. Thus, the compounds of the invention are useful in the prevention and treatment of a wide range of diseases mediated (in whole or in part) by HTRAl. The compounds of the invention are also useful for inhibiting HTRAl protease activity in an eye or locus of an arthritis or related condition.
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Paragraph 0264; 0266
(2018/04/11)
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- Highly Stable Zr(IV)-Based Metal-Organic Frameworks for the Detection and Removal of Antibiotics and Organic Explosives in Water
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Antibiotics and organic explosives are among the main organic pollutants in wastewater; their detection and removal are quite important but challenging. As a new class of porous materials, metal-organic frameworks (MOFs) are considered as a promising platform for the sensing and adsorption applications. In this work, guided by a topological design approach, two stable isostructural Zr(IV)-based MOFs, Zr6O4(OH)8(H2O)4(CTTA)8/3 (BUT-12, H3CTTA = 5′-(4-carboxyphenyl)-2′,4′,6′-trimethyl-[1,1′:3′,1″-terphenyl]-4,4″-dicarboxylic acid) and Zr6O4(OH)8(H2O)4(TTNA)8/3 (BUT-13, H3TTNA = 6,6′,6″-(2,4,6-trimethylbenzene-1,3,5-triyl)tris(2-naphthoic acid)) with the the-a topological structure constructed by D4h 8-connected Zr6 clusters and D3h 3-connected linkers were designed and synthesized. The two MOFs are highly porous with the Brunauer-Emmett-Teller surface area of 3387 and 3948 m2 g-1, respectively. Particularly, BUT-13 features one of the most porous water-stable MOFs reported so far. Interestingly, these MOFs represent excellent fluorescent properties, which can be efficiently quenched by trace amounts of nitrofurazone (NZF) and nitrofurantoin (NFT) antibiotics as well as 2,4,6-trinitrophenol (TNP) and 4-nitrophenol (4-NP) organic explosives in water solution. They are responsive to NZF and TNP at parts per billion (ppb) levels, which are among the best performing luminescent MOF-based sensing materials. Simultaneously, both MOFs also display high adsorption abilities toward these organic molecules. It was demonstrated that the adsorption plays an important role in the preconcentration of analytes, which can further increase the fluorescent quenching efficiency. These results indicate that BUT-12 and -13 are favorable materials for the simultaneous selective detection and removal of specific antibiotics and organic explosives from water, being potentially useful in monitoring water quality and treating wastewater.
- Wang, Bin,Lv, Xiu-Liang,Feng, Dawei,Xie, Lin-Hua,Zhang, Jian,Li, Ming,Xie, Yabo,Li, Jian-Rong,Zhou, Hong-Cai
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supporting information
p. 6204 - 6216
(2016/06/09)
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- A robust doubly interpenetrated metal-organic framework constructed from a novel aromatic tricarboxylate for highly selective separation of small hydrocarbons
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A microporous metal-organic framework, for the first time, has been developed for highly selective separation of industrially important C 1, C2 and C3 hydrocarbons at room temperature.
- He, Yabing,Zhang, Zhangjing,Xiang, Shengchang,Fronczek, Frank R.,Krishna, Rajamani,Chen, Banglin
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supporting information; experimental part
p. 6493 - 6495
(2012/08/08)
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- A modular molecular tweezer designed using CAVEAT
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A pair of water-soluble molecular tweezers designed using the computer program CAVEAT were prepared and their binding to an N-ethylquinolinium cation was demonstrated by 1H NMR spectroscopy. The Royal Society of Chemistry 2006.
- Huang, Haidong,Drueckhammer, Dale G.
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p. 2995 - 2997
(2008/09/19)
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- AMINOALCOHOL DERIVATIVES
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The present invention relates to a compound of the formula [I]: wherein (a), in which -Y-, R4, R5 and R6 are4 R5each as defined in the description, etc., R1 is hydrogen, halogen, lower alkyl, hydroxy, etc., R2 is hydrogen, lower alkyl or hydroxy(lower)alkyl, R3 is hydrogen or an amino protective group, 20 R7 is hydrogen, lower alkyl, cyclo(lower)alkyl, lower R9 alkenyl, -Z-R9 or (b), in which -Z- is -0-, -S-, R9 -SO- or -SO2-, and each R9 is independently hydrogen, lower alkyl, cyclo(lower)alkyl, etc., and R8 is -D-E-R10, in which -D- is -CONHSO2- or -S02NHCO-, E is bond or lower alkylene, and R10is halogen, cyano, carboxy, etc., or a prodrug thereof or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of ulcer, overactive bladder, and the like.
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Page/Page column 74
(2010/10/20)
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