28505-57-9Relevant academic research and scientific papers
Targeting MgrA-mediated virulence regulation in Staphylococcus aureus
Sun, Fei,Zhou, Lu,Zhao, Bing-Chuan,Deng, Xin,Cho, Hoonsik,Yi, Chengqi,Jian, Xing,Song, Chun-Xiao,Luan, Chi-Hao,Bae, Taeok,Li, Zigang,He, Chuan
, p. 1032 - 1041 (2011)
Increasing antibiotic resistance in human pathogens necessitates the development of new approaches against infections. Targeting virulence regulation at the transcriptional level represents a promising strategy yet to be explored. A global transcriptional regulator, MgrA in Staphylococcus aureus, was identified previously as a key virulence determinant. We have performed a fluorescence anisotropy (FA)-based high-throughput screen that identified 5, 5-methylenedisalicylic acid (MDSA), which blocks the DNA binding of MgrA. MDSA represses the expression of α-toxin that is up-regulated by MgrA and activates the transcription of protein A, a gene down-regulated by MgrA. MDSA alters bacterial antibiotic susceptibilities via an MgrA-dependent pathway. A mouse model of infection indicated that MDSA could attenuate S. aureus virulence. This work is a rare demonstration of utilizing small molecules to block protein-DNA interaction, thus tuning important biological regulation at the transcriptional level.
Crystallization-induced light-emission enhancement of diphenylmethane derivatives
Guieu, Samuel,Rocha, Jo?o,Silva, Artur M.S.
, p. 9329 - 9334 (2013/10/01)
A family of diphenylmethane derivatives has been synthesized and their luminescence properties characterized. While in solution the compounds are weakly emissive, showing no aggregation-induced emission enhancement, the crystals of three dialkyl 5,5′-methylenebis(2-hydroxybenzoate) samples exhibit intense emission. This emission enhancement upon crystallization is ascribed to particular molecular packing, which stiffens the structure of the compounds via hydrogen bonds, preventing consecutive π-π interactions.
NEW METHYLENEBISPHENYL COMPOUNDS USEFUL IN THE TREATMENT OF INFLAMMATION
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Page/Page column 53, (2008/12/07)
There is provided compounds of formula (I), wherein Rx, Ry, X1, X2, L1, L2, Y1 and Y2 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.
Methylenedisalicylic acid derivatives: New PTP1B inhibitors that confer resistance to diet-induced obesity
Shrestha, Suja,Bhattarai, Bharat Raj,Chang, Kyung Ja,Lee, Keun-Hyeung,Cho, Hyeongjin
, p. 2760 - 2764 (2008/02/04)
Methylenedisalicylic acid derivatives were synthesized and their inhibitory activities against protein tyrosine phosphatases (PTPases) examined. Two of the compounds, 8 and 9, showed Ki values of 9.4 and 6.3 μM against PTP1B, 4- and 7-fold lower values compared to those against TC-PTP. They were reversible and slow-binding inhibitors against PTP1B. When compound 8 was fed to a mouse model, the weight gain and adipocyte fat storage induced by a high-fat-diet were significantly suppressed.
Use of chemical chelators as reversal agents for drug-induced neuromuscular block
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Page/Page column 13, (2008/06/13)
The invention relates to the use of chemical chelators for the preparation of a medicament for the reversal of drug-induced neuromuscular block, to a kit for providing neuromuscular block and its reversal, and to cyclophane derivatives having general formula (A) wherein R is (a), (b) or (c); or general formula (B) wherein X is (a), (b) or (d), or a pharmaceutically acceptable salt thereof.
Anionic cyclophanes as potential reversal agents of muscle relaxants by chemical chelation
Cameron, Kenneth S.,Fielding, Lee,Mason, Rona,Muir, Alan W.,Rees, David C.,Thorn, Simon,Zhang, Ming-Qiang
, p. 753 - 755 (2007/10/03)
A series of carboxyl-containing cyclophanes have been designed and synthesised as chemical chelators (or host molecules) of cationic muscle relaxant drugs (or guest molecules). Three of these cyclophane derivatives, 1-3, have been shown by NMR to form 1:1 complexes with the muscle relaxants pancuronium, 4 and gallamine, 5 in D2O, with association constants up to 104 M-1. When tested in an in vitro chick biventer muscle preparation, the cyclophanes reversed the neuromuscular block induced by pancuronium and gallamine, with 3 having the most effective reversal against pancuronium (EC50 40 μM).
