Anionic Cyclophanes as Potential Reversal Agents of Muscle Relaxants by Chemical Chelation

Cameron, Kenneth S.; Fielding, Lee A.; Mason, Rona; Muir, Alan W.; Rees, David C.; Thorn, Simon N.; Zhang, Ming Qiang

doi:10.1016/s0960-894x(02)00017-3

Cited by 22 publications

(15 citation statements)

References 17 publications

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“…Compound 7 was obtained according to literature methods (Cameron et al, 2002; Guo et al, 2005). Briefly, MDSA (1 g) was dissolved in 20 mL of methanol and then 1 mL of HCl (~10 M) was added.…”

Section: Methodsmentioning

confidence: 99%

Targeting MgrA-Mediated Virulence Regulation in Staphylococcus aureus

Sun

Zhou

Bing

et al. 2011

Chemistry & Biology

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SUMMARY 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 which identified 5, 5-methylenedisalicylic acid (MDSA) that 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.

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Section: Methodsmentioning

confidence: 99%

Targeting MgrA-Mediated Virulence Regulation in Staphylococcus aureus

Sun

Zhou

Bing

et al. 2011

Chemistry & Biology

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“…For the chemistry and applications of methylene bisphenol derivatives, see: Ogata et al (1975); Mé ric et al (1993); Shrestha et al (2007); Cameron et al (2002). For the preparation, see: Cushman & Kanamathareddy (1990); Mé ric et al (1993).…”

Section: Related Literaturementioning

confidence: 99%

Dimethyl 5,5′-methylenebis(2-hydroxybenzoate)

2012

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In the title compound, C17H16O6, the two methyl salicylate moieties are related by crystallographic twofold rotational symmetry with the two benzene rings close to being perpendicular [inter-ring dihedral angle = 86.6 (8)°]. Intramolecular phenolic O—H⋯O hydrogen bonds with carboxyl O-atom acceptors are present, with these groups also involved in centrosymmetric cyclic intermolecular O—H⋯O hydrogen-bonding associations [graph set R 2 2(4)], giving infinite chains extending across (101).

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“…A possible mechanism to control the duration of the block is removal of the NMB drug by means of chemical chelation. 3 A modified -cyclodextrin, Org 25969, is being developed as a potent and rapid reversal agent for rocuronium bromide.…”

Section: Introductionmentioning

confidence: 99%