University of London

Mitsui Norin Co., Ltd.

School of Pharmacy

Paul Stapleton

Peter William Taylor

Yukihiko Hara

James C Anderson

Catherine Headley

Contemplated methods and compositions further increase susceptibility of sensitized MRSA against various antibiotic drugs. Most preferably, the MRSA is already sensitized with a galloylated catechin (e.g., ECG), and further sensitization is achieved by exposure to a non-galloylated catechin (e.g., EC), and most preferably the corresponding non-galloylated catechin.

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There is provided a novel compound of the general formula I in which each of Rto Ris hydrogen, aryl, Calkyl, trialkylsilyl or acyl; Rto Rare individually selected from hydrogen, hydroxy, Calkoxy and acyloxy; Rand Rare H, Calkyl, trialkylsilyl or acyl; X is O or NR, and R is H or Me; in which any of the alkyl groups including alkyl groups in alkoxy, acyl and acyloxy groups may be substituted by aryl, Calkyl, Calkoxy, hydroxyl, trialkylsiloxy or acyloxy groups; with the proviso that Rand Rare not both OH when Ris H or OH, Rand Rare both H, and X is O. The amide compounds (X is NR) are analogues of epigallocatechin gallate or epicatechin galate, with an amide bond in place of the natural ester bond, with resistance to hydrolysis by esterase enzymes. The ester compounds (X is O) have a different hydroxylation pattern on the B ring as compared to the natural products. The compounds may be used to modulate the resistance to &#x3b2;-lactam antibiotics of various infections, especially methicillin resistant(MRSA). Pharmaceutical compositions containing the novel compounds and combinations of the novel compounds and &#x3b2;-lactam antibiotics are described.

Compounds for use in the treatment of infection

Growing community of inventors

London, United Kingdom

Paul Stapleton