Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2011-04-19
2011-04-19
Chung, Susannah (Department: 1626)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S438000, C546S190000, C546S199000, C564S123000
Reexamination Certificate
active
07928129
ABSTRACT:
New carboxyphenyl-glycylboronic acid transition-state analog inhibitors, representative of a class of compounds effective against class C β-lactamase AmpC. The new compounds improve inhibition by over two-orders of magnitude compared to analogous glycylboronic acids, with Ki values as low as 1 nM.
REFERENCES:
patent: 4963655 (1990-10-01), Kinder et al.
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Powers et al., Structures of Ceftazidime and its Transitional state analogues in complex with AmpC β-Lactamase, Biochemistry, vol. 40, pp. 9207-9214, 2001.
Sperka, et al., Bioorganic & Medicinal Chemistry Letters, 15, 2005, 3086-3090, especially p. 3086, Col. 1, second paragraph.
Powers, et al., “The complexed structure and antimicrobial activity of a non β-lactamase inhibitor of AmpC β-lactamase” Protein Science, 8, 2330-2337, published 1999.
Weston, et al., “Structure-based enhancement of boronic acid-based inhibitors of AmpC β-lactmase” J. Med. Chem., 41, 4577-4586, 1998.
Morandi, et al., “Nanomolar Inhibitors of AmpC β-lactamase” JACS, 125, 685-695, 2003.
Powers, et al. Structures of Cefazidime and Its Transition-State Analogue in Complex with AmpC β-Lactamase: Implications for Resistance Mutations and Inhibitor Design, Biochemistry, 40, 9207-9214, published on web Jul. 10, 2001.
Kinder, et al. “Acylamido boronic acids and difluoroborane analogs of amino acids,” M. Med. Chem. vol. 28, pp. 1917-1925, 1985.
Prati Fabrio
Shoichet Brian K.
Chung Susannah
Northwestern University
Reinhart Boerner Van Deuren s.c.
University of Modena
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