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Bromotyrosine-derived natural and synthetic products as inhibitors of mycothiol-S-conjugate amidase

Academic Article
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Overview

related to degree

  • Hughes, Robert Owen, Ph.D. in Chemistry, Scripps Research 1997 - 2002
  • Pfefferkorn, Jeff, Ph.D. in Chemistry, Scripps Research 1997 - 2001

authors

  • Nicholas, G. M.
  • Eckman, L. L.
  • Ray, S.
  • Hughes, Robert Owen
  • Pfefferkorn, Jeff
  • Barluenga, S.
  • Nicolaou, K.C.
  • Bewley, C. A.

publication date

  • September 2002

journal

  • Bioorganic & Medicinal Chemistry Letters  Journal

abstract

  • A series of bromotyrosine-derived compounds, including marine natural products and members of a psammaplin A-inspired combinatorial synthetic library, were screened for their ability to inhibit the Mycobacterium tuberculosis detoxification enzyme mycothiol-S-conjugate amidase (MCA). Correlations between the structures and their respective IC(50) values (which range from 3 microM to 2.7 mM) should prove valuable when optimizing more potent inhibitors of MCA.

subject areas

  • Amidohydrolases
  • Anti-Bacterial Agents
  • Enzyme Inhibitors
  • Inhibitory Concentration 50
  • Mycobacterium tuberculosis
  • Structure-Activity Relationship
  • Tyrosine
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Identity

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/s0960-894x(02)00385-2

PubMed ID

  • 12161164
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Additional Document Info

start page

  • 2487

end page

  • 2490

volume

  • 12

issue

  • 17

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