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Comprehensive physicochemical, pharmacokinetic and activity profiling of anti-TB agents
Author(s) -
Suresh B. Lakshminarayana,
Tan Bee Huat,
Paul C. Ho,
Ujjini H. Manjunatha,
Véronique Dartois,
Thomas Dick,
Srinivasa P. S. Rao
Publication year - 2014
Publication title -
journal of antimicrobial chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.124
H-Index - 194
eISSN - 1460-2091
pISSN - 0305-7453
DOI - 10.1093/jac/dku457
Subject(s) - pharmacokinetics , potency , pharmacology , bioavailability , in vivo , drug discovery , drug , metabolic stability , chemistry , in vitro , medicine , biology , biochemistry , microbiology and biotechnology
The discovery and development of TB drugs has met limited success, with two new drugs approved over the last 40 years. Part of the difficulty resides in the lack of well-established in vitro or in vivo targets of potency and physicochemical and pharmacokinetic parameters. In an attempt to benchmark and compare such properties for anti-TB agents, we have experimentally determined and compiled these parameters for 36 anti-TB compounds, using standardized and centralized assays, thus ensuring direct comparability across drugs and drug classes.

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