A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis

Véronique Dartois, Clifton E. Barry

Research output: Contribution to journalReview article

71 Scopus citations

Abstract

Tuberculosis is a bacterial disease that predominantly affects the lungs and results in extensive tissue pathology. This pathology contributes to the complexity of drug development as it presents discrete microenvironments within which the bacterium resides, often under conditions where replication is limited and intrinsic drug susceptibility is low. This consolidated pathology also results in impaired vascularization that limits access of potential lead molecules to the site of infection. Translating these considerations into a target-product profile to guide lead optimization programs involves implementing unique in vitro and in vivo assays to maximize the likelihood of developing clinically meaningful candidates.

Original languageEnglish (US)
Pages (from-to)4741-4750
Number of pages10
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number17
DOIs
StatePublished - Sep 1 2013

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Keywords

  • Drug discovery
  • Tuberculosis

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