4.5 Review

Oxadiazole scaffolds in anti-tuberculosis drug discovery

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 29, Issue 16, Pages 1999-2007

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.06.054

Keywords

Tuberculosis; Oxadiazole; Regioisomer; Bioisoster; Linker

Funding

  1. University Grants Commission, India [F.25-1/2014-15(BSR), F.5-63/2007(BSR)]
  2. DST-INSPIRE, India [IF130396]

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With the increasing number of cases of latent and drug resistant tuberculosis, there is an urgent need to develop new, potent molecules capable of combating this deadly disease. Molecules containing oxadiazoles are one such class that could be considered to fulfil this need. Oxadiazole regioisomers have been explored in drug discovery programs for their ability to act as effective linkers and also as pharmacophoric features. Oxadiazoles can act as bioisosteric replacements for the hydrazide moiety which can be found in first line anti-TB drugs, and some have been also reported to interact with newer anti-TB targets. In this context, the present review describes the potential of oxadiazoles as antituberculosis agents.

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