TB Research

Pyrimidine derivatives with antitubercular activity

Finger V, Kufa M, Soukup O, Castagnolo D, Roh J, Korabecny J

European journal of medicinal chemistry · 2022-11

Abstract

Small molecules with antitubercular activity containing the pyrimidine motif in their structure have gained more attention after three drugs, namely GSK 2556286 (GSK-286), TBA-7371 and SPR720, have entered clinical trials. This review provides an overview of recent advances in the hit-to-lead drug discovery studies of antitubercular pyrimidine-containing compounds with the aim to highlight their structural diversity. In the first part, the review discusses the pyrimidine compounds according to their targets, pinpointing the structure-activity relationships of each pyrimidine family. The second part of this review is concentrated on antitubercular pyrimidine derivatives with a yet unexplored or speculative target, dividing the compounds according to their structural types.

MeSH terms

  • Mycobacterium tuberculosis
  • Pyrimidines
  • Antitubercular Agents
  • Structure-Activity Relationship
  • Drug Discovery