TB Research

Pyrazole and imidazo[1,2-b]pyrazole Derivatives as New Potential Antituberculosis Agents

Meta E, Brullo C, Tonelli M, Franzblau SG, Wang Y, Ma R, Baojie W, Orena BS, et al. (10 authors)

Medicinal chemistry (Shariqah (United Arab Emirates)) · 2019-01

Abstract

Background We screened a large library of differently decorated imidazo-pyrazole and pyrazole derivatives as possible new antitubercular agents and this preliminary screening showed that many compounds are able to totally inhibit Mycobacterium growth (>90 %). Among the most active compounds, we selected some new possible hits based on their similarities and, at the same time, on their novelty with respect to the pipeline drugs. Methods In order to increase the potency and obtain more information about structure-activity relationship (SAR), we designed and synthesized three new series of compounds (2a-e, 3a-e, and 4a-l). Conclusion Performed tests confirmed that both new pyrazoles and imidazo-pyrazoles could represent a new starting point to obtain more potent compounds and further work is now underway to identify the protein targets of this new class of anti-TB agents.

MeSH terms

  • Vero Cells
  • Animals
  • Mycobacterium tuberculosis
  • Imidazoles
  • Pyrazoles
  • Antitubercular Agents
  • Microbial Sensitivity Tests
  • Structure-Activity Relationship
  • Small Molecule Libraries
  • Chlorocebus aethiops