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
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.