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

2019 ◽  
Vol 15 (1) ◽  
pp. 17-27 ◽  
Author(s):  
Elda Meta ◽  
Chiara Brullo ◽  
Michele Tonelli ◽  
Scott G. Franzblau ◽  
Yuehong Wang ◽  
...  

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. </P><P> 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.

2005 ◽  
Vol 15 (3) ◽  
pp. 527-530 ◽  
Author(s):  
Michel Belley ◽  
Michel Gallant ◽  
Bruno Roy ◽  
Karine Houde ◽  
Nicolas Lachance ◽  
...  

2017 ◽  
Vol 130 ◽  
pp. 419-432 ◽  
Author(s):  
Jan Němeček ◽  
Pavel Sychra ◽  
Miloslav Macháček ◽  
Markéta Benková ◽  
Galina Karabanovich ◽  
...  

Planta Medica ◽  
1998 ◽  
Vol 64 (06) ◽  
pp. 511-515 ◽  
Author(s):  
Masahiro Kitaoka ◽  
Hiroshi Kadokawa ◽  
Machiko Sugano ◽  
Kazuo Ichikawa ◽  
Motohiko Taki ◽  
...  

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