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Medicinal Chemistry

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ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

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Research Article

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

Author(s): Elda Meta, Chiara Brullo*, Michele Tonelli, Scott G. Franzblau, Yuehong Wang, Rui Ma, Wan Baojie, Beatrice S. Orena, Maria R. Pasca and Olga Bruno

Volume 15, Issue 1, 2019

Page: [17 - 27] Pages: 11

DOI: 10.2174/1573406414666180524084023

Price: $65

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.

Keywords: Pyrazole, imidazo[1, 2-b]pyrazole, antitubercular agents, MABA, LORA, Tuberculosis (TB).

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