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

[ Vol. 15 , Issue. 1 ]

Author(s):

Elda Meta, Chiara Brullo*, Michele Tonelli, Scott G. Franzblau, Yuehong Wang, Rui Ma, Wan Baojie , Beatrice S Orena, Maria Rosalia Pasca and Olga Bruno   Pages 17 - 27 ( 11 )

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.

Affiliation:

Department of Pharmacy, Medicinal Chemistry Section, University of Genoa, Viale Benedetto XV, 3 -16132 Genoa, Department of Pharmacy, Medicinal Chemistry Section, University of Genoa, Viale Benedetto XV, 3 -16132 Genoa, Department of Pharmacy, Medicinal Chemistry Section, University of Genoa, Viale Benedetto XV, 3 -16132 Genoa, Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL 60612, Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL 60612, Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL 60612, Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL 60612, Department of Biology and Biotechnology "Lazzaro Spallanzani", University of Pavia, via Ferrata 9, 27100 Pavia, Department of Biology and Biotechnology "Lazzaro Spallanzani", University of Pavia, via Ferrata 9, 27100 Pavia, Department of Pharmacy, Medicinal Chemistry Section, University of Genoa, Viale Benedetto XV, 3 -16132 Genoa



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