Antitubercular 2-Pyrazolylpyrimidinones: Structure-Activity Relationship and Mode-of-Action Studies.

doi:10.1021/acs.jmedchem.0c01727

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Article

Antitubercular 2-Pyrazolylpyrimidinones: Structure-Activity Relationship and Mode-of-Action Studies.

Journal of medicinal chemistry - 14 Jan 2021

Soares de Melo Candice, Singh Vinayak, Myrick Alissa, Simelane Sandile B, Taylor Dale, Brunschwig Christel, Lawrence Nina, Schnappinger Dirk, Engelhart Curtis A, Kumar Anuradha, Parish Tanya, Su Qin, Myers Timothy G, Boshoff Helena I M, Barry Clifton E, Sirgel Frederick A, van Helden Paul D, Buchanan Kirsteen I, Bayliss Tracy, Green Simon R, Ray Peter C, Wyatt Paul G, Basarab Gregory S, Eyermann Charles J, Chibale Kelly, Ghorpade Sandeep R

Abstract excerpt

Phenotypic screening of a Medicines for Malaria Venture compound library against Mycobacterium tuberculosis (Mtb) identified a cluster of pan-active 2-pyrazolylpyrimidinones. The biology triage of these actives using various tool strains of Mtb suggested a novel mechanism of action. The compounds were bactericidal against replicating Mtb and retained potency against clinical isolates of Mtb. Although selected...

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PMID: 33395287
DOI: 10.1021/acs.jmedchem.0c01727
PMCID: PMC7816196

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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