Novel Pyrazole-Containing Compounds Active against .
Abstract
In this study, a series of 49 five-membered heterocyclic compounds containing either a pyridine- or a pyrrole-type nitrogen were synthesized and tested against . Among them, only the 1,3,5-trisubstituted pyrazoles - exhibited minimum inhibitory concentration values in the low micromolar range, and some also exhibited an improved physicochemical profile without cytotoxic effects. Three pyrazoles were subjected to an animal tuberculosis efficacy model, and compound induced a statistically significant difference in lung bacterial counts compared with untreated mice. Moreover, to determine the target of this series, resistors were generated, and whole genome sequencing revealed mutations in the gene.
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64008
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0x95644003c57E6F55A65596E3D9Eac6813e3566dA
Article ID:
64008
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10.1021/acsmedchemlett.9b00204
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Scimatic Chain (ID: 481)
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