Synthesis, biological evaluation and computational studies of pyrazole derivatives as Mycobacterium tuberculosis CYP121A1 inhibitors.
Autor: | Alshabani LA; School of Pharmacy & Pharmaceutical Sciences, Cardiff University King Edward VII Avenue Cardiff CF10 3NB UK simonsc@cardiff.ac.uk., Kumar A; Department of Biochemistry, Jacobs School of Medicine and Biomedical Science, University at Buffalo Buffalo New York-14203 USA., Willcocks SJ; Department of Infection Biology, The London School of Hygiene and Tropical Medicine London WC1E 7HT UK.; Mycobacteria Research Laboratory, Institute of Structural and Molecular Biology, Department of Biological Sciences, Birkbeck, University of London London WC1E 7HX UK., Srithiran G; Mycobacteria Research Laboratory, Institute of Structural and Molecular Biology, Department of Biological Sciences, Birkbeck, University of London London WC1E 7HX UK., Bhakta S; Mycobacteria Research Laboratory, Institute of Structural and Molecular Biology, Department of Biological Sciences, Birkbeck, University of London London WC1E 7HX UK., Estrada DF; Department of Biochemistry, Jacobs School of Medicine and Biomedical Science, University at Buffalo Buffalo New York-14203 USA., Simons C; School of Pharmacy & Pharmaceutical Sciences, Cardiff University King Edward VII Avenue Cardiff CF10 3NB UK simonsc@cardiff.ac.uk. |
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Jazyk: | angličtina |
Zdroj: | RSC medicinal chemistry [RSC Med Chem] 2022 Aug 16; Vol. 13 (11), pp. 1350-1360. Date of Electronic Publication: 2022 Aug 16 (Print Publication: 2022). |
DOI: | 10.1039/d2md00155a |
Abstrakt: | A series of imidazole and triazole diarylpyrazole derivatives were prepared using an efficient 5-step synthetic scheme and evaluated for binding affinity with Mycobacterium tuberculosis (Mtb) CYP121A1 and antimycobacterial activity against Mtb H37Rv. Antimycobacterial susceptibility was measured using the spot-culture growth inhibition assay (SPOTi): the imidazoles displayed minimum inhibitory concentration (MIC Competing Interests: There are no conflicts to declare. (This journal is © The Royal Society of Chemistry.) |
Databáze: | MEDLINE |
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