Synthesis and evaluation of functionalized benzoboroxoles as potential anti-tuberculosis agents Dedicated to Professor Neil K. Garg on the occasion of his receipt of the Tetrahedron Young Investigator Award

Mohammad A. Alam, Kriti Arora, Shirisha Gurrapu, Sravan K. Jonnalagadda, Grady L. Nelson, Paul Kiprof, Subash C. Jonnalagadda, Venkatram R. Mereddy

    Research output: Contribution to journalArticlepeer-review

    18 Scopus citations

    Abstract

    Several derivatives of aminobenzoboroxole have been prepared starting from 2-boronobenzaldehyde. All of these derivatives have been evaluated for their anti-mycobacterial activity on Mycobacterium smegmatis and cytotoxicity on breast cancer cell line MCF7. Based on these studies, all the tested molecules have been found to be generally non-toxic and benzoboroxoles with unsubstituted (primary) amines have been found to exhibit good anti-mycobacterial activity. Some of the key compounds have been evaluated for their anti-tubercular activity on Mycobacterium tuberculosis H37Rv using 7H9 and GAST media. 7-Bromo-6-aminobenzoboroxole 4 has been identified as the lead candidate compound for further development.

    Original languageEnglish (US)
    Pages (from-to)3795-3801
    Number of pages7
    JournalTetrahedron
    Volume72
    Issue number26
    DOIs
    StatePublished - Jun 30 2016

    All Science Journal Classification (ASJC) codes

    • Biochemistry
    • Drug Discovery
    • Organic Chemistry

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