Author(s): Chiaradia LD, Mascarello A, Purificao M, Vernal J, Cordeiro MN,
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Abstract In the search for lead compounds for new drugs for tuberculosis, the activity of 38 synthetic chalcones were assayed for their potential inhibitory action towards a protein tyrosine phosphatase from Mycobacterium tuberculosis--PtpA. The compounds were obtained by aldolic condensation between aldehydes and acetophenones, under basic conditions. Five compounds presented moderate or good activity. The structure-activity analysis reveals that the predominant factor for the activity is the molecule planarity/hydrophobicity and the nature of the substituents.
This article was published in Bioorg Med Chem Lett
and referenced in Medicinal Chemistry