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ID: ALA1152134

Journal: Bioorg Med Chem Lett

Title: Synthetic chalcones as efficient inhibitors of Mycobacterium tuberculosis protein tyrosine phosphatase PtpA.

Authors: Chiaradia LD, Mascarello A, Purificação M, Vernal J, Cordeiro MN, Zenteno ME, Villarino A, Nunes RJ, Yunes RA, Terenzi H.

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.

CiteXplore: 18930396

DOI: 10.1016/j.bmcl.2008.09.105