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Diarylethenes Display In Vitro Anti-TB Activity and Are Efficient Hits Targeting the Mycobacterium tuberculosis HU Protein

Angelica Suarez, Maria and Valencia, Jhesua and Camilo Cadena, Christian and Maiti, Raktim and Datta, Chandreyee and Puerto, Gloria and Hipolito Isaza, Jose and San Juan, Homero and Nagaraja, Valakunja and David Guzman, Juan (2017) Diarylethenes Display In Vitro Anti-TB Activity and Are Efficient Hits Targeting the Mycobacterium tuberculosis HU Protein. In: MOLECULES, 22 (8).

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Official URL: http://doi.org/10.3390/molecules22081245

Abstract

Tuberculosis continues to be a great source of concern in global health because of the large reservoir of humans infected with the bacilli and the appearance of clinical isolates resistant to a wide array of anti-tuberculosis drugs. New drugs with novel mechanisms of action on new targets are urgently required to reduce global tuberculosis burden. Mycobacterium tuberculosis nucleoid associated protein (NAP) HU has been shown to be druggable and essential for the organism's survival. In this study, four diarylethenes were synthesized using a one-pot decarboxylated Heck-coupling of coumaric acids with iodoanisoles. The prepared compounds 1-4 were tested for their in vitro growth inhibition of M. tuberculosis H37Rv using the spot culture growth inhibition assay, displaying minimum inhibitory concentrations between 9 and 22 mu M. Their cytotoxicity against BHK-21 cell line showed half inhibition at concentrations between 98 and 729 mu M. The most selective hit (SI = 81), demonstrated inhibition of M. tuberculosis HU protein involved in maintaining bacterial genome architecture.

Item Type: Journal Article
Additional Information: Copy right for this article belongs to the MDPI AG, ST ALBAN-ANLAGE 66, CH-4052 BASEL, SWITZERLAND
Department/Centre: Division of Biological Sciences > Microbiology & Cell Biology
Depositing User: Id for Latest eprints
Date Deposited: 23 Sep 2017 05:04
Last Modified: 23 Sep 2017 05:04
URI: http://eprints.iisc.ac.in/id/eprint/57876

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