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Molecules 2017, 22(8), 1245; doi:10.3390/molecules22081245

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

Departamento de Química y Biología, División de Ciencias Básicas, Universidad del Norte, Km 5 vía Puerto Colombia, Barranquilla 081007, Colombia
Departamento de Medicina, División de Ciencias de la Salud, Universidad del Norte, Km 5 vía Puerto Colombia, Barranquilla 081007, Colombia
Department of Microbiology and Cell Biology, Indian Institute of Science, Bangalore 560012, India
Laboratorio de Micobacterias, Instituto Nacional de Salud, Calle 26 No. 51-20-Zona 6 CAN, Bogotá 111321, Colombia
Grupo de Investigación en Productos Naturales y Alimentos (GIPNA), Departamento de Química, Universidad del Valle, Cali 760032, Colombia
Author to whom correspondence should be addressed.
Received: 9 July 2017 / Accepted: 22 July 2017 / Published: 25 July 2017
(This article belongs to the Special Issue Emerging Drug Discovery Approaches against Infectious Diseases)
View Full-Text   |   Download PDF [1833 KB, uploaded 25 July 2017]   |  


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 14 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 µM. Their cytotoxicity against BHK-21 cell line showed half inhibition at concentrations between 98 and 729 µM. The most selective hit (SI = 81), demonstrated inhibition of M. tuberculosis HU protein involved in maintaining bacterial genome architecture. View Full-Text
Keywords: diarylethenes; stilbenes; tuberculosis; cytotoxicity; HU protein diarylethenes; stilbenes; tuberculosis; cytotoxicity; HU protein

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Suarez, M.A.; Valencia, J.; Cadena, C.C.; Maiti, R.; Datta, C.; Puerto, G.; Isaza, J.H.; San Juan, H.; Nagaraja, V.; Guzman, J.D. Diarylethenes Display In Vitro Anti-TB Activity and Are Efficient Hits Targeting the Mycobacterium tuberculosis HU Protein. Molecules 2017, 22, 1245.

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