Next Article in Journal
Chalcone Derivatives: Promising Starting Points for Drug Design
Next Article in Special Issue
Synthesis and Biological Activity of Novel O-Alkyl Derivatives of Naringenin and Their Oximes
Previous Article in Journal
Electronic Spectroscopy of Phthalocyanine and Porphyrin Derivatives in Superfluid Helium Nanodroplets
Previous Article in Special Issue
Repositioning FDA Drugs as Potential Cruzain Inhibitors from Trypanosoma cruzi: Virtual Screening, In Vitro and In Vivo Studies
Article Menu
Issue 8 (August) cover image

Export Article

Open AccessArticle
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

1
Departamento de Química y Biología, División de Ciencias Básicas, Universidad del Norte, Km 5 vía Puerto Colombia, Barranquilla 081007, Colombia
2
Departamento de Medicina, División de Ciencias de la Salud, Universidad del Norte, Km 5 vía Puerto Colombia, Barranquilla 081007, Colombia
3
Department of Microbiology and Cell Biology, Indian Institute of Science, Bangalore 560012, India
4
Laboratorio de Micobacterias, Instituto Nacional de Salud, Calle 26 No. 51-20-Zona 6 CAN, Bogotá 111321, Colombia
5
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]   |  

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 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
Figures

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).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

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.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top