| Autor: |
Suarez, María Angélica, Valencia, Jhesua, Cadena, Christian Camilo, Maiti, Raktim, Datta, Chandreyee, Puerto, Gloria, Isaza, José Hipólito, Juan, Homero San, Nagaraja, Valakunja, Guzman, Juan David |
| Předmět: |
|
| Zdroj: |
Molecules; Aug2017, Vol. 22 Issue 8, p1245, 8p, 3 Diagrams, 1 Chart |
| Abstrakt: |
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 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. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
|
