Duggirala, Sridevi ; Napoleon, John Victor ; Nankar, Rakesh P. ; Senu Adeeba, V. ; Manheri, Muraleedharan K. ; Doble, Mukesh (2016) FtsZ inhibition and redox modulation with one chemical scaffold: Potential use of dihydroquinolines against mycobacteria European Journal of Medicinal Chemistry, 123 . pp. 557-567. ISSN 0223-5234
Full text not available from this repository.
Official URL: http://doi.org/10.1016/j.ejmech.2016.07.058
Related URL: http://dx.doi.org/10.1016/j.ejmech.2016.07.058
Abstract
The dual effect of FtsZ inhibition and oxidative stress by a group of 1,2-dihydroquinolines that culminate in bactericidal effect on mycobacterium strains is demonstrated. They inhibited the non-pathogenic Mycobacterium smegmatis mc(2) 155 with MIC as low as 0.9 μg/mL and induced filamentation. Detailed studies revealed their ability to inhibit polymerization and GTPase activity of MtbFtsZ (Mycobacterial filamentous temperature sensitive Z) with an IC50 value of ∼40 μM. In addition to such target specific effects, these compounds exerted a global cellular effect by causing redox-imbalance that was evident from overproduction of ROS in treated cells. Such multi-targeting effect with one chemical scaffold has considerable significance in this era of emerging drug resistance and could offer promise in the development of new therapeutic agents against tuberculosis.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to Elsevier Science. |
| ID Code: | 132340 |
| Deposited On: | 15 Dec 2022 07:33 |
| Last Modified: | 15 Dec 2022 07:33 |
Repository Staff Only: item control page
