|
Title
|
|
|
|
2,3-dideoxy hex-2-enopyranosid-4-uloses as promising new anti-tubercular agents : design, synthesis, biological evaluation and SAR studies
| |
|
Author
|
|
|
|
| |
|
Abstract
|
|
|
|
| The alarming resurgence of tuberculosis (TB) underlines the urgent need for development of new and potent anti-TB drugs. Towards this goal we herein report the design and synthesis of 2,3-dideoxy hex-2-enopyranosid-4-uloses as promising new anti-tubercular agents. These easily accessible, small molecules were found to exhibit in vitro activity against Mycobacterium tuberculosis H37Rv in a MIC range of 0.78 μg/mL to 25 μg/mL. A detailed SAR study on these hex-2-enopyranosid-4-uloses led to the identification of compound 5g (S007-724) which on the basis of low MIC (0.78 μg/mL-M. tuberculosis H37Rv; 1.56 μg/mL-MDR, SDR strains of M. tuberculosis; 0.78 μg/mL-inhibition of intracellular replication of M. tuberculosis) and SI value of 13.5 has been identified as a promising lead molecule. |
| |
|
Language
|
|
|
|
English
| |
|
Source (journal)
|
|
|
|
European journal of medicinal chemistry. - Paris, 1974, currens
| |
|
Publication
|
|
|
|
Paris
:
2011
| |
|
ISSN
|
|
|
|
0223-5234
| |
|
DOI
|
|
|
|
10.1016/J.EJMECH.2011.03.002
| |
|
Volume/pages
|
|
|
|
46
:6
(2011)
, p. 2217-2223
| |
|
Article Reference
|
|
|
|
000291118600030
| |
|
ISI
|
|
|
|
000291118600030
| |
|
Medium
|
|
|
|
E-only publicatie
| |
|
Full text (Publisher's DOI)
|
|
|
|
| |
|