Ontology highlight
ABSTRACT:
SUBMITTER: Nelson KM
PROVIDER: S-EPMC4667731 | biostudies-literature | 2015 Jul
REPOSITORIES: biostudies-literature
Nelson Kathryn M KM Viswanathan Kishore K Dawadi Surendra S Duckworth Benjamin P BP Boshoff Helena I HI Barry Clifton E CE Aldrich Courtney C CC
Journal of medicinal chemistry 20150709 14
MbtA catalyzes the first committed biosynthetic step of the mycobactins, which are important virulence factors associated with iron acquisition in Mycobacterium tuberculosis. MbtA is a validated therapeutic target for antitubercular drug development. 5'-O-[N-(Salicyl)sulfamoyl]adenosine (1) is a bisubstrate inhibitor of MbtA and exhibits exceptionally potent biochemical and antitubercular activity. However, 1 suffers from suboptimal drug disposition properties resulting in a short half-life (t(1 ...[more]