Ontology highlight
ABSTRACT:
SUBMITTER: Neres J
PROVIDER: S-EPMC2800054 | biostudies-literature | 2008 Sep
REPOSITORIES: biostudies-literature
Neres João J Labello Nicholas P NP Somu Ravindranadh V RV Boshoff Helena I HI Wilson Daniel J DJ Vannada Jagadeshwar J Chen Liqiang L Barry Clifton E CE Bennett Eric M EM Aldrich Courtney C CC
Journal of medicinal chemistry 20080809 17
5'-O-[N-(salicyl)sulfamoyl]adenosine (Sal-AMS) is a prototype for a new class of antitubercular agents that inhibit the aryl acid adenylating enzyme (AAAE) known as MbtA involved in biosynthesis of the mycobactins. Herein, we report the structure-based design, synthesis, biochemical, and biological evaluation of a comprehensive and systematic series of analogues, exploring the structure-activity relationship of the purine nucleobase domain of Sal-AMS. Significantly, 2-phenyl-Sal-AMS derivative 2 ...[more]