Inhibition of Siderophore Biosynthesis by 2-Triazole Substituted Analogues of 5'-O-[N-(Salicyl)sulfamoyl]adenosine: Antibacterial Nucleosides Effective against Mycobacterium tuberculosis.

[摘要]：The synthesis, biochem., and biol. evaluation of a systematic series of 2-triazole derivs. of 5'-O-[N-(salicyl)sulfamoyl]adenosine (Sal-AMS) are described as inhibitors of aryl acid adenylating enzymes (AAAE) involved in siderophore biosynthesis by Mycobacterium tuberculosis. Structure-activity relationships revealed a remarkable ability to tolerate a wide range of substituents at the 4-position of the triazole moiety, and a majority of the compds. possessed sub-nanomolar apparent inhibition consts. However, the in vitro potency did not always translate into whole cell biol. activity against M. Tuberculosis, suggesting that intrinsic resistance plays an important role in the obsd. activities. Addnl., the well-known valence tautomerism between 2-azidopurines and their fused tetrazole counterparts led to an unexpected facile acylation of the purine N-6 amino group.

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