Figure 2.

Synthesis and activity of Kang amides. A screen of more than 100 Kang amides identified 17 compounds with improved activity against wild-type (WT) S. aureus compared to Kang A. (a) Reaction used for the synthesis of Kang amides and summary of screening hits with improved activity against WT S. aureus. (b) MIC values (μg/mL) for Kang A and Rif against WT and Rif^R H481Y and S486L S. aureus strains. (c) Structural modifications and MIC values (μg/mL) of hits against WT and Rif^RS. aureus strains. Amines used for synthesis are shown. A subset of the semisynthetic derivatives, highlighted in red, was subjected to downstream analyses. The C5 and N29 amides were synthesized and screened using diastereomeric mixtures of 2-cyclopropylpyrrolidine and 2-methylpyrrolidine, respectively.