Figure 1. Propargyl-linked antifolates potently bind S. aureus DHFR.

a) Depiction of a general scaffold for the propargyl-linked antifolates with the pyrimidine ring (A), phenyl ring (B) and aryl ring (Ar) shown along with possible positions for substitutions (R₆, R_P, R_2′ and R_3′) b) Illustration of compound 1, a biphenyl propargyl-linked antifolate, with labeled atom positions b) Active site depiction from the structure of the SaDHFR:NADPH:1 ternary complex showing active site residues (orange), NADPH (magenta) and compound 1 (blue).