Figures & data
Figure 1. The design of target compounds.
Scheme 1. The synthetic route of aminoguanidine-linked alkynyl derivatives.
Table 1. Inhibitory activity (MIC, μg/mL) of compounds 3a–3j and 6a–6k against Gram-positive bacteria and Gram-negative bacteria.
Table 2. Inhibitory activity (MIC, µg/mL) of compounds 3c–3e, 3g, 3i, 3j, 6a, 6b and 6e against clinical isolates of multidrug-resistant strains.
Figure 2. Propensity of the development of bacterial resistance towards compound 3g by (A) S. aureus and (B) E. coli.
Figure 3. Bactericidal activities of compound 3g and norfloxacin against MRSA.
Figure 4. Interactions of compound 3g and 6e with P. aeruginosa LpxC (A for 3g; B for 6e).
Figure 5. Interactions of (A) compound 3g and (B) 6e with E. coli LpxC.
Figure 6. Overlay of 6e and LPC-009 binding to (A) P. aeruginosa LpxC and (B) E. coli LpxC.
Figure 7. Interactions of compound (A) 3g and (B) 6e with E. coli FabH.
Table 3. The Inhibitory activity (IC50, µg/mL) of compounds 3e, 3f, 3g, 3i, 6a, 6b, 6e and 6k against cancer cell lines A549 and SGC7901 and normal cell lines L02.