Ester derivatives of Dictyostelium differentiation-inducing factors exhibit antibacterial activity, possibly via a prodrug-like function

Table 1 Comparison of antimicrobial activity (MIC^a) of DIF derivatives against MSSA, MRSA, VSE, and VRE (VanA)

Compound	cLogP^b	HSA	S. aureus		E. faecalis	E. faecium
Compound	cLogP^b	HSA	MSSA	MRSA	VSE	VRE (VanA)
DIF-1 (1)	3.278	0 (%)	6.25 (μM)	12.5 (μM)	50 (μM)	50 (μM)
DIF-1 (1)	3.278	5	> 100	> 100	> 100	> 100
DIF-3 (2)	2.895	0	50	50	> 100	> 100
DIF-3 (2)	2.895	5	> 100	> 100	> 100	> 100
Ph-DIF-1 (3)	5.457	0	3.13	0.78	1.56	1.56
Ph-DIF-1 (3)	5.457	5	> 100	> 100	> 100	> 100
Bu-DIF-3 (4)	4.482	0	0.78	0.78	6.25	1.56
Bu-DIF-3 (4)	4.482	5	> 100	> 100	> 100	> 100
DIF-1-NH₂ (5)	1.391	0	> 100	> 100	> 100	> 100
NH₂-Bu-DIF-3 (6)	2.595	0	> 100	> 100	> 100	> 100
Vancomycin	− 0.9062	0	0.39	0.39	1.56	> 100
Vancomycin	− 0.9062	5	0.63	0.75	0.75	> 100

^aMinimum inhibitory concentration (MIC) values of the indicated compounds were assessed using MSSA (ATCC, 29213), MRSA (43300), VSE (29212), and VRE (VanA) (700221) in the presence or absence of 5% HSA. MIC values are the mean of triplicate determination, and those below 10 μM are given in bold
^bcLogP (hydrophobic index) values of the compounds are also presented

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