Table 1.

Potency enhancement and PAMPA data from ortho-substitution of biphenyl mannosides.

Compound	HAI Titer EC>90 (μM)	Biofilm Prevention IC50 (μM)	MW (g/mol)	PSA	CLogD7.4	PAMPA LogPe (cm2/sec)
1 (ester)	1.00	0.94	390.4	126	1.17	−5.42
4a (F)	0.75		408.4	126	1.00
4b (Cl)	0.03	0.26	424.8	126	1.64	−4.29
4c (Me)	0.12	0.33	404.4	126	1.82
4d (CF3)	0.03	0.17	458.4	126	1.62	−3.91
4e (OMe)	0.19	0.89	420.4	135	0.47
6 (m-CO2Me)	1.0		448.4	152	0.93	−4.08
2 (amide)	0.50	1.35	389.4	128	0.28
5a (Cl)	0.12	0.52	423.8	128	0.75
5b (Me)	0.06	0.16	403.4	128	0.93	−3.89
5c (CF3)	0.03	0.13	457.4	128	0.73
3 (di-amide)	0.37	0.74	446.4	158	0.71	−4.51
7 (CF3)	0.01	0.043	514.5	158	1.15	−6.27
8 (Me)	0.02	0.073	460.5	158	1.35	−8.46