Table 1. P. aeruginosa Antibacterial Activity and Physicochemical Properties of Siderophore-Conjugated Monocarbam Analogs.

	PAO1 MICa	PBP3ckon	human PPBd,g	hydrolytic stabilitye,g
compd	(μg/mL)	(M–1 s–1)	(% free)	t1/2 (h)
1	1	4.9 × 104	NT	95 ± 2.6
2	4	2.6 × 105	62 ± 8.8	>150f
3	0.78b	1.7 × 105	5 ± 0.1	NT
4a	0.78b	8.1 × 104	6 ± 0.5	NT
4b	0.25	7.2 × 104	4 ± 0.9	117 ± 17
7a	0.13	3.2 × 105	6 ± 0.2	86 ± 13
7b	0.25	1.7 × 105	9 ± 2.2	93 ± 12
7c	0.25	6.2 × 105	7 ± 0.5	100 ± 8.5
7d	1	>4.0 × 105	3 ± 0.04	>150f
7e	1	5.4 × 105	4 ± 0.1	87 ± 5.7
7f	0.5	4.5 × 105	4 ± 0.3	94 ± 8.4
7g	0.5	2.5 × 105	9 ± 0.2	71 ± 23
7h	0.5	4.1 × 105	8 ± 0.1	61 ± 9.1
7i	0.5	3.0 × 105	8 ± 0.2	NT
7j	<0.6	>4.0 × 105	NT	102 ± 7.1
9a	1	2.5 × 105	20 ± 9.3	102 ± 7.1
9b	4	1.5 × 105	12 ± 1.0	82 ± 7.1
10a	0.25	5.0 × 105	27 ± 8.7	85 ± 4.7
10b	1	3.2 × 105	6 ± 1.5	118 ± 23

^aPAO1 = P. aeruginosa ARC545.

^bMICs reported in μM.

^cP. aeruginosa PBP3.

^dn = 3, standard deviation.

^epH = 7.4, 37 °C.

^fNot determined.

^gNT = not tested.