Antibacterial activity (MICs) of PBD-biaryl conjugates as determined using five staphylococcal and two enterococcal clinical isolates. Compounds eliciting MIC values of ≤4 mg/L for all seven Gram-positive bacteria were considered effective. The numbering system for the components of the compound library is shown in Table S1. PBD, pyrrolo(2,1-c)(1,4)benzodiazepine; Py, 1-methylpyrrol-3-amine; PyM, (1,5-dimethylpyrrol-2-yl)methanamine; Im, 1-methylimidazol-4-amine; In, 1-methylindol-5-amine; Bzf, benzofuran-5-amine; Bzt, benzothiophen-5-amine; BztMC, methyl 5-aminobenzothiophene-2-carboxylate; MPB, 4-(1-methyl-1H-pyrrol-3-yl)benzenamine; FB, 4-(3-furyl)benzenamine; TB, 4-(3-thienyl)benzenamine; MTaB, 3-(2-methylthiazol-4-yl)benzenamine; TdB, 4-(thiadiazol-4-yl)benzenamine; MB, 4-morpholinobenzenamine; MPpB, 4-(4-methylpiperazin-1-yl)benzenamine; MMB, 4-(morpholinomethyl)benzenamine; MEB, 4-(2-morpholinoethoxy)benzenamine; MEPM, [4-(2-morpholinoethoxy)phenyl]methanamine; MPA, 6-morpholinopyridin-3-amine.