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. 2006 Apr 6;72(1):20–33. doi: 10.1016/j.antiviral.2006.03.005

Table 5.

Vancomycin type aglycons and their derivatives Inline graphic

LCTA Code no. X Y Z HIV-1 (CEM)
 FIPV (CRFK)
 SARS-CoV (Vero)
EC50 (μM) IC50 (μM) EC50 (μM) CC50 (μM) EC50 (μM) CC50 (μM)
Vancomycin aglycon (VA) and its derivatives W = Cl
 890 65 H OH H 65 >500 >80 >80 >80 >80
 1130 66 H (1-Adam)CH2NH H 3.0 ± 0 NT >20 68 ± 16 57 ± 12 >100
 1131 67 H (2-Adam)NH H 3.0 ± 0 NT 24 ± 21 83 ± 24 51 ± 8 >100
 1132 68 H H2N(CH2)10NH H 2.5 ± 0.7 NT >20 73 ± 29 26 ± 13 >100



Vancomycin aglycon hexapeptide (VAH) and its derivatives W = Cl, first amino acid (N-Me-d-Leu) is absent (=H)
 1147 69 H OH – ≥125 NT >100 >100 >100 >100
 1136 70 H (1-Adam)CH2NH – 20.0 ± 7.1 NT >20 ≥100 >100 >100



Eremomycin aglycon (EA) and its derivatives W = H
 312 71 H OH H 50 >500 >80 >80 >80 >80
 891 72 H NH(CH2)3N+Me2C10H21 H 3.5 ± 0.7 57 ± 4 >16 52 ± 1 26 ± 6 >80
 902 73 CH2N[CH2CH2]2NBnPh-p OH H 5.5 ± 0.7 >500 29 ± 2 >80 35 ± 2 >80
 930 74 CH2N[CH2CH2]2NBnPh-p OH Boc 4.5 ± 0.7 >100 14 ± 12 >80 34 ± 8 >80
 935 75*a CH2N[CH2CH2]2NBnPh-p NHMe Boc 4.0 ± 0 >100 3.6 ± 1.6a >50 52 ± 20 >100
 936 76 CH2N[CH2CH2]2NBnPh-p NHMe H 4.0 ± 1.7 >100 >80 >80 15 ± 2 >100
 1060 77 H (1-Adam)CH2NH H 1.6 ± 0.36 148 ± 3 23 ± 9 >100 32 ± 2 >100
 1061 78 H p-FBnNH H 41.7 ± 20.2 >250 >80 >100 >100 >100
 1062 79 H (Perhydroiso-quinolin-1-yl)NH H 63.3 ± 53.5 >250 46 ± 23 >100 >100 >100
 1063 80 H 1,3-dicyclohexylureide H 7.5 ± 4.8 >250 >80 >100 55 ± 9 >100
 1133 81 H (2-Adam)NH H 8.5 ± 2.1 NT 48 ± 13 >100 59 ± 9 >100
 1134 82 H H2N(CH2)10NH H 8.5 ± 2.1 NT >20 76 ± 25 29 ± 2 >100



Eremomycin aglycon hexapeptide (EAH) and its derivatives W = H, first amino acid (N-Me-d-Leu) is absent (=H)
 311 83 H OH d-Trp 7.3 ± 0.58 >250 28 ± 1 >100 >80 >100
 964 84 H OH – 115 ± 21.2 >250 >80 >80 >80 >80
 966 85 CH2NHAdam-2 NHMe – 13 ± 9.9 >250 25 ± 15 >50 >80 >80
 1135 86 H (2-Adam)NH – 50.0 ± 0 NT >100 >100 >100 >100
 1138 87 H H2N(CH2)10NH – ≥25 NT >100 >100 72 ± 24 >100
 1140 88 H p-F-Ph-N[CH2CH2]2N – 12 NT >20 ≥100 55 ± 2 >100



De-Cl-eremomycin aglycon (De-Cl-EA) and its derivatives, W = H
 1139 89 H OH H >125 NT >100 >100 >100 >100
 1141 90 H (1-Adam)CH2NH H 8.5 ± 2.1 NT >4 53 ± 33 46 ± 11 >100
 1142 91 H (2-Adam)NH H 8.5 ± 2.1 NT >20 79 ± 30 48 ± 0 >100
 1143 92 H H2N(CH2)10NH H 15.0 ± 0 NT >20 ≥100 60 ± 17 >100



De-Cl-eremomycin aglycon hexapeptide (De-Cl-EAH) and its derivatives W = H, first amino acid (N-Me-d-Leu) is absent (=H)
 1148 93 H (1-Adam)CH2NH – 30.0 ± 7.1 NT 52 ± 9 ≥100 >100 >100
 1149 94 H H2N(CH2)10NH – >25 NT >100 >100 78 ± 10 >100
a

Antiviral values in italics denotes EC50 values equal or lower than 10 μg/ml. An asterix after the compound code no. indicates a selectivity (CC50/EC50) of >10 for the compound against either FIPV and/or SARS-CoV.