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

Table 1.

Vancomycin and eremomycin type glycopeptides and their derivatives substituted at the X, Y and R positions Inline graphic

LCTA Code no. X Y R HIV-1 (CEM)
 FIPV (CRFK)
 SARS-CoV (Vero)
EC50 (μM) IC50 (μM) EC50 (μM) CC50 (μM) EC50 (μM) CC50 (μM)
Vancomycin (Van) and its derivatives W = Cl, S1 = Glc, S2 = vancosamine, S3 = H
 878 1 H OH H >250 >500 >100 >100 >100 >100
 854 2 H NHC10H21 H >10 30 ± 2 >50 50 ± 1 >80 >80
 892 3 H NH(CH2)3N+Me2C10H21 H 5.5 ± 0.7 172 ± 15 >80 >80 57 ± 14 >80
 893 4 H NHMe H >250 >500 >80 >80 >80 >80
 941 5 CH2N[CH2CH2]2NBnBu-p OH H 12 ± 3.5 >100 30 ± 12 >50 37 ± 2 >100
 1002 6 H OH BnPhCI-p NTa NT 20 61 22 ± 14 >100



Eremomycin (Ere) and its derivatives W = H, S1 = Glc, S2 = S3 = eremosamine
 516 7 H OH H >250 >500 >100 >100 >100 >100
 177 8 H CH3(CH2)2O H NT NT >80 >80 >80 >80
 200 9 H CH3(CH2)11O H NT NT >16 18 ± 4 27 ± 4 >80
 261 10 H NHMe H >250 >500 >80 >80 >80 >80
 284 11 CH2NHC10H21 OH H >20 24 ± 13 >16 44 ± 3 >40 54 ± 22
 288 12 CH2NMeCH2(CHOH)4CH2OH OH H >250 >250 >80 >80 >80 >80
 289 13c CH2NHC18H37 OH H >10 15 ± 2 3.4 ± 1.4 15 ± 2 65 ± 48 >80
 302b 14 H OH H NT NT >80 >80 >80 >80
 298 15c CH2NHC12H25 OH H >10 94 ± 4 8.9 ± 1 69 ± 8 31 ± 2 >80
 340 16 H NHC10H21 H >10 9.4 ± 4.7 >16 19.5 ± 5 >40 53 ± 15
 353 17 H NHBnCI-p H >250 >250 >80 >80 >80 >80
 356 18 CH2NHBnPh-p OH H 17.5 ± 11 >500 >80 >80 51 ± 17 >100
 368 19 H OH C10H21 >20 44 ± 2 >16 51 ± 0 43 ± 26 >80
 375 20 H OH BnCI-p >250 >250 >80 >80 >80 >80
 512 21 CH2N[CH2CH2]2NC10H21 OH H >2 18 ± 11 >10 16 ± 1 >10 45 ± 8
 518 22 CH2N[CH2CH2]2NBnPh-p OH H >10 53 ± 15 >50 52 ± 6 14 ± 0 >80
 670 23 H NH(CH2)4CH(CONH(CH2)3NMe2)NHBnOBu-p H >50 117 ± 18 >80 >80 >80 >80
 717 24 H OH Bn(PhCI-p)-p >10 44 ± 1 >50 60 ± 5 33 ± 11 >100
 728 25 CH2NH(CH2)3N+Me2C10H21 NH(CH2)3NMe2 H 7.0 ± 0 27 ± 7 >60 61 ± 0 >40 45 ± 1
 766 26 CH2N[CH2CH2]2NBnBu-p OH H 1.4 ± 0.6 96 ± 13 14 ± 4 58 ± 9 33 ± 1 >80
 768 27c CH2N[CH2CH2]2NBnBu-p NHMe H 0.43 ± .3 40 ± 4 5.4 ± 0.2 28 ± 3 14 ± 2 50 ± 6
 770 28 H OC11H23 H >10 7.6 ± 1 >16 35 ± 4 44 ± 9 >80
 784 29 CH2NH(CH2)3N+Me2C10H21 OH H >20 44 ± 3 >80 >80 >80 >80
 826 30c H NH(CH2)3N+Me2 C10H21 H >20 38 ± 1 6.9 ± 0.4 48 ± 1 >40 56 ± 21
 827 31 H NH(CH2)6NH2 H >100 >100 >80 >80 >80 >80
 828 32 H NH(CH2)10NH2 H >20 >100 >80 >80 >80 .80
 829 33 H NHBnCH2NH2-p H >100 >100 >80 >80 >80 >80
 832 34 H NHBnNHC10H21-p H >4 5 ± 0.5 >16 21 ± 8 22 ± 1 >80
 833 35 H NHBnN+Me2C10H21-p H >20 19 ± 8 14 ± 7 41 ± 5 >40 46 ± 0
 834 36 H NHCH2C5H4N+C10H21 H >20 35 ± 2 >16 72 ± 9 >80 >80
 837 37 H NHBnPhCI-p H >10 8.6 ± 0.2 >20 27 ± 8 30 ± 24 >80
 846 38 H NHBnPh-p H >10 35 ± 1 >50 53 ± 4 31 ± 8 >100
 847 39 CH2NHBnPhCI-p OH H 22.5 ± 3.5 106 ± 65 12 ± 3 54 ± 8 22 ± 12 >100
 848 40 H NHBnBu-p H >50 29 ± 12 >50 52 ± 3 50 ± 3 >100
 864 41 H NHC7H15 H ≫50 182 ± 013 >80 >80 60 ± 19 >100
 869 42 H NHBnNBu2 H ≫10 30 ± 2 37 ± 16 49 ± 8 35 ± 19 >100
 921 43 CH2N[CH2CH2]2NCOCH2NHBnBu-p OH H >10 63 ± 29 42 >80 45 ± 11 >80
 923 44 H N[CH2CH2]2NCH CH2 NHBnBu-p H >50 >100 >60 66 ± 12 31 ± 7 >100
 972 45 H NHCH((CH2)4NH2)CONHBnBu-p H >50 104 ± 11 >16 73 ± 7 >80 >80
a

NT, not tested.

b

Carboxyeremomycin.

c

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.