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

Table 4.

N-Deacyl-A40926 (DA40), demannosyl-N-deacylA40926 (DMDA40) and their derivatives Inline graphic

LCTA Code no. X Y1 = Y2 Z1 Z2 HIV-1 (CEM)
 FIPV (CRFK)
 SARS-CoV (Vero)
EC50 (μM) IC50 (μM) EC50 (μM) CC50 (μM) EC50 (μM) CC50 (μM)
DA40926 and its derivatives S = Man
 519 55 H OH H H >250 >500 >80 >80 >80 >80
 700 56 H NH(CH2)3N+Me2BnPh-p H H 4.0 ± 1.4 32 ± 5 >50 63 ± 3 >80 >80



DMDA40926 and its derivatives S = H
 599 57 H OH H H 115 ± 21 >500 >80 >80 >80 >80
 604 58 H NH(CH2)3NMe2 p-BuOBn p-BuOBn 5.0 ± 0.7 80 ± 6 >50 53 ± 7 >80 >80
 605 59 H NH(CH2)3NMe2 H p-BuBn 12 ± 3.5 >250 >60 63 ± 3 58 ± 2 >80
 613 60*a CH2N[CH2CH2]2NBnPh-p OH H p-BuBn 3.5 81 4.5 ± 0.4a 50 ± 0 21 ± 7 >80
 614 61a CH2N[CH2CH2]2NBnPh-p NH(CH2)3NMe2 H p-BuBn 3.5 ± 2.1 212 ± 54 5.9 ± 1.5 30 ± 9 21 ± 5 >80
 737 62*a CH2N[CH2CH2]2NBnBu-p OH H H 20 ± 7 106 ± 2 7.5 ± 1.8 >80 43 ± 6 >80
 738 63 CH2NH(CH2)3N+C10H21Me2 OH H H 3.5 92 23 ± 17 >80 >80 >80
 740 64 CH2NH(CH2)3N+C10H21Me2 NH(CH2)3NMe2 H H 3.5 ± 0.7 92 ± 5 >50 55 ± 2 52 ± 21 >80
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.