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. 2015 Sep 1;212(Suppl 2):S425–S434. doi: 10.1093/infdis/jiv223

Table 1.

Preliminary SAR of Aminoacetamide Sulfonamide Scaffold

Compound Inline graphic
 HIV/EBOV-GP
R1 R2 R3 IC90, µmol/L CC50, µmol/L SI
MBX2254 2-Ph 4-Me 4-OMe 8.6 >50 ND
6 175 342 4-OMe 3-OMe 4-Me >100 >100 ND
6 367 388 2,5-diOMe 2-Cl 4-Me 1.6 50 31
6 175 402 3-Me 2-Cl 4-Me 3.2 >100 >31
5 534 655 4-OEt 4-Me H 0.8 >100 >125
6 068 478 2-F 3-Me H 0.8 50 63

Abbreviations: CC50, 50% cytotoxic concentration; HIV/EBOV-GP, Ebola pseudotype; IC90, 90% inhibitory concentration; ND, not determined; SAR, structure activity relationship; SI, selectivity index.