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. Author manuscript; available in PMC: 2021 Aug 14.
Published in final edited form as: ACS Infect Dis. 2020 Jul 20;6(8):2057–2072. doi: 10.1021/acsinfecdis.0c00122

Table 4.

Structures and EC50 Values for MMV676477 Structural Analogsa

Compound ID Structure Amastigote EC50 ±
SE (nM)
Promastigote EC50 ±
SE (nM)
RAW 264.7 cells
CC50 ± SE (nM)
graphic file with name nihms-1688956-t0008.jpg
R =
MMV676477 2-SCH3 79 ± 8.4 2400 ± 35 2200 ± 410
SW100 H 1100 ± 84 2000 ± 130 690 ± 140
SW22 graphic file with name nihms-1688956-t0009.jpg 160 ± 3.2 6700 ± 53 1300 ± 42
SW72 4-OCH3 180 ± 8.2 7500 ± 880 > 10,000
SW41 3-CI, 4-F 20 ± 0.9 780 ± 29 2400 ±100
SW73 2-CF3 68 ± 3.9 3200 ± 87 1500 ± 140
graphic file with name nihms-1688956-t0010.jpg
R =
SW75 H 290 ± 22 11200 ± 260 9900 ± 2800
SW23 −C(O)CH3 > 3000 > 50,000 > 10,000
SW101 −C(O)NH-(4-CH3-C6H4) 1100 ± 91 8200 ± 1600 3000 ± 250
SW102 −C(O)NH-(4-OCH3-C6H4) 2400 ± 160 13000 ± 1400 5200 ± 380
SW74 −C(O)-(3-pyridyl) 250 ± 40 9200 ± 1300 4200 ± 520
SW10 graphic file with name nihms-1688956-t0011.jpg > 5000 > 50,000 > 10,000
a

EC5072h and CC5072h values for structural analogs of MMV676477 against L. amazonensis axenic amastigotes and promastigotes and the Mϕ cell line RAW 264.7 are shown. Shown are mean EC5072h or CC5072h values (nM) calculated from three biological replicates ± SE. Structure of each compound is provided. See Supplemental Methods for synthesis of these analogs.