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. Author manuscript; available in PMC: 2024 Oct 13.
Published in final edited form as: ACS Infect Dis. 2023 Sep 11;9(10):1964–1980. doi: 10.1021/acsinfecdis.3c00245

Table 4.

Benzamide SAR: Physicochemical, In Vitro ADME, Antimalarial, and Cytotoxicity Data

graphic file with name nihms-1962359-t0013.jpg
Compd LogD7.4 PSA (Å2) Kinetic Sol6.5 (μg/mL) h/m CLint(μL/min/mg protein) P. falciparumIC50 (μM) L6 IC50 (μM)
30 0.9 59.1 >100 19/18 9.4 160
31 0.9 59.1 >100 11/10 11 190
32 2.1 46.2 50-100 11/110 0.13 96
33 2.0 70.0 25–50 <7/160 0.39 150
34 1.1 66.4 25–50 61/84a 15 84
35 1.3 66.4 >100 16/60 5.1 210
36 2.1 46.2 >100 13/43 1.3 110
37 1.2 66.4 12.5–25 7/36 1.1 200
a

Apparent non-NADPH-mediated degradation.