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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 2.

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

graphic file with name nihms-1962359-t0011.jpg
Compd LogD7.4 PSA (Å2) Kinetic Sol6.5 (μg/mL) h/m CLint(μL/min/mg protein) P. falciparumIC50 (μM) L6 IC50 (μM)
10 1.8 64.5 >100 22/76 >190 >380
11 2.5 50.7 >100 11/54a 95 250
12 1.5 49.3 >100 11/27 83 >390
13 2.6 29.1 >25 62/81 100 190
14 2.4 37.4 >100 110/220a 77 >380
15 2.9 37.4 25–50 310/>870b 100 83
16 3.7 43.4 >100 14/16 100 210
a

Apparent non-NADPH-mediated degradation detected.

b

Rapid metabolic degradation, estimate only.