Table 2. In Vitro Antitrypanosomal Activity and Cytotoxicity of R₂ Analogues.

compound	R2	MW	cLogPa	tPSAa	pIC50b
					T. brucei	MRC-5
2	H	272.3	3.1	70.1	7.2 ± 0.2	<4.2
11	Me	286.3	3.0	59.3	7.1 ± 0.1	<4.2
21a	Et	300.3	3.4	59.3	6.6 ± 0.4	<4.2
21b	nPr	314.4	3.9	59.3	6.8 ± 0.2	<4.2
21c	iPr	314.4	3.8	59.3	5.2 ± 0.1	<4.2
21d	-(CH2)2OMe	330.4	3.0	68.5	<4.2	<4.2
22	-(CH2)2OH	316.3	2.3	79.5	6.2 ± 0.1	<4.2
21e	-(CH2)2CONH2	343.4	1.9	102.4	5.5 ± 0.3	<4.2
21f	-(CH2)2Ph-4-OMe	404.5	4.9	68.5	<4.2	<4.2

^acLogP and tPSA are adopted from CDD Vault.

^bMean values ± standard deviations, n ≥ 2.