Table 3.

Exploring alternative R¹ substituents on R²/R³-unsubstituted aminopyrazoles. Fold selectivity >5 for any compound is highlighted in red.

Entry	Compound	R1	X	C. neoformans EC50a (μM)	C. neoformans fold- selectivityb	C. albicans EC50c (μM)	C. albicans fold- selectivityb
1	56	CH3	A	0.088	1.5	0.111	0.4
2	57		B	0.286	4.4	0.624	0.7
3	58		C	0.142	5.1	0.377	0.7
4	59	iPr	A	0.125	1.3	0.076	0.7
5	60		B	0.250	2.6	0.309	0.7
6	61		C	0.097	3.6	0.161	0.7
7	62	iBu	A	0.062	1.1	0.035	0.7
8	63		B	0.103	1.7	0.117	0.6
9	64		C	0.041	2.3	0.057	0.6
10	65		A	0.051	0.7	0.009	1.2
11	66		B	0.026	1.7	0.015	0.9
12	67		C	0.018	1.3	0.008	0.8
13	68	Ph	A	0.061	0.5	0.014	0.8
14	69		B	0.044	0.9	0.021	0.7
15	70		C	0.037	0.8	0.015	0.8
16	71	Cy	A	0.087	0.4	0.013	0.9
17	72		B	0.045	1.0	0.016	1.0
18	73		C	0.035	1.0	0.014	1.0
19	74	Bn	A	0.052	0.8	0.015	0.8
20	75		B	0.043	1.1	0.018	0.8
21	76		C	0.036	1.1	0.015	0.8
22	77		A	0.058	1.7	0.041	0.7
23	78		B	0.207	1.6	0.143	0.7
24	79		C	0.199	1.8	0.164	0.7
25	80		A	0.074	0.9	0.033	0.7
26	81		B	0.106	1.2	0.080	0.6
27	82		C	0.058	1.4	0.041	0.8
28	83		A	0.044	12.8	0.366	1.1
29	84		B	0.040	0.8	0.012	0.9
30	85		C	0.036	0.8	0.012	0.8
31	86		B	0.063	0.9	0.025	0.8
32	87		C	0.048	1.1	0.021	0.9

EC₅₀ and selectivity values were determined as described for Table 1.