Inhibition of AspH by 2OG derivatives.

	2OG derivativea	IC50b,c [μM]		2OG derivativea	IC50b,c [μM]		2OG derivativea	IC50b,c [μM]
1		Inactive	12		0.61 ± 0.09	23		12.9 ± 1.3
2		1.2 ± 0.5	13		0.47 ± 0.08	24		Inactive
3		5.7 ± 1.1	14		0.51 ± 0.12	25		Inactive
4		48.2 ± 13.1	15		0.70 ± 0.11	26		Inactive
5		6.8 ± 0.9	16		0.25 ± 0.05	27		Inactive
6		1.6 ± 0.3	17		0.43 ± 0.05	28		Inactive
7		2.6 ± 0.8	18		0.17 ± 0.03	29		Inactive
8		6.3 ± 2.6	19		0.3 ± 0.1	30		Inactive
9		3.6 ± 1.4	20d		5.2 ± 1.7	31		Inactive
10		4.7 ± 0.2	21e		19.3 ± 1.6	32		Inactive
11		Inactive	22		Inactive	33		3.3 ± 1.0

^aAll chiral 2OG derivatives were prepared as racemic mixtures.

^bMean of three independent runs (n = 3; mean ± SD). AspH inhibition assays were performed as described in the ESI using 50 nM His₆-AspH_315–758 and 1.0 μM hFX-CP_101–119 (ESI Fig. S1d) as a substrate.

^c2OG derivatives were termed inactive when the IC₅₀-values were >50 μM. The AspH inhibition assays were of good quality which high S/N ratios and Z′-factors⁴⁰ (>0.5 for each plate) indicate (ESI Fig. S3).

^dMixture of racemic diastereomers, dr (cis : trans) = 2.5 : 1.

^e(±)-(2-Exo,3-endo)-diastereomer.