Table 1.

In vitro activity of compounds 1a,b–6a,b.

Structure	Series A R = m-CNPh			Series B R = p-NO2Ph
	%RA *	IC50 ** (µM)		%RA *	IC50 ** (µM)
	I			II
	3.1 ± 1.0		6.3 ± 0.9	18.2 ± 5.1	7.6 ± 1.6
	1a			1b
	23.7 ± 5.0		35.5 ± 1.9	22.5 ±10.8	18.6 ± 1.7
	2a			2b
	24.8 ± 1.8		41.9 ± 7.3	32.8 ± 2.3	-
	3a			3b
	38.0 ± 7.6		-	23.0 ± 7.8	21.1 ± 2.7
	4a			4b
	21.2 ± 1.0		39.3 ± 3.0	18.2 ± 4.9	27.5 ± 2.3
	5a			5b
	75.0 ± 9.8		-	59.0 ± 4.3	-
	6a			6b
	67.9 ± 6.6		-	32.7 ± 7.8	-

* % residual enzymatic activity at 100 µM; ** only for compounds with %RA ≤ 25%.