Table 1.

SIRT1 and SIRT2 enzymatic inhibitory assay data of reference compounds and key compounds in the generated small-molecule compound library

COMPD	R1	R2	R3	R4	R5	SIRT1a	SIRT2b
AK-722	-	-	-	-	-	-c	15.5
Salermide15,20	-	-	-	-	-	76 (IC50-μM)	45.0
Sirtinol15,30	-	-	-	-	-	38 (IC50-μM)	103.4
EX-52726	-	-	-	-	-	98 (IC50-nM)	19.6
4	H	H	H	H	H	-	-
6	CN	H	H	H	H	-	-
7	CN	H	H	H	NO2	-	-
8	CONH2	H	H	H	NO2	1%	17.6 ± 3.4
9	CONH2	H	H	H	NH2	-	-
11	CN	H	H	H	CN	-	-
12	CONH2	H	H	H	CONH2	-	-
16	H	H	H	CONH2	H	-	-
20	H	SO2NHtBu	H	H	H	12%	29.8 ± 4.9
22	H	NO2	H	H	H	-	-
23	CONH2	H	H	H	H	-	-
24	CONHtBu	H	H	H	H	-	100.0 ± 6.8
25	NO2	H	H	H	H	-	-
26	H	H	CONH2	H	H	-	-
27	CONH2	H	H	H	Cl	-	-
28	CONH2	H	H	H	CN	-	-
29	CONH2	H	CH3	H	NO2	23%	77.5 ± 12.0
30	CONH2	H	H	NO2	H	-	-
31	CONH2	H	H	CH2OH	H	-	-
32	CH2OH	H	H	CH2OH	H	-	-
33	CH2OH	H	H	H	CH2OH	-	-

^aInhibition at 100 μM;

^bIC₅₀ (μM) ± SD;

^cInhibition <25% at 50 μM