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. 2011 Apr 18;2(7):538–543. doi: 10.1021/ml200070g

Table 3. Structures and KHK Inhibition Results for Analogues of 7 with Variation of R₂ and R₃.

graphic file with name ml-2011-00070g_0007.jpg

compd^a	R₂	N-R₃	IC₅₀ (nM)^b
36	CH₂-c-Bu	piperazino	18
37	CH₂CH₂-c-Pr	piperazino	50
38	CH₂CH₂OMe	piperazino	7.0
39	CH₂(2-thienyl)	piperazino	30
40	CH₂(2-thiazolyl)	piperazino	16
41	CH₂(2-pyridyl)	piperazino	9.8
42	H	piperazino	7.1
43	CH₂-c-Pr	(R)-3-(NH₂)-piperidino	18
44	CH₂-c-Pr	(S)-3-(NH₂)-piperidino	23
45	CH₂-c-Pr	4-(NH₂CH₂)-piperidino	10
46	CH₂-c-Pr	3-(NH₂CH₂)-azetidino	30
47	CH₂-c-Pr	2,6-diazaspiro[3.3]hept-2-yl	8.0
48	CH₂-c-Pr	MeNHCH₂CH₂NMe-	130
49	CH₂-c-Pr	4-(Me₂NCH₂)-piperidino	140
50	CH₂-c-Pr	N-Me-piperazino	110

^a

See Table 1.

^b

Inhibition of recombinant human KHK-C.