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. Author manuscript; available in PMC: 2017 Nov 15.
Published in final edited form as: Bioorg Med Chem Lett. 2016 Oct 6;26(22):5573–5579. doi: 10.1016/j.bmcl.2016.09.072

Table 1.

Structure–activity relationship for JWS analogs containing a modified 4-nitropyridazine on targets relevant to neurocognitive disorders

graphic file with name nihms824135t1.jpg
R1 R2 AChE (IC50 µM) BuChE (IC50 µM) M1(%) M2(%) M3(%) M4(%)
JWS H H 0.47 10 80 97 32 74
5 Me Me 2.72 n.t. 74 63 48 67
6 Et Et 2.54 18.8 n.t. n.t. n.t. n.t.
7 H Me 0.68 28.4 79 78 46 57
8 H Ph 0.26 4.46 40 34 38 16
9 Ph H 0.46 22.7 40 37 27 18
10 Me Ph 0.16 3.71 84 72 63 58
11 Ph Me 0.72 n.t. 60 40 52 37
12 Ph Ph 0.19 7.05 76 51 73 48
13 Thiophene Thiophene 0.35 2.28 n.t. n.t. n.t. n.t.