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. 2017 Sep 15;8(10):1105–1109. doi: 10.1021/acsmedchemlett.7b00300

Table 1. Inhibitory Profile of Compounds 2ai against hCA I, II, IV, and VIIa.

    Ki (nM)
compd (Het)Ar hCA I hCA II hCA IV hCA VII
2a Ph 466.1 376.5 3912.1 6.8
2b 4-ClC6H4 453.0 182.1 608.2 0.96
2c 4-FC6H4 428.7 742.2 1036.5 9.4
2d 4-MeOC6H4 317.9 53.3 3643.4 0.97
2e 2-MeC6H4 70.7 61.7 961.2 0.93
2f 2-EtOC6H4 216.3 866.5 2299.7 0.84
2g 3,4-(MeO)2C6H4 847.6 723.6 8302.6 0.87
2h 3-pyridyl 316.0 848.3 1826.6 0.84
2i 5-pyrimidinyl 274.5 703.2 2296.0 0.83
1a 4-FC6H4 2343.0 76.1 9726.0 303.5
1b 4-ClC6H4 960.5 46.7 8142.0 269.0
AAZ   250.0 12.1 74.0 6.0
a

Mean Ki values from three different stopped-flow assays (errors were in the range of ±5–10% of the reported values). Inhibitory profile of compounds 1ab23 is provided for comparison.