Table 3.
UT-A1 Inhibition by 1,2,4-Triazoloquinoxalines with Different R3
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compound | R1 | R2 | R3 | isolated yield (%) |
UT-A1 IC50 (µM) |
8be | A | H | CH3 | 65 | 2.7 |
8bf | A | CH2CH3 | CH3 | 73 | 1.4 |
8bg | A | CH(CH3)2 | CH3 | 99 | 1.2 |
8bh | A | CH2CH2CH3 | CH3 | 80 | 0.4 |
8bi | A | H | Cl | 70 | >20 |
8bj | A | H | F | 67 | 1.2 |
8bk | B | H | F | 40 | 1.5 |
8bl | A | CH2CH2CH3 | F | 48 | 0.3 |