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. 2015 Mar 11;59(4):1977–1982. doi: 10.1128/AAC.04149-14

TABLE 3.

Comparative activities of 3-diarylether ELQs containing 6-position halogens and 7-position OCH3 groups

ELQ Substituent at position:
IC50 value (nM) or ratio fora:
3 6 7 Dd2 C2B/Dd2 D1/Dd2
271 DAEb H H 12 2.8 0.2
298 DAE H OCH3 5.5 0.7 0.8
314 DAE F H 33 1.3 3.4
316 DAE F OCH3 3.1 1.1 3.6
296 DAE Cl H 29 0.9 16
300 DAE Cl OCH3 6.6 0.7 24
339 DAE Br H 170 1.1 14
340 DAE Br OCH3 25 0.4 65
a

IC50 values were averaged from ≥3 independent experiments run in triplicate. The standard deviations were <10%.

b

DAE, para-OCF3 diaryl ether side chain, as present in ELQ-300.