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. Author manuscript; available in PMC: 2010 May 14.
Published in final edited form as: Bioorg Med Chem Lett. 2009 Jan 23;19(13):3686–3692. doi: 10.1016/j.bmcl.2009.01.057

Table 1.

PDE4A inhibition by compounds 5-10, 17 and 18.

Analogue # R1 R2 PDE4A
IC50 (nM)
graphic file with name nihms-191949-t0006.jpg 5 −OCH3 −OCH3 6.7 ± 0.4
6 −OCypent −OCH3 13 ± 0.8
7 −OCH2Cyprop −OCH3 6.1 ± 0.9
8 −OCH2Cyprop −OCHF2 11 ± 0.7
9 −O(3-THF)[rac] −OCH3 3.4 ± 0.4
10 −O(3-THF)[R] −OCH3 3.0 ± 0.2
17 −O(3-THF)[S] −OCH3 7.3 ± 3.8
18 −O(3-THF)[R] −OCH3 1.5 ± 0.7
*

data represents the results from three seperate experiments (SD provided). Definitions: OCH3 = methoxy, OCypent = cyclopentyloxy, OCH2Cyprop = cyclopropylmethoxy, OCHF2 = 2-difluoromethoxy, O(3-THF) = O-3-tetrahydrofuranyl [racemic, R or S enantiomers].