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Apremilast, a cAMP phosphodiesterase-4 inhibitor, demonstrates anti-inflammatory activity in vitro and in a model of psoriasis.
Schafer PH, Parton A, Gandhi AK, Capone L, Adams M, Wu L, Bartlett JB, Loveland MA, Gilhar A, Cheung YF, Baillie GS, Houslay MD, Man HW, Muller GW, Stirling DI. Schafer PH, et al. Among authors: stirling di. Br J Pharmacol. 2010 Feb;159(4):842-55. doi: 10.1111/j.1476-5381.2009.00559.x. Epub 2009 Dec 24. Br J Pharmacol. 2010. PMID: 20050849 Free PMC article.
Thalidomide analogs and PDE4 inhibition.
Muller GW, Shire MG, Wong LM, Corral LG, Patterson RT, Chen Y, Stirling DI. Muller GW, et al. Among authors: stirling di. Bioorg Med Chem Lett. 1998 Oct 6;8(19):2669-74. doi: 10.1016/s0960-894x(98)00475-2. Bioorg Med Chem Lett. 1998. PMID: 9873600
Discovery of (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitor.
Man HW, Schafer P, Wong LM, Patterson RT, Corral LG, Raymon H, Blease K, Leisten J, Shirley MA, Tang Y, Babusis DM, Chen R, Stirling D, Muller GW. Man HW, et al. J Med Chem. 2009 Mar 26;52(6):1522-4. doi: 10.1021/jm900210d. J Med Chem. 2009. PMID: 19256507
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