Identification of a potent new chemotype for the selective inhibition of PDE4

AP Skoumbourdis, R Huang, N Southall…

Index: Skoumbourdis, Amanda P.; Huang, Ruili; Southall, Noel; Leister, William; Guo, Vicky; Cho, Ming-Hsuang; Inglese, James; Nirenberg, Marshall; Austin, Christopher P.; Xia, Menghang; Thomas, Craig J. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 4 p. 1297 - 1303

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Citation Number: 27

Abstract

A series of substituted 3, 6-diphenyl-7H-[1, 2, 4] triazolo [3, 4-b][1, 3, 4] thiadiazines were prepared and analyzed as inhibitors of phosphodiesterase 4 (PDE4). Synthesis, structure– activity relationships, and the selectivity of a highly potent analogue against related phosphodiesterase isoforms are presented.

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