Identification of a potent new chemotype for the selective inhibition of PDE4 |
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| Authors: | 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 |
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| Institution: | NIH Chemical Genomics Center, National Human Genome Research Institute, NIH, 9800 Medical Center Drive, MSC 3370, Bethesda, MD 20892-3370, USA. |
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| Abstract: | A series of substituted 3,6-diphenyl-7H-1,2,4]triazolo3,4-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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