Bioorg Med Chem Lett. 2008 Feb 15;18(4):1297-303. Epub 2008 Jan 11.

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

Skoumbourdis AP, Huang R, Southall N, Leister W, Guo V, Cho MH, Inglese J, Nirenberg M, Austin CP, Xia M, Thomas CJ.

Source

NIH Chemical Genomics Center, National Human Genome Research Institute, NIH, 9800 Medical Center Drive, MSC 3370, Bethesda, MD 20892-3370, USA.

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.

PMID:: 18243697; [PubMed - indexed for MEDLINE]
PMCID:: PMC2268978

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