title: Identification of a potent new chemotype for the selective inhibition of PDE4.
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.
authors.affiliation: NIH Chemical Genomics Center, National Human Genome Research Institute, NIH, 9800 Medical Center Drive, MSC 3370, Bethesda, MD 20892-3370, USA.
authors.forename: Amanda P
authors.initials: AP
authors.lastname: Skoumbourdis
authors.forename: Ruili
authors.initials: R
authors.lastname: Huang
authors.forename: Noel
authors.initials: N
authors.lastname: Southall
authors.forename: William
authors.initials: W
authors.lastname: Leister
authors.forename: Vicky
authors.initials: V
authors.lastname: Guo
authors.forename: Ming-Hsuang
authors.initials: MH
authors.lastname: Cho
authors.forename: James
authors.initials: J
authors.lastname: Inglese
authors.forename: Marshall
authors.initials: M
authors.lastname: Nirenberg
authors.forename: Christopher P
authors.initials: CP
authors.lastname: Austin
authors.forename: Menghang
authors.initials: M
authors.lastname: Xia
authors.forename: Craig J
authors.initials: CJ
authors.lastname: Thomas
mesh_terms: D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors; D058988:Phosphodiesterase 4 Inhibitors; D010726:Phosphodiesterase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013829:Thiadiazines / Q000737:chemistry* / Q000494:pharmacology*; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D007527:Isoenzymes; D058988:Phosphodiesterase 4 Inhibitors; D010726:Phosphodiesterase Inhibitors; D013829:Thiadiazines; D014230:Triazoles