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Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors by Amanda P. Skoumbourdis; Christopher A. LeClair; Eduard Stefan; Adrian G. Turjanski; William Maguire; Steven A. Titus; Ruili Huang; Douglas S. Auld; James Inglese; Christopher P. Austin; Stephen W. Michnick; Menghang Xia; Craig J. Thomas is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors about?
An expansion of structure-activity studies on a series of substituted 7H- [1,2,4]triazolo [3,4-b][1,3,4]thiadiazine PDE4 inhibitors and the introduction of a related [1,2,4]triazolo [4,3-b]pyridazine based inhibitor of PDE4 is presented. The development of SAR included strategic incorporation of known substituents on the critical catachol diether moiety of the 6-phenyl appendage on each heterocyclic core. From these studies, (R ) were identified as highly potent PDE4A inhibitors. Each of these analogues was submitted across a panel of 21 PDE family members and was shown to be highly selective for PDE4 isoforms (PDE4A, PDE4B, PDE4C, PDE4D). Both 10 and 18 were then evaluated in divergent cell-based assays to assess their relevant use as probes of PDE4 activity. Finally, docking studies with selective ligands (including 10 and 18) were undertaken to better understand this chemotypes ability to bind and inhibit PDE4 selectively.
Who reads Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Amanda P. Skoumbourdis; Christopher A. LeClair; Eduard Stefan; Adrian G. Turjanski; William Maguire; Steven A. Titus; Ruili Huang; Douglas S. Auld; James Inglese; Christopher P. Austin; Stephen W. Michnick; Menghang Xia; Craig J. Thomas
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)
- Published
- 2009
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)