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Can I read 1,5-Substituted nipecotic amides: Selective PDE8 inhibitors displaying diastereomer-dependent microsomal stability on EtoBox?
1,5-Substituted nipecotic amides: Selective PDE8 inhibitors displaying diastereomer-dependent microsomal stability by Michael P. DeNinno; Stephen W. Wright; Michael S. Visser; John B. Etienne; Dianna E. Moore; Thanh V. Olson; Benjamin N. Rocke; Melissa P. Andrews; Cynthia Zarbo; Michele L. Millham; Brian P. Boscoe; David D. Boyer; Shawn D. Doran; Karen L. Houseknecht is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is 1,5-Substituted nipecotic amides: Selective PDE8 inhibitors displaying diastereomer-dependent microsomal stability about?
The first highly potent and selective PDE8 inhibitors are disclosed. The initial tetrahydroisoquinoline hit was transformed into a nipecotic amide series in order to address a reactive metabolite issue. Reduction of lipophilicity to address metabolic liabilities uncovered an interesting diastereomer-dependent trend in turnover by human microsomes.
Who reads 1,5-Substituted nipecotic amides: Selective PDE8 inhibitors displaying diastereomer-dependent microsomal stability?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Michael P. DeNinno; Stephen W. Wright; Michael S. Visser; John B. Etienne; Dianna E. Moore; Thanh V. Olson; Benjamin N. Rocke; Melissa P. Andrews; Cynthia Zarbo; Michele L. Millham; Brian P. Boscoe; David D. Boyer; Shawn D. Doran; Karen L. Houseknecht
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)
- Published
- 2011
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)