Nanomolar Inhibitors for Two Distinct Biological Target Families from a Single Synthetic Sequence: A Next Step in Combinatorial Library Design?
✍ Scribed by Christopher J. Burns; Robert D. Groneberg; Joseph M. Salvino; Gerard McGeehan; Stephen M. Condon; Robert Morris; Matthew Morrissette; Rose Mathew; Shelley Darnbrough; Kent Neuenschwander; Anthony Scotese; Stevan W. Djuric; John Ullrich; Richard Labaudiniere
- Publisher
- John Wiley and Sons
- Year
- 1998
- Tongue
- English
- Weight
- 101 KB
- Volume
- 37
- Category
- Article
- ISSN
- 0044-8249
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✦ Synopsis
One common synthetic route creates small-molecule libraries directed toward two functionally distinct target families. The novel structural template 1 can independently display the necessary pharmacophore patterns for inhibition of members of two different biomolecular target families, the matrix metalloproteinases (MMPs) or the phosphodiesterases (PDEs). The incorporation of multiple target family directed design elements into combinatorial library design could help expedite the pharmaceutical lead discovery process. Z=OR' (PDE4), H (MMPs).