Nanomolar Inhibitors for Two Distinct Biological Target Families from a Single Synthetic Sequence: A Next Step in Combinatorial Library Design?

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 me...

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Bibliographic Details
Published in:Angewandte Chemie International Edition 1998-11, Vol.37 (20), p.2848-2850
Main Authors: Burns, Christopher J., Groneberg, Robert D., Salvino, Joseph M., McGeehan, Gerard, Condon, Stephen M., Morris, Robert, Morrissette, Matthew, Mathew, Rose, Darnbrough, Shelley, Neuenschwander, Kent, Scotese, Anthony, Djuric, Stevan W., Ullrich, John, Labaudiniere, Richard
Format: Article
Language:English
Subjects:
Combinatorial chemistry
Drug design
Enzyme inhibitors
Metalloenzymes
Phosphodiesterases
Online Access:Get full text
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Summary: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).
ISSN:1433-7851
1521-3773
DOI:10.1002/(SICI)1521-3773(19981102)37:20<2848::AID-ANIE2848>3.0.CO;2-C