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

Autor:	Christopher J. Burns, Shelley Darnbrough, Salvino Joseph M, Groneberg Robert D, Stevan W. Djuric, Matthew M. Morrissette, Robert L. Morris, Kent Neuenschwander, Richard Labaudiniere, Rose Mathew, Anthony C. Scotese, Stephen M. Condon, Gerard McGeehan, John W. Ullrich
Rok vydání:	1998
Předmět:	Library design Biological target Computer science Design elements and principles Sequence (biology) General Chemistry Pharmacophore Multiple target Combinatorial chemistry Catalysis
Zdroj:	Angewandte Chemie International Edition. 37:2848-2850
ISSN:	1521-3773 1433-7851
DOI:	10.1002/(sici)1521-3773(19981102)37:20<2848::aid-anie2848>3.0.co;2-c
Popis:	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).
Databáze:	OpenAIRE
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