Highly efficient and versatile Synthesis of Libraries of constrained b-strand Mimetics

Cyprian Ogbu; Maher Qabar; P. Boatman; Jan Urban; Joseph Meara; Mark Ferguson; John Tulinsky; Chris Lum; Suresh Babu; Mark. Blaskovich; Hiroshi Nakanishi; Fuqiang Ruan; Bolong Cao; Ryan Minarik; Tom Little; Sherry Nelson; Minh Nguyen; Anna Gall; Michael Kahn

doi:10.3390/ecsoc-2-01688

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Parallel Synthesis of 1,2,3-Thiadiazoles Employing a "Catch and Release" Strategy

Highly efficient and versatile Synthesis of Libraries of constrained b-strand Mimetics

Cyprian O. Ogbu

¹,

Maher N Qabar

¹,

P. Douglas Boatman

¹,

Jan Urban

¹,

Joseph P. Meara

¹,

Mark D. Ferguson

¹,

John Tulinsky

¹,

Chris Lum

¹,

Suresh Babu

¹,

Mark. A. Blaskovich

¹,

Hiroshi Nakanishi

^{1, 2},

Fuqiang Ruan

¹,

Bolong Cao

¹,

Ryan Minarik

¹,

Tom Little

¹,

Sherry Nelson

¹,

Minh Nguyen

¹,

Anna Gall

¹,

Michael Kahn

^{*

1, 2}

¹ Molecumetics Ltd., 2023 120th Avenue NE, Bellevue,WA 98005-2199, U.S.A.
² University of Washington, Department of Pathobiology,SC-38, Seattle, WA 98195, U.S.A.

Published: 01 November 1998 by MDPI in The 2nd International Electronic Conference on Synthetic Organic Chemistry session Combinatorial Synthesis, Parallel Synthesis and Automation

https://doi.org/10.3390/ecsoc-2-01688

Abstract: The general approach of using a bicyclic template to produce inhibitors of the protease superfamily of enzymes has been investigated. The Diels-Alder cycloaddition reaction on solid support has been found to be highly efficient for the synthesis of libraries of compounds that mimic the b-strand secondary structure of proteins. Several potent and selective inhibitors of proteases have been discovered

Keywords: n/a

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