Lois L. Wright
Research Triangle Park
42 Papers
485 Citations
Lois L. Wright is an academic researcher from Research Triangle Park. The author has contributed to research in topics: Cathepsin K & Protease. The author has an hindex of 21, co-authored 42 publications.
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Papers
Novel Rho Kinase Inhibitors with Anti-inflammatory and Vasodilatory Activities
Chris P. Doe,Ross G. Bentley,David J. Behm,Robert Lafferty,Robert A. Stavenger,David Kendall Jung,Mark James Bamford,Terry Panchal,Eugene T. Grygielko,Lois L. Wright,Gary K. Smith,Zunxuan Chen,Christine Webb,Sanjay S. Khandekar,Tracey Yi,Robert B. Kirkpatrick,Edward Dul,Larry J. Jolivette,Joseph P. Marino,Robert N. Willette,Dennis Lee,Erding Hu +21 more
TL;DR: Two aminofurazan-based ROCK inhibitors are characterized, GSK269962A and SB-772077-B, as members of a novel class of compounds that potently inhibit ROCK enzymatic activity and may enable us to further evaluate the potential beneficial effects of ROCK inhibition in animal models of cardiovascular as well as other chronic diseases.
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Discovery of Aminofurazan-azabenzimidazoles as Inhibitors of Rho-Kinase with High Kinase Selectivity and Antihypertensive Activity
Robert A. Stavenger,Haifeng Cui,Sarah E. Dowdell,Robert G. Franz,Dimitri Gaitanopoulos,Krista B. Goodman,Mark A. Hilfiker,Robert L. Ivy,Jack D. Leber,Joseph P. Marino,Hye-Ja Oh,Andrew Q. Viet,Weiwei Xu,Guosen Ye,Daohua Zhang,Yongdong Zhao,Larry J. Jolivette,Martha S. Head,Semus Simon,Patricia A. Elkins,Robert B. Kirkpatrick,Edward Dul,Sanjay S. Khandekar,Tracey Yi,David Kendall Jung,Lois L. Wright,Gary K. Smith,David J. Behm,Christopher P. Doe,Ross Bentley,Zunxuan X. Chen,Erding Hu,Dennis Lee +32 more
TL;DR: Appropriate substitution on the 6-position of the azabenzimidazole core provided subnanomolar enzyme potency in vitro while dramatically improving selectivity over a panel of other kinases.
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Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds
Andrew Spaltenstein,Merrick R. Almond,William J. Bock,Darryl Cleary,Furfine Eric Steven,Richard J. Hazen,Wieslaw M. Kazmierski,Francesco G. Salituro,Roger D. Tung,Lois L. Wright +9 more
TL;DR: In this paper, a trans 3,5-dibenzyl-2-oxo pyrrolidinone ring system was used to synthesize a 50 pM enzyme inhibitor against HIV protease in vitro.
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Discovery of potent pyrrolidone-based HIV-1 protease inhibitors with enhanced drug-like properties.
TL;DR: Pyrrolidone 2-based inhibitors exemplified by 17b and 19b are identified, which uniquely accommodate both high enzyme potency and which provide a platform for fine-tuning of drug-like properties in this class of PIs by additional chemical manipulations on the meta-position.
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Novel and potent cyclic cyanamide-based cathepsin K inhibitors.
David N. Deaton,Anne M. Hassell,Robert B. McFadyen,Aaron B. Miller,Larry R. Miller,Lisa M. Shewchuk,Francis X. Tavares,Derril H. Willard,Lois L. Wright +8 more
TL;DR: Starting from a PDE IV inhibitor hit derived from high throughput screening of the compound collection, a key pyrrolidine cyanamide pharmacophore was identified and modifications of the pyrrollidine ring produced enhancements in cathepsin K inhibition.
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