10 Papers
60 Citations
Powell Eugene is an academic researcher from Johnson & Johnson Pharmaceutical Research and Development. The author has contributed to research in topics: Serine protease & Proteases. The author has an hindex of 6, co-authored 10 publications.
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Papers
Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase.
Michael N. Greco,Michael J. Hawkins,Powell Eugene,Harold R. Almond,Lawrence de Garavilla,Jeffrey Hall,Lisa Minor,Yuanping Wang,Thomas W. Corcoran,Enrico Di Cera,Angelene M. Cantwell,Savvas N. Savvides,Bruce P. Damiano,Bruce E. Maryanoff +13 more
TL;DR: A series of beta-carboxamido-phosphon(in)ic acids was identified as a new structural motif for obtaining potent inhibitors of human mast cell chymase and revealed key interactions within the enzyme active site.
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Nonpeptide inhibitors of cathepsin G: optimization of a novel beta-ketophosphonic acid lead by structure-based drug design.
Michael N. Greco,Michael J. Hawkins,Powell Eugene,Harold R. Almond,Thomas W. Corcoran,Lawrence de Garavilla,Jack A. Kauffman,Rosario Recacha,Debashish Chattopadhyay,Patricia Andrade-Gordon,Bruce E. Maryanoff +10 more
TL;DR: It is evident that the beta-ketophosphonic acid unit can form the basis for a novel class of serine protease inhibitors.
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Orally Active Benzamide Antipsychotic Agents with Affinity for Dopamine D2, Serotonin 5-HT1A, and Adrenergic α1 Receptors
Allen B. Reitz,Ellen W. Baxter,Ellen E. Codd,Coralie B. Davis,Alfonzo D. Jordan,Bruce E. Maryanoff,Cynthia A. Maryanoff,Mcdonnell Mark E,Powell Eugene,Michael J. Renzi,Mary R. Schott,Malcolm K. Scott,Richard P. Shank,Jeffry L. Vaught +13 more
TL;DR: The design, synthesis, and evaluation of a series of related (aminomethyl)benzamides in assays predictive of antipsychotic activity in humans, which had notable affinity for dopamine D2, serotonin 5-HT1A, and alpha1-adrenergic receptors are described.
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Novel thrombin inhibitors that are based on a macrocyclic tripeptide motif
Michael N. Greco,Powell Eugene,Leonard R. Hecker,Patricia Andrade-Gordon,Jack A. Kauffman,Joan M. Lewis,Venkatapathy Ganesh,Alexander Tulinsky,Bruce E. Maryanoff +8 more
TL;DR: A series of macrocyclic α-keto amides containing the D-Phe-Pro-Arg (fPR) motif were synthesized and evaluated in vitro as inhibitors of human α-thrombin and bovine trypsin this paper.
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Benzothiazole hydroxy ureas as inhibitors of 5-lipoxygenase: use of the hydroxyurea moiety as a replacement for hydroxamic acid.
TL;DR: A novel series of N-[(2-benzothiazolylthio)alkyl]-N'-hydroxyurea derivatives (9-25) was synthesized and evaluated for biological activity as inhibitors of 5-lipoxygenase both in vivo and in vitro.
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