Výsledky vyhledávání - "Gregory B. Poli"

Discovery of an Orally Efficacious Inhibitor of Coagulation Factor Xa Which Incorporates a Neutral P1 Ligand

Publikováno v: Journal of Medicinal Chemistry. 46:681-684

The discovery and SAR of ketopiperazino methylazaindole factor Xa inhibitors are described. Structure-activity data suggesting that this class of inhibitors does not bind in the canonical mode were confirmed by an X-ray crystal structure showing the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::956fd950e025e469056ca84123c291bd
https://doi.org/10.1021/jm020384z

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A conformationally constrained inhibitor with an enhanced potency for β-tryptase and stability against semicarbazide-sensitive amine oxidase (SSAO)

Autor: Jie Wang, Qingping Wang, Roy J. Vaz, Guyan Liang, Jennifer Cairns, Keith Sides, Joseph T. Tsay, Zhicheng Zhao, Gregory T Stoklosa, Yong Mi Choi-Sledeski, Patrick Wai-Kwok Shum, Xin Chen, Anne Minnich, Gregory B. Poli, Thaddeus R. Nieduzak

Publikováno v: Bioorganicmedicinal chemistry letters. 20(22)

A novel β-tryptase inhibitor with a basic benzylamine P1 group, a piperidine-amide linker, and a substituted indole P4 group was discovered. A substitution at 4-indole position was introduced to constrain the conformational flexibility of the inhibi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5de7864d6da9350249661c5c64ee07b6
https://pubmed.ncbi.nlm.nih.gov/20855210

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Structure-based design, synthesis, and profiling of a β-tryptase inhibitor with a spiro-piperidineamide scaffold, benzylamine P1 group, and a substituted indole P4 group

Autor: Guyan Liang, Xin Chen, Gregory B. Poli, Qingping Wang, Yong Mi Choi-Sledeski, Roy J. Vaz, Joseph T. Tsay, Anne Minnich, Keith Sides

Publikováno v: MedChemComm. 2:794

A β-tryptase inhibitor with a basic benzylamine P1 group, a substituted indole P4 group, and a spiro-piperidineamide scaffold linker was designed, synthesized, and tested for its β-tryptase potency and ADMET properties. Comparing to its non-spiro a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a756fce5d94f38069ed857e17eefa56c
https://doi.org/10.1039/c1md00104c

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