Výsledky vyhledávání - "Kevin M. McGowan"

Towards a TREK-1/2 (TWIK-Related K+ Channel 1 and 2) dual activator tool compound: Multi-dimensional optimization of BL-1249

Autor: Joshua M. Wieting, Darren W. Engers, Haruto Kurata, Kevin M. McGowan, Takahiro Mori, Yuzo Iwaki, Thomas M. Bridges, Kentaro Yashiro, Craig W. Lindsley, Jerod S. Denton, Masaya Kokubo

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 29:1601-1604

This letter describes a focused, multi-dimensional optimization campaign around BL-1249, a fenamate class non-steroidal anti-inflammatory and a known activator of the K2P potassium channels TREK-1 (K2P2.1) and TREK-2 (K2P10.1). While BL-1249 has been

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::60bbe63c14adcf6638d2f3aed00c6a65
https://doi.org/10.1016/j.bmcl.2019.04.048

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Prevalence and Outcomes of Multi-Drug Resistant Blood Stream Infections Among Nursing Home Residents Admitted to an Acute Care Hospital

Autor: Sainfer Aliyu, Kevin M McGowan, Lama Kanawati, Seife Yohannes, Maria Elena Ruiz, Dilbi Hussain

Publikováno v: Journal of intensive care medicine. 37(4)

Objective: The prevalence of multi-drug resistant organism (MDRO) colonization in nursing home residents has been well documented, but little is known about the impact of MDRO bloodstream infections (BSIs). The aim of this study was to assess the pre

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b833e8c44d06a2d24859b4e86f0e73c8
https://pubmed.ncbi.nlm.nih.gov/33938320

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VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides

Autor: Colleen M. Niswender, Kevin M. McGowan, Carson W. Reed, Jerri M. Rook, Vincent B. Luscombe, Craig W. Lindsley, Annie L. Blobaum, Darren W. Engers, Matthew T. Loch, Hanna F. Roenfanz, P. Jeffrey Conn, Branden J. Stansley, Alice L. Rodriguez, Paul K. Spearing, Eileen M. Engelberg, Daniel H. Remke

Publikováno v: ACS Medicinal Chemistry Letters. 8:1326-1330

Herein, we report the structure–activity relationships within a series of mGlu7 NAMs based on an N-(2-(1H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamide core with excellent CNS penetration (Kp 1.9–5.8 and Kp,uu 0.4–1.4). Analogues in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::97d6c42ce8acd7d17c8e70f2dbcf2dd5
https://doi.org/10.1021/acsmedchemlett.7b00429

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Selective inhibition of M5 muscarinic acetylcholine receptors attenuates cocaine self-administration in rats

Autor: Kevin M. McGowan, Craig W. Lindsley, Barak W. Gunter, Michael Bubser, Carrie K. Jones, Robert W. Gould

Publikováno v: Addiction Biology. 23:1106-1116

Cocaine use disorder (CUD) remains a debilitating health problem in the United States for which there are no Food and Drug Administration-approved treatment options. Accumulating anatomical and electrophysiological evidence indicates that the muscari

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d72e6f519a0b80191df3ff1fea177107
https://doi.org/10.1111/adb.12567

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One pot synthesis of unsymmetrical ketones from carboxylic and boronic acids via PyClU-mediated acylative Suzuki coupling

Autor: Kevin M. McGowan, Steven W. Ingram, Pedro M. Garcia-Barrantes, Craig W. Lindsley

Publikováno v: Tetrahedron Letters. 58:898-901

A synthetic procedure for the preparation of ketones from easily accessible carboxylic acids has been developed. This methodology proceeds via in situ activation of the carboxylic acid with PyClU, followed by the palladium-catalyzed acylative cross-c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9c3e85cfaf0e53ef1644cd8408f7a9b7
https://doi.org/10.1016/j.tetlet.2017.01.064

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Continued optimization of the M 5 NAM ML375: Discovery of VU6008667, an M 5 NAM with high CNS penetration and a desired short half-life in rat for addiction studies

Autor: Kevin M. McGowan, Craig W. Lindsley, Hykeyung P. Cho, Carrie K. Jones, P. Jeffrey Conn, Thomas M. Bridges, Kellie D. Nance

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 27:1356-1359

This letter describes the continued optimization of M5 NAM ML375 (VU0483253). While a valuable in vivo tool compound, ML375has an excessively long elimination half-life in rat (t1/2=80h), which can be problematic in certain rodent addiction paradigms

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5aaf9531d7c6a4972102842847a3d385
https://doi.org/10.1016/j.bmcl.2017.02.020

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Ligand-based virtual screen for the discovery of novel M5 inhibitor chemotypes

Autor: Kellie D. Nance, Alexander R. Geanes, P. Jeffrey Conn, Hykeyung P. Cho, Craig W. Lindsley, Carrie K. Jones, Kevin M. McGowan, Jens Meiler

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 26:4487-4491

This letter describes a ligand-based virtual screening campaign utilizing SAR data around the M5 NAMs, ML375 and VU6000181. Both QSAR and Shape scores were employed to virtually screen a 98,000-member compound library. Neither approach alone proved p

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dff9a41213b4cdedc46065cafa95286b
https://doi.org/10.1016/j.bmcl.2016.07.071

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Biological activity of the bryostatin analog Merle 23 on mouse epidermal cells and mouse skin

Autor: Gary E. Keck, Michelle A. Herrmann, Jin-Qiu Chen, Stuart H. Yuspa, Peter M. Blumberg, Mark E. Petersen, David O. Baumann, Jessica S. Kelsey, Christophe Cataisson, Kevin M. McGowan

Publikováno v: Molecular Carcinogenesis. 55:2183-2195

Bryostatin 1, a complex macrocyclic lactone, is the subject of multiple clinical trials for cancer chemotherapy. Although bryostatin 1 biochemically functions like the classic mouse skin tumor promoter phorbol 12-myristate 13-acetate (PMA) to bind to

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1cf21fdb97208f40efb8a23f346bf97b
https://doi.org/10.1002/mc.22460

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A Multimodal Sepsis Quality-Improvement Initiative Including 24/7 Screening and a Dedicated Sepsis Response Team-Reduced Readmissions and Mortality

Autor: Sean Shenghsiu Huang, Andrea Ryan, Kevin M McGowan, Seife Yohannes, Muhtadi Alnababteh

Publikováno v: Critical Care Explorations

Objectives: To evaluate if a hospitalwide sepsis performance improvement initiative improves compliance with the Centers for Medicare and Medicaid Services-mandated sepsis bundle interventions and patient outcomes. Study Design: Retrospective analysi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::47b9a865c5584e9612dcbf15fd2d46d8
https://doi.org/10.1097/cce.0000000000000251

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Synthesis and Biological Evaluation of Fluorescent Bryostatin Analogues

Autor: Xiaoling Luo, Noemi Kedei, Kevin M. McGowan, Thomas Cummins, Agnes Czikora, Randall C. Johnson, Jin-Qiu Chen, Mark E. Petersen, Gary E. Keck, Peter M. Blumberg, Nancy E. Lewin, Sharon Kirk, Sarangan Ravichandran

Publikováno v: Chembiochem : a European journal of chemical biology. 19(8)

To investigate the cellular distribution of tumor-promoting vs. non-tumor-promoting bryostatin analogues, we synthesized fluorescently labeled variants of two bryostatin derivatives that have previously shown either phorbol ester-like or bryostatin-l

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bf1fdd692691f0eccdddc0baf6b905b6
https://pubmed.ncbi.nlm.nih.gov/29424951

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