Search Results - "Schrimpf, Michael"
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Avian behaviour changes in response to human activity during the COVID-19 lockdown in the United Kingdom
Published in Proceedings of the Royal Society. B, Biological sciences (28-09-2022)“…Human activities may impact animal habitat and resource use, potentially influencing contemporary evolution in animals. In the United Kingdom, COVID-19…”
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Antiviral Drug Discovery for the Treatment of COVID-19 Infections
Published in Viruses (04-05-2022)“…The coronavirus disease 2019 (COVID-19) pandemic is caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), a recently emerged human…”
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3
Regional breeding bird assessment of the Antarctic Peninsula
Published in Polar biology (01-02-2020)“…Conservation of seabirds in remote polar regions requires accurate information on the location of breeding sites, which is often limited by logistical…”
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4
Reduced human activity during COVID-19 alters avian land use across North America
Published in Science advances (24-09-2021)“…The COVID-19 pandemic resulted in extraordinary declines in human mobility, which, in turn, may affect wildlife. Using records of more than 4.3 million birds…”
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5
Development of a sensitive high-throughput enzymatic assay capable of measuring sub-nanomolar inhibitors of SARS-CoV2 Mpro
Published in SLAS discovery (01-09-2024)“…The SARS-CoV-2 main protease (Mpro) is essential for viral replication because it is responsible for the processing of most of the non-structural proteins…”
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Metabolism and Disposition of a Novel Selective α 7 Neuronal Acetylcholine Receptor Agonist ABT-126 in Humans: Characterization of the Major Roles for Flavin-Containing Monooxygenases and UDP-Glucuronosyl Transferase 1A4 and 2B10 in Catalysis
Published in Drug metabolism and disposition (01-04-2018)“…Mass balance, metabolism, and excretion of ABT-126, an 7 neuronal acetylcholine receptor agonist, were characterized in healthy male subjects ( = 4) after a…”
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Metabolism and Disposition of a Novel Selective α7 Neuronal Acetylcholine Receptor Agonist ABT-126 in Humans: Characterization of the Major Roles for Flavin-Containing Monooxygenases and UDP-Glucuronosyl Transferase 1A4 and 2B10 in Catalysis
Published in Drug metabolism and disposition (01-04-2018)“…Mass balance, metabolism, and excretion of ABT-126, an α7 neuronal acetylcholine receptor agonist, were characterized in healthy male subjects (n = 4) after a…”
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8
Discovery of ABBV/GLPG-3221, a Potent Corrector of CFTR for the Treatment of Cystic Fibrosis
Published in ACS medicinal chemistry letters (14-11-2019)“…Cystic fibrosis (CF) is a genetic disorder that affects multiple tissues and organs. CF is caused by mutations in the CFTR gene, resulting in insufficient or…”
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Phytoplankton Communities in Green Bay, Lake Michigan after Invasion by Dreissenid Mussels: Increased Dominance by Cyanobacteria
Published in Diversity (Basel) (2014)“…Biological invasions of aquatic systems disrupt ecological communities, and cause major changes in diversity and ecosystem function. The Laurentian Great Lakes…”
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10
Trade-offs in prey quality and quantity revealed through the behavioral compensation of breeding seabirds
Published in Marine ecology. Progress series (Halstenbek) (24-07-2012)“…Many productive ocean ecosystems are also highly variable, resulting in complex trophic interactions. We analyzed interannual patterns in the diet of a…”
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SAR of α7 nicotinic receptor agonists derived from tilorone: Exploration of a novel nicotinic pharmacophore
Published in Bioorganic & medicinal chemistry letters (15-02-2012)“…The well-known interferon-inducer tilorone was found to possess potent affinity for the agonist site of the α7 neuronal nicotinic receptor (Ki=56nM). SAR…”
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12
Synthesis and SAR of 4-aminocyclopentapyrrolidines as orally active N-type calcium channel inhibitors for inflammatory and neuropathic pain
Published in Bioorganic & medicinal chemistry letters (01-09-2013)“…A novel series of N-type calcium channel inhibitors have been discovered. Optimization of potency and HT-ADME properties provides 4-aminocyclopentapyrrolidines…”
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13
A Model Approach for Estimating Colony Size, Trends, and Habitat Associations of Burrow-Nesting Seabirds
Published in The Condor (Los Angeles, Calif.) (01-05-2013)“…We present a prototype monitoring strategy for estimating the density and number of occupied burrows of burrow-nesting seabirds. We use data and management…”
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14
SAR of alpha 7 nicotinic receptor agonists derived from tilorone: Exploration of a novel nicotinic pharmacophore
Published in Bioorganic & medicinal chemistry letters (15-02-2012)“…The well-known interferon-inducer tilorone was found to possess potent affinity for the agonist site of the alpha 7 neuronal nicotinic receptor (Ki = 56 nM)…”
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15
Synthesis and evaluation of new radioligands [11 C]A-833834 and [11 C]A-752274 for positron-emission tomography of α7-nicotinic acetylcholine receptors
Published in Nuclear medicine and biology (01-04-2013)“…Abstract Introduction α7-nicotinic acetylcholine receptor (α7-nAChR) is one of the major neuronal nAChR subtypes. α7-nAChR is involved in variety of neuronal…”
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16
Structure−Activity Studies and Analgesic Efficacy of N-(3-Pyridinyl)-Bridged Bicyclic Diamines, Exceptionally Potent Agonists at Nicotinic Acetylcholine Receptors
Published in Journal of medicinal chemistry (26-07-2007)“…A series of exceptionally potent agonists at neuronal nicotinic acetylcholine receptors (nAChRs) has been investigated. Several N-(3-pyridinyl) derivatives of…”
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17
Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors
Published in Bioorganic & medicinal chemistry letters (15-03-2009)“…Several N-pyridin-3-yl spirobicyclic diamines, designed as conformationally restricted analogs of tebanicline (ABT-594), were synthesized as novel ligands for…”
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18
Design of ligands for the nicotinic acetylcholine receptors: the quest for selectivity
Published in Current topics in medicinal chemistry (2004)“…In the last decade, nicotinic acetylcholine receptors (nAChRs) have emerged as important targets for drug discovery. The therapeutic potential of nicotinic…”
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Synthesis and Structure−Activity Relationship Studies of 3,6-Diazabicyclo[3.2.0]heptanes as Novel α4β2 Nicotinic Acetylcholine Receptor Selective Agonists
Published in Journal of medicinal chemistry (01-11-2007)“…A series of novel, potent neuronal nicotinic acetylcholine receptor (nAChR) ligands derived from 3,6-diazabicyclo[3.2.0]heptane have been synthesized and…”
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20
Syntheses and structure–activity relationship (SAR) studies of 2,5-diazabicyclo[2.2.1]heptanes as novel α7 neuronal nicotinic receptor (NNR) ligands
Published in Bioorganic & medicinal chemistry letters (15-06-2010)“…A series of biaryl substituted 2,5-diazabicyclo[2.2.1]heptanes were synthesized as potent and selective α7 NNR agonists. Among them, compound 18e shows a α7…”
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