Search Results - "McAtee, Jeff"
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Exploration of the P1 residue in 3CL protease inhibitors leading to the discovery of a 2-tetrahydrofuran P1 replacement
Published in Bioorganic & medicinal chemistry (15-02-2024)“…[Display omitted] •P1 analogues with aldehyde warhead prepared and tested against 3CLpro in SARS-CoV-2.•Discovery of 2-THF as P1 residue with potent inhibition…”
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Cassette dosing for pharmacokinetic screening in drug discovery: comparison of clearance, volume of distribution, half-life, mean residence time, and oral bioavailability obtained by cassette and discrete dosing in rats
Published in Journal of pharmaceutical sciences (01-09-2011)“…The purpose of this investigation was to compare selected pharmacokinetic (PK) parameters obtained by cassette and discrete dosing of compounds in rats. The…”
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Discovery of 1-(1,3,5-triazin-2-yl)piperidine-4-carboxamides as inhibitors of soluble epoxide hydrolase
Published in Bioorganic & medicinal chemistry letters (15-06-2013)“…1-(1,3,5-Triazin-yl)piperidine-4-carboxamide inhibitors of soluble epoxide hydrolase were identified from high through-put screening using encoded library…”
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The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore
Published in Bioorganic & medicinal chemistry letters (01-09-2013)“…Lead optimization of piperidine amide HTS hits, based on an anilino-thiazole core, led to the identification of analogs which displayed low nanomolar blocking…”
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Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid‑4 (TRPV4)
Published in Journal of medicinal chemistry (08-11-2018)“…A novel series of pyrrolidine sulfonamide transient receptor potential vanilloid-4 (TRPV4) antagonists was developed by modification of a previously reported…”
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