Výsledky vyhledávání - "Christopher D Aretz"

Synthesis and Biological Characterization of a Series of 2-Sulfonamidebenzamides as Allosteric Modulators of MrgX1

Autor: Swagat Sharma, Qi Peng, Anish K. Vadukoot, Christopher D. Aretz, Aaron A. Jensen, Alexander I. Wallick, Xinzhong Dong, Corey R. Hopkins

Publikováno v: ACS Med Chem Lett

[Image: see text] The present study describes our continued efforts in the discovery and characterization of a series of 2-sulfonamidebenzamides as allosteric modulators of MrgX1. MrgX1 has been shown to be an attractive target as a nonopioid recepto

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c41db227b3095c3d83563ef62827730c
https://pubmed.ncbi.nlm.nih.gov/35586421

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Synthesis and SAR Studies of 1H-Pyrrolo[2,3-b]pyridine-2-carboxamides as Phosphodiesterase 4B (PDE4B) Inhibitors

Autor: Cortney E. Heim, Nagsen Gautam, Amy Aldrich, Sushil Kumar, Swagat Sharma, Anish K. Vadukoot, Yazen Alnouti, Christopher D. Aretz, Corey R. Hopkins, Tammy Kielian

Publikováno v: ACS Med Chem Lett

[Image: see text] Herein we report the synthesis, SAR, and biological evaluation of a series of 1H-pyrrolo[2,3-b]pyridine-2-carboxamide derivatives as selective and potent PDE4B inhibitors. Compound 11h is a PDE4B preferring inhibitor and exhibited a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e282c52fb693d94bf235e60cf8e8ca31
https://doi.org/10.1021/acsmedchemlett.9b00369

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Further synthesis and biological characterization of a series of 2-sulfonamidebenzamides as allosteric modulators of MrgX1

Autor: Corey R. Hopkins, Xinzhong Dong, Swagat Sharma, Qi Peng, Alexander Wallick, Christopher D Aretz, Anish K. Vadukoot, Aaron Jensen

The present study describes our continued efforts in the discovery and characterization of a series of 2-sulfonamidebenzamides as allosteric modulators of MrgX1. MrgX1 has been shown to be an attractive target as a non-opioid receptor for the potenti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7660425de7c53565282262c8d207f26e
https://doi.org/10.33774/chemrxiv-2021-7cq5k

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Discovery, synthesis and biological characterization of a series of N-(1-(1,1-dioxidotetrahydrothiophen-3-yl)-3-methyl-1H-pyrazol-5-yl)acetamide ethers as novel GIRK1/2 potassium channel activators

Autor: Christopher D. Aretz, Yazen Alnouti, Lauren Lesiak, C. David Weaver, Yashpal S. Chhonker, Nikilesh V. Dhuria, Sushil Kumar, Yu Du, Nagsen Gautam, Swagat Sharma, Corey R. Hopkins

Publikováno v: RSC Med Chem

The present study describes the discovery and characterization of a series of N-(1-(1,1-dioxidotetrahydrothiophen-3-yl)-3-methyl-1H-pyrazol-5-yl)acetamide ethers as G protein-gated inwardly-rectifying potassium (GIRK) channel activators. From our pre

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2820c33e200f746c3cd7ae11f0a6780c
https://europepmc.org/articles/PMC8372201/

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Further SAR on the (Phenylsulfonyl)piperazine Scaffold as Inhibitors of the Aedes aegypti Kir1 (AeKir) Channel and Larvicides

Autor: Sujay V. Kharade, Christopher D. Aretz, Renata Rusconi Trigueros, Jerod S. Denton, Corey R. Hopkins, Erick J. Martinez Rodriguez, Peter M. Piermarini, Keagan S. Chronister

Publikováno v: ChemMedChem

Zika virus (ZIKV), dengue fever (DENV) and chikungunya (CHIKV) are arboviruses that are spread to humans from the bite of an infected adult female Aedes aegypti mosquito. As there are no effective vaccines or therapeutics for these diseases, the prim

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2875d4c3f84c83f069257f8ae9701128
https://pubmed.ncbi.nlm.nih.gov/32926544

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Mechanism of SmI2 Reduction of 5-Bromo-6-oxo-6-phenylhexyl Methanesulfonate Studied by Spin Trapping with 2-Methyl-2-nitrosopropane

Autor: Christopher D. Aretz, Gareth R. Eaton, Bryan J. Cowen, Joseph McPeak, Sandra S. Eaton

Publikováno v: The Journal of Organic Chemistry. 83:10688-10692

The radical formed by reduction of 5-bromo-6-oxo-6-phenylhexyl methanesulfonate, an α-bromoketone, with SmI2 was spin trapped with 2-methyl-2-nitrosopropane. Electron paramagnetic resonance spectra of the spin adduct and the adduct formed in the ana

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::72f5ac9cb5856df706c204e427e0de27
https://doi.org/10.1021/acs.joc.8b01517

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Discovery of Small Molecule Renal Outer Medullary Potassium (ROMK) Channel Inhibitors: A Brief History of Medicinal Chemistry Approaches To Develop Novel Diuretic Therapeutics

Autor: Anish K. Vadukoot, Corey R. Hopkins, Christopher D. Aretz

Publikováno v: Journal of medicinal chemistry. 62(19)

The renal outer medullary potassium (ROMK) channel is a member of the inwardly rectifying family of potassium (Kir, Kir1.1) channels. It is primarily expressed in two regions of the kidney, the cortical collecting duct (CCD) and the thick ascending l

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1313234285cbc2b0017d5d8be0d870c7
https://pubmed.ncbi.nlm.nih.gov/31034224

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