Discovery of carbon-11 labeled sulfonamide derivative: A PET tracer for imaging brain NLRP3 inflammasome

[Display omitted] We report herein the discovery of a positron emission tomography (PET) tracer for the (NOD)-like receptor protein 3 (NLRP3). Our recent medicinal chemistry campaign on developing sulfonamide-based NLRP3 inhibitors led to an analog, 1, with a methoxy substituent amenable to labeling...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2021-02, Vol.34, p.127777-127777, Article 127777
Hauptverfasser:	Xu, Yulong, Xu, Yiming, Blevins, Hallie, Lan, Yu, Liu, Yan, Yuan, Gengyang, Striar, Robin, Zagaroli, Julia S., Tocci, Darcy R., Langan, Amelia G., Zhang, Can, Zhang, Shijun, Wang, Changning
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Blockable uptake Blood-brain barrier (BBB) penetration Blood-Brain Barrier - metabolism Carbon Radioisotopes Chemistry Chemistry, Medicinal Chemistry, Organic Drug Discovery Inflammasomes - analysis Inflammasomes - metabolism Life Sciences & Biomedicine Mice Mice, Inbred C57BL Molecular Structure NLR Family, Pyrin Domain-Containing 3 Protein - analysis NLR Family, Pyrin Domain-Containing 3 Protein - metabolism NLRP3 Pharmacology & Pharmacy Physical Sciences Positron emission tomography (PET) Positron Emission Tomography Computed Tomography Radiopharmaceuticals - chemical synthesis Radiopharmaceuticals - chemistry Radiopharmaceuticals - metabolism Science & Technology Sulfonamide derivative Sulfonamides - chemical synthesis Sulfonamides - chemistry Sulfonamides - metabolism
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