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2 results on '"Isaac E. Marx"'

1. Correction to 'Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement'

Author

Robert T. Fremeau, Robert S. Foti, Hanh Nho Nguyen, Jeff S. McDermott, Jean Wang, Christiane Bode, Bingfan Du, Joseph Ligutti, Thomas Dineen, Hua Gao, Thomas Kornecook, Jonathan Roberts, Brian E. Hall, Charles Kreiman, Liyue Huang, Matthew Weiss, Jessica Able, Min-Hwa Jasmine Lin, Paul E. Rose, Isaac E. Marx, Emily A. Peterson, Violeta Yu, Erin F. DiMauro, Bryan D. Moyer, Daniel S. La, Beth D. Youngblood, Dong Liu, Margaret Y. Chu-Moyer, Hakan Gunaydin, and Howard Bregman

Subjects
Pharmacokinetics, business.industry, In vivo, Organic Chemistry, Drug Discovery, Target engagement, Potency, Medicine, Pharmacology, business, Biochemistry
Abstract

Human genetic evidence has identified the voltage-gated sodium channel Na

Published
2017

2. Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement

Author

Min-Hwa Jasmine Lin, Paul E. Rose, Violeta Yu, Hakan Gunaydin, Robert T. Fremeau, Charles Kreiman, Daniel S. La, Joseph Ligutti, Matthew Weiss, Beth D. Youngblood, Thomas Dineen, Thomas Kornecook, Dong Liu, Bingfan Du, Brian E. Hall, Erin F. DiMauro, Jean Wang, Isaac E. Marx, Robert S. Foti, Emily A. Peterson, Jessica Able, Liyue Huang, Margaret Chu-Moyer, Jeff S. McDermott, Christiane Bode, Bryan D. Moyer, Howard Bregman, Jonathan Roberts, and Hua Gao

Subjects
biology, 010405 organic chemistry, Sodium channel, Organic Chemistry, Sulfonamide (medicine), Nav1.5, Pharmacology, 01 natural sciences, Biochemistry, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, chemistry.chemical_compound, chemistry, Pharmacokinetics, In vivo, Drug Discovery, biology.protein, Quinazoline, medicine, Potency, Dosing, medicine.drug
Abstract

Human genetic evidence has identified the voltage-gated sodium channel NaV1.7 as an attractive target for the treatment of pain. We initially identified naphthalene sulfonamide 3 as a potent and selective inhibitor of NaV1.7. Optimization to reduce biliary clearance by balancing hydrophilicity and hydrophobicity (Log D) while maintaining NaV1.7 potency led to the identification of quinazoline 16 (AM-2099). Compound 16 demonstrated a favorable pharmacokinetic profile in rat and dog and demonstrated dose-dependent reduction of histamine-induced scratching bouts in a mouse behavioral model following oral dosing.

Published
2016

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