ACS Medicinal Chemistry Letters p. 1062 - 1067 (2016)
Update date:2022-08-05
Topics:
Marx, Isaac E.
Dineen, Thomas A.
Able, Jessica
Bode, Christiane
Bregman, Howard
Chu-Moyer, Margaret
Dimauro, Erin F.
Du, Bingfan
Foti, Robert S.
Fremeau, Robert T.
Gao, Hua
Gunaydin, Hakan
Hall, Brian E.
Huang, Liyue
Kornecook, Thomas
Kreiman, Charles R.
La, Daniel S.
Ligutti, Joseph
Lin, Min-Hwa Jasmine
Liu, Dong
McDermott, Jeff S.
Moyer, Bryan D.
Peterson, Emily A.
Roberts, Jonathan T.
Rose, Paul
Wang, Jean
Youngblood, Beth D.
Yu, Violeta
Weiss, Matthew M.
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.
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