title: Substituted biaryl pyrazoles as sodium channel blockers.
abstract: Voltage-gated sodium channels have been shown to play a critical role in neuropathic pain. A series of low molecular weight biaryl substituted pyrazole carboxamides were identified with good in-vitro potency and in-vivo efficacy. Compound 26, a Nav1.7 blocker has excellent efficacy in the Chung model of neuropathic pain.
authors: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. sriram_tyagarajan@merck.com
authors: Sriram
authors: S
authors: Tyagarajan
authors: Prasun K
authors: PK
authors: Chakravarty
authors: Bishan
authors: B
authors: Zhou
authors: Brett
authors: B
authors: Taylor
authors: Michael H
authors: MH
authors: Fisher
authors: Mathew J
authors: MJ
authors: Wyvratt
authors: Kathy
authors: K
authors: Lyons
authors: Tracy
authors: T
authors: Klatt
authors: Xiaohua
authors: X
authors: Li
authors: Sanjeev
authors: S
authors: Kumar
authors: Brande
authors: B
authors: Williams
authors: John
authors: J
authors: Felix
authors: Birgit T
authors: BT
authors: Priest
authors: Richard M
authors: RM
authors: Brochu
authors: Vivien
authors: V
authors: Warren
authors: McHardy
authors: M
authors: Smith
authors: Maria
authors: M
authors: Garcia
authors: Gregory J
authors: GJ
authors: Kaczorowski
authors: William J
authors: WJ
authors: Martin
authors: Catherine
authors: C
authors: Abbadie
authors: Erin
authors: E
authors: McGowan
authors: Nina
authors: N
authors: Jochnowitz
authors: William H
authors: WH
authors: Parsons
mesh_terms: D000818:Animals; D004285:Dogs; D000882:Haplorhini; D006801:Humans; D008862:Microsomes, Liver / Q000378:metabolism; D062556:NAV1.7 Voltage-Gated Sodium Channel; D009437:Neuralgia / Q000188:drug therapy*; D011720:Pyrazoles / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D051381:Rats; D026941:Sodium Channel Blockers / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D015222:Sodium Channels / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D062556:NAV1.7 Voltage-Gated Sodium Channel; D011720:Pyrazoles; C486866:SCN9A protein, human; D026941:Sodium Channel Blockers; D015222:Sodium Channels