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Discovery of pyrrolo-benzo-1,4-diazines as potent Na(v)1.7 sodium channel blockers.
Ho, Ginny D; Tulshian, Deen; Bercovici, Ana; Tan, Zheng; Hanisak, Jennifer; Brumfield, Stephanie; Matasi, Julius; Heap, Charles R; Earley, William G; Courneya, Brandy; Herr, R Jason; Zhou, Xiaoping; Bridal, Terry; Rindgen, Diane; Sorota, Steve; Yang, Shu-Wei.
Affiliation
  • Ho GD; Discovery Chemistry, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Tulshian D; Discovery Chemistry, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Bercovici A; Discovery Chemistry, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Tan Z; Discovery Chemistry, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Hanisak J; Discovery Chemistry, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Brumfield S; Discovery Chemistry, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Matasi J; Discovery Chemistry, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Heap CR; Department of Medicinal Chemistry, AMRI Global, Albany, NY 12203, United States.
  • Earley WG; Department of Medicinal Chemistry, AMRI Global, Albany, NY 12203, United States.
  • Courneya B; Department of Medicinal Chemistry, AMRI Global, Albany, NY 12203, United States.
  • Herr RJ; Department of Medicinal Chemistry, AMRI Global, Albany, NY 12203, United States.
  • Zhou X; In Vivo Pharmacology Group, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Bridal T; Cardiorenal Group, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Rindgen D; Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Sorota S; Cardiorenal Group, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Yang SW; Discovery Chemistry, Merck Research Laboratory, Kenilworth, NJ 07033, United States. Electronic address: shu-wei.yang@merck.com.
Bioorg Med Chem Lett ; 24(17): 4110-3, 2014 Sep 01.
Article in En | MEDLINE | ID: mdl-25113934
A series of pyrrolo-benzo-1,4-diazine analogs have been synthesized and displayed potent Nav1.7 inhibitory activity and moderate selectivity over Nav1.5. The syntheses, structure-activity relationships, and selected pharmacokinetic data of these analogs are described. Compound 41 displayed anti-nociceptive efficacy in the rat CFA pain model at 100 mpk oral dosing.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Quinoxalines / Spiro Compounds / Sodium Channel Blockers / Drug Discovery / NAV1.7 Voltage-Gated Sodium Channel Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2014 Document type: Article Affiliation country: United States Country of publication: United kingdom
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Quinoxalines / Spiro Compounds / Sodium Channel Blockers / Drug Discovery / NAV1.7 Voltage-Gated Sodium Channel Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2014 Document type: Article Affiliation country: United States Country of publication: United kingdom