title: Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping.
abstract: We describe the medicinal chemistry approach that generated a novel indole series of EP(1) receptor antagonists. The SAR of this new template was evaluated and culminated in the identification of compound 12g which demonstrated in vivo efficacy in a preclinical model of inflammatory pain.
authors: Neurology Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom. adrian.2.hall@gsk.com
authors: Adrian
authors: A
authors: Hall
authors: Andy
authors: A
authors: Billinton
authors: Susan H
authors: SH
authors: Brown
authors: Anita
authors: A
authors: Chowdhury
authors: Gerard M P
authors: GM
authors: Giblin
authors: Paul
authors: P
authors: Goldsmith
authors: David N
authors: DN
authors: Hurst
authors: Alan
authors: A
authors: Naylor
authors: Sadhana
authors: S
authors: Patel
authors: Tiziana
authors: T
authors: Scoccitti
authors: Pamela J
authors: PJ
authors: Theobald
mesh_terms: D000818:Animals; D006801:Humans; D006860:Hydrogen Bonding; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008862:Microsomes, Liver / Q000187:drug effects / Q000378:metabolism; D008958:Models, Molecular; D015394:Molecular Structure; D051381:Rats; D018078:Receptors, Prostaglandin E / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D058306:Receptors, Prostaglandin E, EP1 Subtype; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry
chemical_list: D007211:Indoles; C545635:PTGER1 protein, human; D018078:Receptors, Prostaglandin E; D058306:Receptors, Prostaglandin E, EP1 Subtype; D013844:Thiazoles; C030374:indole