title: 2,4(5)-Diarylimidazoles: synthesis and biological evaluation of a new class of sodium channel blockers against hNa(v)1.2.
abstract: A small family of novel 2,4(5)-diarylimidazoles were prepared through a simple and efficient synthesis and evaluated as potential inhibitors of hNa(v)1.2 sodium channel currents. One member of this series (4) exhibited profound inhibition of Na(v)1.2 currents, emerging as a promising lead compound for further structure-activity relationship studies for the development of novel sodium channel blockers.
authors.affiliation: Dipartimento Farmaceutico, Università degli Studi di Parma, V.le G.P. Usberti, 27/A, I-43100 Parma, Italy.
authors.forename: Mirko
authors.initials: M
authors.lastname: Rivara
authors.forename: Aparna R
authors.initials: AR
authors.lastname: Baheti
authors.forename: Marco
authors.initials: M
authors.lastname: Fantini
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Cocconcelli
authors.forename: Chiara
authors.initials: C
authors.lastname: Ghiron
authors.forename: Christopher L
authors.initials: CL
authors.lastname: Kalmar
authors.forename: Natasha
authors.initials: N
authors.lastname: Singh
authors.forename: Ellen C
authors.initials: EC
authors.lastname: Merrick
authors.forename: Manoj K
authors.initials: MK
authors.lastname: Patel
authors.forename: Valentina
authors.initials: V
authors.lastname: Zuliani
mesh_terms: D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D015640:Ion Channel Gating; D008956:Models, Chemical; D015394:Molecular Structure; D062551:NAV1.2 Voltage-Gated Sodium Channel; D009419:Nerve Tissue Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D020033:Protein Isoforms; D012964:Sodium / Q000737:chemistry; D026941:Sodium Channel Blockers / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015222:Sodium Channels / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D007093:Imidazoles; D062551:NAV1.2 Voltage-Gated Sodium Channel; D009419:Nerve Tissue Proteins; D020033:Protein Isoforms; C568251:SCN2A protein, human; D026941:Sodium Channel Blockers; D015222:Sodium Channels; D012964:Sodium