2,4(5)-Diarylimidazoles: synthesis and biological evaluation of a new class of sodium channel blockers against hNa(v)1.2.
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.
Rivara
Mirko
M
Dipartimento Farmaceutico, Università degli Studi di Parma, V.le G.P. Usberti, 27/A, I-43100 Parma, Italy.
Baheti
Aparna R
AR
Fantini
Marco
M
Cocconcelli
Giuseppe
G
Ghiron
Chiara
C
Kalmar
Christopher L
CL
Singh
Natasha
N
Merrick
Ellen C
EC
Patel
Manoj K
MK
Zuliani
Valentina
V
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
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