title: Expedited SAR study of high-affinity ligands to the alpha(2)delta subunit of voltage-gated calcium channels: Generation of a focused library using a solution-phase Sn2Ar coupling methodology.
abstract: The SAR of the lead compound 3, a novel ligand for the alpha(2)delta subunit of voltage-gated calcium channels, was rapidly explored. Utilizing a parallel solution-phase Sn2Ar coupling approach, a focused library was obtained. The library was evaluated in vitro and afforded a series of analogues with improved potencies. The SAR trends of the library are also described.
authors.affiliation: Department of Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA. cchen9@san.rr.com
authors.forename: Chixu
authors.initials: C
authors.lastname: Chen
authors.forename: Brian
authors.initials: B
authors.lastname: Stearns
authors.forename: Tao
authors.initials: T
authors.lastname: Hu
authors.forename: Naomi
authors.initials: N
authors.lastname: Anker
authors.forename: Angelina
authors.initials: A
authors.lastname: Santini
authors.forename: Jeannie M
authors.initials: JM
authors.lastname: Arruda
authors.forename: Brian T
authors.initials: BT
authors.lastname: Campbell
authors.forename: Purabi
authors.initials: P
authors.lastname: Datta
authors.forename: Jayashree
authors.initials: J
authors.lastname: Aiyar
authors.forename: Benitio
authors.initials: B
authors.lastname: Munoz
mesh_terms: D015220:Calcium Channels / Q000737:chemistry / Q000187:drug effects / Q000378:metabolism*; D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D006801:Humans; D015640:Ion Channel Gating; D008024:Ligands; D021122:Protein Subunits / Q000737:chemistry / Q000378:metabolism*; D012996:Solutions / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D015220:Calcium Channels; D008024:Ligands; D021122:Protein Subunits; D012996:Solutions; C494035:voltage gated calcium channel subunit Ca alpha2delta-1, human