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Bioorg Med Chem Lett ; 18(2): 474-8, 2008 Jan 15.
Article in English | MEDLINE | ID: mdl-18160281

ABSTRACT

T-type calcium channel antagonists were designed using a protocol involving the program SPROUT and constrained by a ComFA-based pharmacophore model. Scaffolds generated by SPROUT were evaluated based on their ability to be translated into structures that were synthetically tractable. From this exercise, a novel series of potent and selective T-type channel antagonists containing a biaryl sulfonamide core were discovered.


Subject(s)
Calcium Channel Blockers/chemistry , Calcium Channel Blockers/pharmacology , Calcium Channels, T-Type/drug effects , Sulfonamides/chemistry , Sulfonamides/pharmacology , Animals , Crystallography, X-Ray , Drug Design , In Vitro Techniques , Patch-Clamp Techniques , Structure-Activity Relationship
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