Design and SAR of selective T-type calcium channel antagonists containing a biaryl sulfonamide core

T-type calcium channel antagonists were designed using a protocol involving the program SPROUT constrained by a ComFA-based pharmacophore model. From this exercise, a novel series of potent and selective T-type channel antagonists containing a biaryl sulfonamide core were discovered. T-type calcium...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2008-01, Vol.18 (2), p.474-478
Main Authors: Hangeland, Jon J., Cheney, Daniel L., Friends, Todd J., Swartz, Stephen, Levesque, Paul C., Rich, Adam J., Sun, Lucy, Bridal, Terry R., Adam, Leonard P., Normandin, Diane E., Murugesan, Natesan, Ewing, William R.
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Calcium Channel Blockers - chemistry
Calcium Channel Blockers - pharmacology
Calcium Channels, T-Type - drug effects
Cardiovascular system
COMFA
Crystallography, X-Ray
Drug Design
In Vitro Techniques
Medical sciences
Miscellaneous
Molecular modelling
Patch-Clamp Techniques
Pharmacology. Drug treatments
SPROUT
Structure-Activity Relationship
Sulfonamide
Sulfonamides - chemistry
Sulfonamides - pharmacology
T-type calcium channel antagonists
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Summary:T-type calcium channel antagonists were designed using a protocol involving the program SPROUT constrained by a ComFA-based pharmacophore model. From this exercise, a novel series of potent and selective T-type channel antagonists containing a biaryl sulfonamide core were discovered. 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.
ISSN:0960-894X
0968-0896
1464-3405
1464-3391
DOI:10.1016/j.bmcl.2007.11.103