Author/Authors :
Jon J. Hangeland، نويسنده , , Daniel L. Cheney، نويسنده , , Todd J. Friends، نويسنده , , Stephen Swartz، نويسنده , , Paul C. Levesque، نويسنده , , Adam J. Rich، نويسنده , , Lucy Sun، نويسنده , , Terry R. Bridal، نويسنده , , Leonard P. Adam، نويسنده , , Diane E. Normandin، نويسنده , , Natesan Murugesan، نويسنده , , William R. Ewing، نويسنده ,
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.
Keywords :
T-type calcium channel antagonists , Molecular modelling , Sulfonamide , CoMFA , sprout
