Virtual Screening to Identify Calcium Channel Blockers SEEKING IMPROVED SAFETY FROM MEDICINAL CHEMISTRY SCAFFOLDS
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Modular, efficient synthesis of asymmetrically substituted piperazine scaffolds as potent calcium channel blockers.
A novel approach to the synthesis of substituted piperazines and their investigation as N-type calcium channel blockers is presented. A common scaffold exhibiting high activity as N-type blockers is N-substituted piperazine. Using recently developed titanium and zirconium catalysts, we describe the efficient and modular synthesis of 2,5-asymmetrically disubstituted piperazines from simple amine...
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