Abstract
Solid-phase synthesis of a 300-member pharmacophore library of 1,4-dihydropyridines from keto ester, diketone and aldehyde building blocks on a cleavable amine polymeric support is described. Screening and serial deconvolution of the combinatorial library has resulted in identification of known and new potent calcium channel blockers.
MeSH terms
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Animals
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Binding, Competitive
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Calcium Channel Blockers / chemical synthesis
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Calcium Channel Blockers / chemistry*
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Calcium Channel Blockers / metabolism
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Calcium Channels / metabolism
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Cerebral Cortex / metabolism
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Dihydropyridines / chemical synthesis
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Dihydropyridines / chemistry*
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Dihydropyridines / metabolism
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Drug Evaluation, Preclinical
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In Vitro Techniques
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Nitrendipine / metabolism
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Radioligand Assay
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Rats
Substances
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Calcium Channel Blockers
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Calcium Channels
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Dihydropyridines
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1,4-dihydropyridine
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Nitrendipine