Abstract
The design and synthesis of a series of potent 1,3,4-trisubstituted-2-oxopiperazine based MC4 agonists are described. The tripeptidomimetic analogs (12a,b and 23) and the dipeptidomimetic 27 displayed single-nanomolar binding affinity and agonist potency for MC4R and excellent selectivity for MC4R relative to MC1R.
MeSH terms
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Drug Design*
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Guanidines / chemical synthesis
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Guanidines / chemistry*
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Guanidines / pharmacology*
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Molecular Structure
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Piperazines / chemical synthesis
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Piperazines / chemistry*
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Piperazines / pharmacology*
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Receptor, Melanocortin, Type 4 / agonists*
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Receptor, Melanocortin, Type 4 / metabolism
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Structure-Activity Relationship
Substances
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Guanidines
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Piperazines
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Receptor, Melanocortin, Type 4