Abstract
A strategy of systematically targeting more rigid analogues of the known MCH R1 receptor antagonist, SB-568849, serendipitously uncovered a binding mode accessible to N-aryl-phthalimide ligands. Optimisation to improve the stability of this compound class led to the discovery of novel N-aryl-quinazolinones, benzotriazinones and thienopyrimidinones as selective ligands with good affinity for human melanin-concentrating hormone receptor 1.
MeSH terms
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Amides / chemical synthesis
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Amides / chemistry
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Amides / pharmacology*
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Anilides / chemistry
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Biphenyl Compounds / chemical synthesis
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Biphenyl Compounds / chemistry
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Biphenyl Compounds / pharmacology*
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Humans
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Molecular Structure
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Receptors, Somatostatin / antagonists & inhibitors*
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Receptors, Somatostatin / metabolism
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Structure-Activity Relationship
Substances
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Amides
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Anilides
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Biphenyl Compounds
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MCHR1 protein, human
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Receptors, Somatostatin
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SB-568849