Abstract
Cyclohexylamino oxazoline 1 (AGN 190837), an analogue of 2 (Bay a6781), is a potent alpha(2) adrenoceptor agonist. On the basis of a design generated by receptor-ligand modeling, a number of cyclohexyl and norbornyl analogues were synthesized wherein the propyl group of 1 was replaced by phenylalkyl subsituents. This resulted in compound 6 being an alpha(2c) selective agonist, as well as 7 and 9 being alpha(2a)/alpha(2c) selective.
MeSH terms
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Adrenergic alpha-2 Receptor Agonists*
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Adrenergic alpha-Agonists / chemical synthesis*
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Adrenergic alpha-Agonists / pharmacology
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Antihypertensive Agents / chemical synthesis
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Antihypertensive Agents / chemistry
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Antihypertensive Agents / pharmacology
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Cloning, Molecular
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Humans
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Indicators and Reagents
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Models, Molecular
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Monte Carlo Method
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Oxazoles / chemical synthesis*
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Oxazoles / chemistry
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Oxazoles / pharmacology
Substances
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Adrenergic alpha-2 Receptor Agonists
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Adrenergic alpha-Agonists
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Antihypertensive Agents
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Indicators and Reagents
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Oxazoles
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cyclohexylamino oxazoline
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BAY-a 6781