Abstract
A novel and facile domino reaction has been developed to synthesize a variety of new derivatives from hydromorphone, amines and paraformaldehyde in good yields in a catalyst-free fashion with high atom efficiency. The products show a mixed MOR/DOR biological characteristic which makes them valuable for further study as opioid analgesics.
MeSH terms
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Analgesics, Opioid / administration & dosage
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Analgesics, Opioid / chemistry
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Analgesics, Opioid / pharmacology*
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Animals
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Dose-Response Relationship, Drug
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Humans
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Injections, Intraperitoneal
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Mice
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Mice, Inbred C57BL
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Mice, Knockout
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Morphine Derivatives / administration & dosage
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Morphine Derivatives / chemistry
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Morphine Derivatives / pharmacology*
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Receptors, Opioid, delta / antagonists & inhibitors*
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Receptors, Opioid, kappa / agonists*
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Receptors, Opioid, kappa / deficiency
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Receptors, Opioid, mu / agonists*
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Receptors, Opioid, mu / antagonists & inhibitors
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Receptors, Opioid, mu / deficiency
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Structure-Activity Relationship
Substances
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Analgesics, Opioid
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Morphine Derivatives
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Receptors, Opioid, delta
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Receptors, Opioid, kappa
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Receptors, Opioid, mu