Abstract
Replacement of the hydroxy cyclopentanone ring in PGE(2) with chemically more stable heterocyclic rings and substitution of the unsaturated alpha-alkenyl chain with a metabolically more stable phenethyl chain led to the development of potent and selective analogs of PGE(2). Compound 10f showed the highest potency and selectivity for EP(4) the receptor.
MeSH terms
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Animals
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Dinoprostone / chemical synthesis*
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Dinoprostone / pharmacology
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Drug Evaluation, Preclinical
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Female
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Humans
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Mice
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Pyrazoles / chemical synthesis*
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Pyrazoles / pharmacology
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Rats
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Receptors, Prostaglandin E / agonists*
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Receptors, Prostaglandin E / physiology
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Receptors, Prostaglandin E, EP2 Subtype
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Receptors, Prostaglandin E, EP4 Subtype
Substances
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PTGER2 protein, human
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PTGER4 protein, human
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Ptger2 protein, mouse
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Ptger4 protein, mouse
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Pyrazoles
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Receptors, Prostaglandin E
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Receptors, Prostaglandin E, EP2 Subtype
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Receptors, Prostaglandin E, EP4 Subtype
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Dinoprostone