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Your search keyword '"David D. Fischer"' showing total 3 results
Start Over Author "David D. Fischer" Journal bioorganic medicinal chemistry letters
3 results on '"David D. Fischer"'

1. Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist.

Author

Xiao Y, Araldi GL, Zhao Z, Reddy A, Karra S, Brugger N, Fischer D, Palmer E, Bao B, and McKenna SD

Subjects
Animals, Female, Guinea Pigs, Humans, Lactams pharmacokinetics, Male, Mice, Ovulation Induction, Receptors, Prostaglandin E, EP2 Subtype, Receptors, Prostaglandin E, EP4 Subtype, Structure-Activity Relationship, Lactams chemical synthesis, Lactams pharmacology, Receptors, Prostaglandin E agonists
Abstract

Gamma-lactam analogs (2) of EP(4) receptor agonists were identified by substitution of the pyrazolidinone ring (1) with a pyrrolidinone ring. Several compounds (such as 2a, 2h) with high potency, selectivity and acceptable PK profiles were discovered. These were assessed in animal models of ovulation induction and bronchoconstriction.

Published
2008
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2. Synthesis and evaluation of novel pyrazolidinone analogs of PGE2 as EP2 and EP4 receptors agonists.

Author

Zhao Z, Araldi GL, Xiao Y, Reddy AP, Liao Y, Karra S, Brugger N, Fischer D, and Palmer E

Subjects
Animals, Dinoprostone pharmacology, Drug Evaluation, Preclinical, Female, Humans, Mice, Pyrazoles pharmacology, Rats, Receptors, Prostaglandin E physiology, Receptors, Prostaglandin E, EP2 Subtype, Receptors, Prostaglandin E, EP4 Subtype, Dinoprostone chemical synthesis, Pyrazoles chemical synthesis, Receptors, Prostaglandin E agonists
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.

Published
2007
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3. Discovery of novel prostaglandin analogs of PGE2 as potent and selective EP2 and EP4 receptor agonists.

Author

Xiao Y, Araldi GL, Zhao Z, Brugger N, Karra S, Fischer D, and Palmer E

Subjects
Animals, Cell Line, Dinoprostone pharmacokinetics, Dinoprostone pharmacology, Half-Life, Humans, Rats, Receptors, Prostaglandin E, EP2 Subtype, Receptors, Prostaglandin E, EP4 Subtype, Dinoprostone analogs & derivatives, Receptors, Prostaglandin E agonists
Abstract

Analogs of PGE(2) with introduction of diene groups at the omega-side chain have been synthesized and evaluated for their binding affinity for EP(2) and EP(4) receptors. An optimized analog (compound 9b) showed high potency and selectivity for the EP(4) receptor over other known receptors.

Published
2007
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