Development of prostaglandin D2 receptor antagonist: discovery of highly potent antagonists
Copyright policy )Development of prostaglandin D2 receptor antagonist: discovery of highly potent antagonists
The process of discovery for highly potent prostaglandin D(2) (PGD(2)) receptor antagonists is reported. A series of N-(p-alkoxy)benzoyl-2-methylindole-4-acetic acids were synthesized and identified as a new class of selective PGD(2) receptor antagonists. Most of them exhibited strong PGD(2) receptor antagonism in binding studies and the cAMP formation assay. The structure-activity relationships (SAR), including subtype selectivity of the synthesized compounds, are also discussed.
Structure-Activity Relationship, Binding Sites, Indoleacetic Acids, Drug Design, Anti-Allergic Agents, Receptors, Prostaglandin, Cyclic AMP, Receptors, Immunologic
Structure-Activity Relationship, Binding Sites, Indoleacetic Acids, Drug Design, Anti-Allergic Agents, Receptors, Prostaglandin, Cyclic AMP, Receptors, Immunologic
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