Discovery of a new class of potent, selective, and orally active prostaglandin D2 receptor antagonists

Bioorganic & Medicinal Chemistry
Kazuhiko TorisuMasaaki Toda

Abstract

The process of discovering a series of N-(p-alkoxy)benzoyl-2-methylindole-4-acetic acid analogs is presented since these compounds represent a new class of potent, selective, and orally active prostaglandin D2 (PGD2) receptor antagonists. Most of these compounds exhibit strong PGD2 receptor binding and PGD2 receptor antagonism in cAMP formation assays. When given orally, these new antagonists dramatically suppress allergic inflammatory responses, such as the PGD2-induced or OVA-induced increase of vascular permeability. Structure-activity relationship (SAR) data are also discussed.

References

Mar 17, 2000·Science·T MatsuokaS Narumiya
Sep 3, 2004·Bioorganic & Medicinal Chemistry Letters·Kazuhiko TorisuMasaaki Toda

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Citations

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May 16, 2006·Bioorganic & Medicinal Chemistry·Atsushi NaganawaMasaaki Toda
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Nov 3, 2021·The Journal of Organic Chemistry·Chenghao YeWanbin Zhang

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