Piperidine derivatives as nonprostanoid IP receptor agonists

Ryoji Hayashi; Hideki Sakagami; Masakazu Koiwa; Hiroaki Ito; Mitsuko Miyamoto; Masafumi Isogaya

doi:10.1016/j.bmcl.2016.03.009

Piperidine derivatives as nonprostanoid IP receptor agonists

Bioorg Med Chem Lett. 2016 May 1;26(9):2360-4. doi: 10.1016/j.bmcl.2016.03.009. Epub 2016 Mar 4.

Authors

Ryoji Hayashi¹, Hideki Sakagami², Masakazu Koiwa², Hiroaki Ito², Mitsuko Miyamoto², Masafumi Isogaya²

Affiliations

¹ Pharmaceutical Research Laboratories, Toray Industries, Inc., 6-10-1 Tebiro, Kamakura, Kanagawa 248-8555, Japan. Electronic address: Ryoji_Hayashi2@nts.toray.co.jp.
² Pharmaceutical Research Laboratories, Toray Industries, Inc., 6-10-1 Tebiro, Kamakura, Kanagawa 248-8555, Japan.

PMID: 26996371
DOI: 10.1016/j.bmcl.2016.03.009

Abstract

The discovery of a new class of nonprostanoid prostaglandin I2 receptor (IP receptor) agonists is reported. Among them, the unique piperidine derivative 31b (2-((1-(2-(N-(4-tolyl)benzamido)ethyl)piperidin-4-yl)oxy)acetic acid) was a good IP receptor agonist and was 50-fold more selective for the human IP receptor than for other human prostanoid receptors. This compound showed good pharmacokinetic properties in dog.

Keywords: Agonist; Benzanilide; IP; Nonprostanoid; Piperidine; Prostacyclin.

MeSH terms

Animals
Dogs
Humans
Piperidines / pharmacology*
Receptors, Epoprostenol / agonists*

Substances

Piperidines
Receptors, Epoprostenol