In vitro intrinsic clearance-based optimization of N3- phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists

DOI: 10.1021/jm900302q

Source and publish data:

Journal of Medicinal Chemistry p. 4161 - 4172 (2009)

Update date:2022-07-30

Topics: In vitro Antagonists

Authors:

Hartz, Richard A.

Ahuja, Vijay T.

Rafalski, Maria

Schmitz, William D.

Brenner, Allison B.

Denhart, Derek J.

Ditta, Jonathan L.

Deskus, Jeffrey A.

Yue, Eddy W.

Arvanitis, Argyrios G.

Lelas, Snjezana

Li, Yu-Wen

Molski, Thaddeus F.

Wong, Harvey

Grace, James E.

Lentz, Kimberley A.

Li, Jianqing

Lodge, Nicholas J.

Zaczek, Robert

Combs, Andrew P.

Olson, Richard E.

Mattson, Ronald J.

Bronson, Joanne J.

Macor, John E.

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Article abstract of DOI:10.1021/jm900302q

A series of pyrazinone-based heterocycles was identified as potent and orally active corticotropinreleasing factor-1 (CRF₁) receptor antagonists. Selected compounds proved efficacious in an anxiety model in rats; however, pharmacokinetic proper

Full text of DOI:10.1021/jm900302q

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