4-Anilino-pyrimidine, novel aldosterone synthase (CYP11B2) inhibitors bearing pyrimidine structures

[Display omitted] 2,2,2-Trifluoro-1-{4-[(4-fluorophenyl)amino]pyrimidin-5-yl}-1-[1-(methylsulfonyl)piperidin-4-yl]ethanol 1 was identified as a novel potent aldosterone synthase inhibitor. Despite large species differences, compound 1 inhibits both human and rodent CYP11B2 in a nano-molar range.

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2017-05, Vol.27 (9), p.1902-1906
Hauptverfasser:	Meguro, Masaki, Miyauchi, Satoru, Kanao, Yukiko, Naito, Satoru, Suzuki, Kanae, Inoue, Shinichi, Yamada, Keisuke, Homma, Tsuyoshi, Chiba, Kiyoshi, Nara, Futoshi, Furuzono, Shinji
Format:	Artikel
Sprache:	eng
Schlagworte:	Aldosterone Aldosterone synthase inhibitor Amino-pyrimidine Aniline Compounds - chemistry Aniline Compounds - pharmacology CYP11B1 CYP11B2 Cytochrome P-450 CYP11B2 - antagonists & inhibitors Cytochrome P-450 CYP11B2 - metabolism Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology HEK293 Cells Humans Pyrimidines - chemistry Pyrimidines - pharmacology
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	[Display omitted] 2,2,2-Trifluoro-1-{4-[(4-fluorophenyl)amino]pyrimidin-5-yl}-1-[1-(methylsulfonyl)piperidin-4-yl]ethanol 1 was identified as a novel potent aldosterone synthase inhibitor. Despite large species differences, compound 1 inhibits both human and rodent CYP11B2 in a nano-molar range.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2017.03.034