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

Autor:	Satoru Naito, Kiyoshi Chiba, Satoru Miyauchi, Shin-ichi Inoue, Keisuke Yamada, Futoshi Nara, Shinji Furuzono, Masaki Meguro, Tsuyoshi Homma, Yukiko Kanao, Kanae Suzuki
Rok vydání:	2017
Předmět:	0301 basic medicine Aldosterone synthase Pyrimidine Stereochemistry Clinical Biochemistry Pharmaceutical Science 030204 cardiovascular system & hematology Biochemistry 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Drug Discovery Cytochrome P-450 CYP11B2 Humans Steroid 11-beta-hydroxylase Enzyme Inhibitors Molecular Biology Ethanol Aldosterone Aniline Compounds biology Organic Chemistry HEK 293 cells 030104 developmental biology HEK293 Cells Pyrimidines chemistry biology.protein Molecular Medicine
Zdroj:	Bioorganicmedicinal chemistry letters. 27(9)
ISSN:	1464-3405
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a631fa9cd4b4a16db8a9097cc54aeefc https://pubmed.ncbi.nlm.nih.gov/28359792 Zobrazit plný text záznamu Full Text from ScienceDirect