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.
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2017-05, Vol.27 (9), p.1902-1906 |
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| container_end_page | 1906 |
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| container_issue | 9 |
| container_start_page | 1902 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 27 |
| creator | Meguro, Masaki Miyauchi, Satoru Kanao, Yukiko Naito, Satoru Suzuki, Kanae Inoue, Shinichi Yamada, Keisuke Homma, Tsuyoshi Chiba, Kiyoshi Nara, Futoshi Furuzono, Shinji |
| description | [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. |
| doi_str_mv | 10.1016/j.bmcl.2017.03.034 |
| format | Article |
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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.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2017.03.034</identifier><identifier>PMID: 28359792</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>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</subject><ispartof>Bioorganic & medicinal chemistry letters, 2017-05, Vol.27 (9), p.1902-1906</ispartof><rights>2017 Elsevier Ltd</rights><rights>Copyright © 2017 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c356t-142c289abb2c12c314114a5d344f2dd3412055ba137fc75aa02f90555181ef053</citedby><cites>FETCH-LOGICAL-c356t-142c289abb2c12c314114a5d344f2dd3412055ba137fc75aa02f90555181ef053</cites><orcidid>0000-0001-7272-2983</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0960894X17302718$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3536,27903,27904,65309</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/28359792$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Meguro, Masaki</creatorcontrib><creatorcontrib>Miyauchi, Satoru</creatorcontrib><creatorcontrib>Kanao, Yukiko</creatorcontrib><creatorcontrib>Naito, Satoru</creatorcontrib><creatorcontrib>Suzuki, Kanae</creatorcontrib><creatorcontrib>Inoue, Shinichi</creatorcontrib><creatorcontrib>Yamada, Keisuke</creatorcontrib><creatorcontrib>Homma, Tsuyoshi</creatorcontrib><creatorcontrib>Chiba, Kiyoshi</creatorcontrib><creatorcontrib>Nara, Futoshi</creatorcontrib><creatorcontrib>Furuzono, Shinji</creatorcontrib><title>4-Anilino-pyrimidine, novel aldosterone synthase (CYP11B2) inhibitors bearing pyrimidine structures</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>[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.</description><subject>Aldosterone</subject><subject>Aldosterone synthase inhibitor</subject><subject>Amino-pyrimidine</subject><subject>Aniline Compounds - chemistry</subject><subject>Aniline Compounds - pharmacology</subject><subject>CYP11B1</subject><subject>CYP11B2</subject><subject>Cytochrome P-450 CYP11B2 - antagonists & inhibitors</subject><subject>Cytochrome P-450 CYP11B2 - metabolism</subject><subject>Enzyme Inhibitors - chemistry</subject><subject>Enzyme Inhibitors - pharmacology</subject><subject>HEK293 Cells</subject><subject>Humans</subject><subject>Pyrimidines - chemistry</subject><subject>Pyrimidines - pharmacology</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kFtLAzEQhYMoWi9_wAfZRwW3ZnJpd8EXLd5A0AcFfQrZ7KxN2SY12RX6701p1Tdh4MBwzsfMIeQY6BAojC5mw2pu2iGjMB5SnkZskQGIkci5oHKbDGg5onlRirc9sh_jjFIQVIhdsscKLstxyQbEiPzK2dY6ny-Wwc5tbR2eZ85_YZvptvaxw-AdZnHpuqmOmJ1O3p8BrtlZZt3UVrbzIWYV6mDdR_bHyGIXetP1AeMh2Wl0G_Foowfk9fbmZXKfPz7dPUyuHnPD5ajLQTDDilJXFTPADAcBILSsuRANq5MAo1JWGvi4MWOpNWVNmTYSCsCGSn5ATtfcRfCfPcZOzW002Lbaoe-jgqLgUFAAnqxsbTXBxxiwUYt0uA5LBVStylUztSpXrcpVlKcRKXSy4ffVHOvfyE-byXC5NmD68stiUNFYdAZrG9B0qvb2P_43LZ-KmQ</recordid><startdate>20170501</startdate><enddate>20170501</enddate><creator>Meguro, Masaki</creator><creator>Miyauchi, Satoru</creator><creator>Kanao, Yukiko</creator><creator>Naito, Satoru</creator><creator>Suzuki, Kanae</creator><creator>Inoue, Shinichi</creator><creator>Yamada, Keisuke</creator><creator>Homma, Tsuyoshi</creator><creator>Chiba, Kiyoshi</creator><creator>Nara, Futoshi</creator><creator>Furuzono, Shinji</creator><general>Elsevier Ltd</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><orcidid>https://orcid.org/0000-0001-7272-2983</orcidid></search><sort><creationdate>20170501</creationdate><title>4-Anilino-pyrimidine, novel aldosterone synthase (CYP11B2) inhibitors bearing pyrimidine structures</title><author>Meguro, Masaki ; Miyauchi, Satoru ; Kanao, Yukiko ; Naito, Satoru ; Suzuki, Kanae ; Inoue, Shinichi ; Yamada, Keisuke ; Homma, Tsuyoshi ; Chiba, Kiyoshi ; Nara, Futoshi ; Furuzono, Shinji</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c356t-142c289abb2c12c314114a5d344f2dd3412055ba137fc75aa02f90555181ef053</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2017</creationdate><topic>Aldosterone</topic><topic>Aldosterone synthase inhibitor</topic><topic>Amino-pyrimidine</topic><topic>Aniline Compounds - chemistry</topic><topic>Aniline Compounds - pharmacology</topic><topic>CYP11B1</topic><topic>CYP11B2</topic><topic>Cytochrome P-450 CYP11B2 - antagonists & inhibitors</topic><topic>Cytochrome P-450 CYP11B2 - metabolism</topic><topic>Enzyme Inhibitors - chemistry</topic><topic>Enzyme Inhibitors - pharmacology</topic><topic>HEK293 Cells</topic><topic>Humans</topic><topic>Pyrimidines - chemistry</topic><topic>Pyrimidines - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Meguro, Masaki</creatorcontrib><creatorcontrib>Miyauchi, Satoru</creatorcontrib><creatorcontrib>Kanao, Yukiko</creatorcontrib><creatorcontrib>Naito, Satoru</creatorcontrib><creatorcontrib>Suzuki, Kanae</creatorcontrib><creatorcontrib>Inoue, Shinichi</creatorcontrib><creatorcontrib>Yamada, Keisuke</creatorcontrib><creatorcontrib>Homma, Tsuyoshi</creatorcontrib><creatorcontrib>Chiba, Kiyoshi</creatorcontrib><creatorcontrib>Nara, Futoshi</creatorcontrib><creatorcontrib>Furuzono, Shinji</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Meguro, Masaki</au><au>Miyauchi, Satoru</au><au>Kanao, Yukiko</au><au>Naito, Satoru</au><au>Suzuki, Kanae</au><au>Inoue, Shinichi</au><au>Yamada, Keisuke</au><au>Homma, Tsuyoshi</au><au>Chiba, Kiyoshi</au><au>Nara, Futoshi</au><au>Furuzono, Shinji</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>4-Anilino-pyrimidine, novel aldosterone synthase (CYP11B2) inhibitors bearing pyrimidine structures</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2017-05-01</date><risdate>2017</risdate><volume>27</volume><issue>9</issue><spage>1902</spage><epage>1906</epage><pages>1902-1906</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>[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.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>28359792</pmid><doi>10.1016/j.bmcl.2017.03.034</doi><tpages>5</tpages><orcidid>https://orcid.org/0000-0001-7272-2983</orcidid></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2017-05, Vol.27 (9), p.1902-1906 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | 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 |
| title | 4-Anilino-pyrimidine, novel aldosterone synthase (CYP11B2) inhibitors bearing pyrimidine structures |
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