1-Hydroxyalkyl-3-phenylthioureas as novel HDL-elevating agents
Thiourea 2 was identified as a potential HDL-elevating agent from a targeted database search. Structure–activity relationship of its analogs is described. A series of 1-hydroxyalkyl-3-phenylthiourea analogs were prepared and evaluated as HDL-and Apo A–I-elevating agents. Derivatives 5h, 7j, 7n, and...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2005-02, Vol.15 (3), p.809-812 |
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| container_end_page | 812 |
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| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 15 |
| creator | Coppola, Gary M. Damon, Robert E. Eskesen, J. Bruce France, Dennis S. Paterniti, James R. |
| description | Thiourea
2 was identified as a potential HDL-elevating agent from a targeted database search. Structure–activity relationship of its analogs is described.
A series of 1-hydroxyalkyl-3-phenylthiourea analogs were prepared and evaluated as HDL-and Apo A–I-elevating agents. Derivatives
5h,
7j,
7n, and
7o were found to be as effective or superior to gemfibrozil (
1). |
| doi_str_mv | 10.1016/j.bmcl.2004.10.094 |
| format | Article |
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2 was identified as a potential HDL-elevating agent from a targeted database search. Structure–activity relationship of its analogs is described.
A series of 1-hydroxyalkyl-3-phenylthiourea analogs were prepared and evaluated as HDL-and Apo A–I-elevating agents. Derivatives
5h,
7j,
7n, and
7o were found to be as effective or superior to gemfibrozil (
1).</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2004.10.094</identifier><identifier>PMID: 15664862</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>Animals ; Apolipoprotein A-I - blood ; Apolipoprotein A-I - drug effects ; Biological and medical sciences ; Cholesterol - administration & dosage ; Cholesterol - blood ; General and cellular metabolism. Vitamins ; Humans ; Lipids - blood ; Lipoproteins, HDL - blood ; Lipoproteins, HDL - drug effects ; Male ; Medical sciences ; Pharmacology. Drug treatments ; Phenylthiourea - analogs & derivatives ; Phenylthiourea - chemical synthesis ; Phenylthiourea - pharmacology ; Rats ; Structure-Activity Relationship ; Weight Gain - drug effects</subject><ispartof>Bioorganic & medicinal chemistry letters, 2005-02, Vol.15 (3), p.809-812</ispartof><rights>2004 Elsevier Ltd</rights><rights>2005 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c384t-c840d8b88907f76885e742829e17ccc53d27efd6c3bd7620fe3afff09ec4e4783</citedby><cites>FETCH-LOGICAL-c384t-c840d8b88907f76885e742829e17ccc53d27efd6c3bd7620fe3afff09ec4e4783</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmcl.2004.10.094$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=16478227$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/15664862$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Coppola, Gary M.</creatorcontrib><creatorcontrib>Damon, Robert E.</creatorcontrib><creatorcontrib>Eskesen, J. Bruce</creatorcontrib><creatorcontrib>France, Dennis S.</creatorcontrib><creatorcontrib>Paterniti, James R.</creatorcontrib><title>1-Hydroxyalkyl-3-phenylthioureas as novel HDL-elevating agents</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>Thiourea
2 was identified as a potential HDL-elevating agent from a targeted database search. Structure–activity relationship of its analogs is described.
A series of 1-hydroxyalkyl-3-phenylthiourea analogs were prepared and evaluated as HDL-and Apo A–I-elevating agents. Derivatives
5h,
7j,
7n, and
7o were found to be as effective or superior to gemfibrozil (
1).</description><subject>Animals</subject><subject>Apolipoprotein A-I - blood</subject><subject>Apolipoprotein A-I - drug effects</subject><subject>Biological and medical sciences</subject><subject>Cholesterol - administration & dosage</subject><subject>Cholesterol - blood</subject><subject>General and cellular metabolism. Vitamins</subject><subject>Humans</subject><subject>Lipids - blood</subject><subject>Lipoproteins, HDL - blood</subject><subject>Lipoproteins, HDL - drug effects</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Phenylthiourea - analogs & derivatives</subject><subject>Phenylthiourea - chemical synthesis</subject><subject>Phenylthiourea - pharmacology</subject><subject>Rats</subject><subject>Structure-Activity Relationship</subject><subject>Weight Gain - drug effects</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2005</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1LAzEQhoMoWqt_wIP0orfUJJsmWRBB6keFghcFbyHNTtrUdLcm2-L-e3dpoTdhYGB4ZublQeiKkiElVNwth7OVDUNGCG8HQ5LzI9SjXHCccTI6Rj2SC4JVzr_O0HlKS0IoJ5yfojM6EoIrwXrogeJJU8TqtzHhuwk4w-sFlE2oF77aRDBp0FZZbSEMJk9TDAG2pvblfGDmUNbpAp04ExJc7nsffb48f4wnePr--jZ-nGKbKV5jqzgp1EypnEgnhVIjkJwplgOV1tpRVjAJrhA2mxVSMOIgM845koPlwKXK-uh2d3cdq58NpFqvfLIQgimh2iQtZCa5oLIF2Q60sUopgtPr6FcmNpoS3VnTS91Z0521btZaa5eu99c3sxUUh5W9pha42QMmWRNcNKX16cCJNiNj3ff7HQeti62HqJP1UFoofARb66Ly_-X4A7xEioM</recordid><startdate>20050201</startdate><enddate>20050201</enddate><creator>Coppola, Gary M.</creator><creator>Damon, Robert E.</creator><creator>Eskesen, J. Bruce</creator><creator>France, Dennis S.</creator><creator>Paterniti, James R.</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>IQODW</scope><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></search><sort><creationdate>20050201</creationdate><title>1-Hydroxyalkyl-3-phenylthioureas as novel HDL-elevating agents</title><author>Coppola, Gary M. ; Damon, Robert E. ; Eskesen, J. Bruce ; France, Dennis S. ; Paterniti, James R.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c384t-c840d8b88907f76885e742829e17ccc53d27efd6c3bd7620fe3afff09ec4e4783</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2005</creationdate><topic>Animals</topic><topic>Apolipoprotein A-I - blood</topic><topic>Apolipoprotein A-I - drug effects</topic><topic>Biological and medical sciences</topic><topic>Cholesterol - administration & dosage</topic><topic>Cholesterol - blood</topic><topic>General and cellular metabolism. Vitamins</topic><topic>Humans</topic><topic>Lipids - blood</topic><topic>Lipoproteins, HDL - blood</topic><topic>Lipoproteins, HDL - drug effects</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><topic>Phenylthiourea - analogs & derivatives</topic><topic>Phenylthiourea - chemical synthesis</topic><topic>Phenylthiourea - pharmacology</topic><topic>Rats</topic><topic>Structure-Activity Relationship</topic><topic>Weight Gain - drug effects</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Coppola, Gary M.</creatorcontrib><creatorcontrib>Damon, Robert E.</creatorcontrib><creatorcontrib>Eskesen, J. Bruce</creatorcontrib><creatorcontrib>France, Dennis S.</creatorcontrib><creatorcontrib>Paterniti, James R.</creatorcontrib><collection>Pascal-Francis</collection><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>Coppola, Gary M.</au><au>Damon, Robert E.</au><au>Eskesen, J. Bruce</au><au>France, Dennis S.</au><au>Paterniti, James R.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>1-Hydroxyalkyl-3-phenylthioureas as novel HDL-elevating agents</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2005-02-01</date><risdate>2005</risdate><volume>15</volume><issue>3</issue><spage>809</spage><epage>812</epage><pages>809-812</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>Thiourea
2 was identified as a potential HDL-elevating agent from a targeted database search. Structure–activity relationship of its analogs is described.
A series of 1-hydroxyalkyl-3-phenylthiourea analogs were prepared and evaluated as HDL-and Apo A–I-elevating agents. Derivatives
5h,
7j,
7n, and
7o were found to be as effective or superior to gemfibrozil (
1).</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>15664862</pmid><doi>10.1016/j.bmcl.2004.10.094</doi><tpages>4</tpages></addata></record> |
| fulltext | fulltext |
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| ispartof | Bioorganic & medicinal chemistry letters, 2005-02, Vol.15 (3), p.809-812 |
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| language | eng |
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| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | Animals Apolipoprotein A-I - blood Apolipoprotein A-I - drug effects Biological and medical sciences Cholesterol - administration & dosage Cholesterol - blood General and cellular metabolism. Vitamins Humans Lipids - blood Lipoproteins, HDL - blood Lipoproteins, HDL - drug effects Male Medical sciences Pharmacology. Drug treatments Phenylthiourea - analogs & derivatives Phenylthiourea - chemical synthesis Phenylthiourea - pharmacology Rats Structure-Activity Relationship Weight Gain - drug effects |
| title | 1-Hydroxyalkyl-3-phenylthioureas as novel HDL-elevating agents |
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