gem-Diphosphonate and gem-phosphonate-phosphate compounds with specific high density lipoprotein inducing activity
New diphosphonate compounds and related derivatives were synthesized and investigated for their activity in specifically inducing plasma high density lipoproteins (HDL) and high density lipoprotein cholesterol (HDL-C) in normal rats. The screening of numerous compounds has permitted the determinatio...
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| Veröffentlicht in: | Journal of medicinal chemistry 1987-08, Vol.30 (8), p.1426-1433 |
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| container_end_page | 1433 |
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| container_issue | 8 |
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| container_title | Journal of medicinal chemistry |
| container_volume | 30 |
| creator | Nguyen Lan Mong Niesor, Eric Bentzen, Craig L |
| description | New diphosphonate compounds and related derivatives were synthesized and investigated for their activity in specifically inducing plasma high density lipoproteins (HDL) and high density lipoprotein cholesterol (HDL-C) in normal rats. The screening of numerous compounds has permitted the determination of the structural variations leading to optimal plasma lipid altering activity, indicating antiatherosclerotic potential. Among the compounds observed to be the most active, dimethyl alpha-(dimethoxyphosphinyl)-p-chlorobenzyl phosphate (20, SR-202, mifobate) was selected for further pharmacological and subsequent clinical development. |
| doi_str_mv | 10.1021/jm00391a027 |
| format | Article |
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The screening of numerous compounds has permitted the determination of the structural variations leading to optimal plasma lipid altering activity, indicating antiatherosclerotic potential. Among the compounds observed to be the most active, dimethyl alpha-(dimethoxyphosphinyl)-p-chlorobenzyl phosphate (20, SR-202, mifobate) was selected for further pharmacological and subsequent clinical development.</description><identifier>ISSN: 0022-2623</identifier><identifier>EISSN: 1520-4804</identifier><identifier>DOI: 10.1021/jm00391a027</identifier><identifier>PMID: 3612689</identifier><identifier>CODEN: JMCMAR</identifier><language>eng</language><publisher>Washington, DC: American Chemical Society</publisher><subject>Animals ; Chemical Phenomena ; Chemistry ; Cholesterol, HDL - blood ; Diphosphonates - chemical synthesis ; Diphosphonates - pharmacology ; Exact sciences and technology ; Lipoproteins, HDL - blood ; Male ; Organic chemistry ; Organometalloidal and organometallic compounds ; P derivatives ; Phosphates - chemical synthesis ; Phosphates - pharmacology ; Preparations and properties ; Rats ; Rats, Inbred Strains ; Structure-Activity Relationship</subject><ispartof>Journal of medicinal chemistry, 1987-08, Vol.30 (8), p.1426-1433</ispartof><rights>1987 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-a383t-449f240d72b83b71acffc147c1a300469d7e8fe44fbe413ffd3559308eb893db3</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://pubs.acs.org/doi/pdf/10.1021/jm00391a027$$EPDF$$P50$$Gacs$$H</linktopdf><linktohtml>$$Uhttps://pubs.acs.org/doi/10.1021/jm00391a027$$EHTML$$P50$$Gacs$$H</linktohtml><link.rule.ids>314,776,780,2752,27053,27901,27902,56713,56763</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=8276517$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/3612689$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Nguyen Lan Mong</creatorcontrib><creatorcontrib>Niesor, Eric</creatorcontrib><creatorcontrib>Bentzen, Craig L</creatorcontrib><title>gem-Diphosphonate and gem-phosphonate-phosphate compounds with specific high density lipoprotein inducing activity</title><title>Journal of medicinal chemistry</title><addtitle>J. Med. Chem</addtitle><description>New diphosphonate compounds and related derivatives were synthesized and investigated for their activity in specifically inducing plasma high density lipoproteins (HDL) and high density lipoprotein cholesterol (HDL-C) in normal rats. The screening of numerous compounds has permitted the determination of the structural variations leading to optimal plasma lipid altering activity, indicating antiatherosclerotic potential. Among the compounds observed to be the most active, dimethyl alpha-(dimethoxyphosphinyl)-p-chlorobenzyl phosphate (20, SR-202, mifobate) was selected for further pharmacological and subsequent clinical development.</description><subject>Animals</subject><subject>Chemical Phenomena</subject><subject>Chemistry</subject><subject>Cholesterol, HDL - blood</subject><subject>Diphosphonates - chemical synthesis</subject><subject>Diphosphonates - pharmacology</subject><subject>Exact sciences and technology</subject><subject>Lipoproteins, HDL - blood</subject><subject>Male</subject><subject>Organic chemistry</subject><subject>Organometalloidal and organometallic compounds</subject><subject>P derivatives</subject><subject>Phosphates - chemical synthesis</subject><subject>Phosphates - pharmacology</subject><subject>Preparations and properties</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Structure-Activity Relationship</subject><issn>0022-2623</issn><issn>1520-4804</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1987</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNptkE1v1DAURS1EVaaFFWskLxBdoBTbz4mTJSoUqEalEmVtOf6Y8ZA4wU6A_vt6NNGoCxbWs945unq6CL2m5JISRj_sekKgoYow8QytaMlIwWvCn6MVIYwVrGLwAp2ltCPZowxO0SlUlFV1s0JxY_vikx-3Q8ovqMliFQzeb5_slv-e6qEfhzmYhP_6aYvTaLV3XuOt32yxsSH56QF3fhzGOEzWB-yDmbUPG6z05P9k-hKdONUl-2qZ5-jn9ef7q6_F-vuXb1cf14WCGqaC88YxToxgbQ2toEo7pykXmioghFeNEbZ2lnPXWk7BOQNl2QCpbVs3YFo4R-8OufmS37NNk-x90rbrVLDDnKQQFTAAnsX3B1HHIaVonRyj71V8kJTIfcPyScPZfrPEzm1vzdFdKs387cJV0qpzUQXt01GrmahKuo8pDppPk_13xCr-kpUAUcr7ux_yRlxXze3dWt5m_-LgK53kbphjyN3998BHxcWhSA</recordid><startdate>19870801</startdate><enddate>19870801</enddate><creator>Nguyen Lan Mong</creator><creator>Niesor, Eric</creator><creator>Bentzen, Craig L</creator><general>American Chemical Society</general><scope>BSCLL</scope><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>19870801</creationdate><title>gem-Diphosphonate and gem-phosphonate-phosphate compounds with specific high density lipoprotein inducing activity</title><author>Nguyen Lan Mong ; Niesor, Eric ; Bentzen, Craig L</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-a383t-449f240d72b83b71acffc147c1a300469d7e8fe44fbe413ffd3559308eb893db3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1987</creationdate><topic>Animals</topic><topic>Chemical Phenomena</topic><topic>Chemistry</topic><topic>Cholesterol, HDL - blood</topic><topic>Diphosphonates - chemical synthesis</topic><topic>Diphosphonates - pharmacology</topic><topic>Exact sciences and technology</topic><topic>Lipoproteins, HDL - blood</topic><topic>Male</topic><topic>Organic chemistry</topic><topic>Organometalloidal and organometallic compounds</topic><topic>P derivatives</topic><topic>Phosphates - chemical synthesis</topic><topic>Phosphates - pharmacology</topic><topic>Preparations and properties</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Nguyen Lan Mong</creatorcontrib><creatorcontrib>Niesor, Eric</creatorcontrib><creatorcontrib>Bentzen, Craig L</creatorcontrib><collection>Istex</collection><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>Journal of medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Nguyen Lan Mong</au><au>Niesor, Eric</au><au>Bentzen, Craig L</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>gem-Diphosphonate and gem-phosphonate-phosphate compounds with specific high density lipoprotein inducing activity</atitle><jtitle>Journal of medicinal chemistry</jtitle><addtitle>J. Med. Chem</addtitle><date>1987-08-01</date><risdate>1987</risdate><volume>30</volume><issue>8</issue><spage>1426</spage><epage>1433</epage><pages>1426-1433</pages><issn>0022-2623</issn><eissn>1520-4804</eissn><coden>JMCMAR</coden><abstract>New diphosphonate compounds and related derivatives were synthesized and investigated for their activity in specifically inducing plasma high density lipoproteins (HDL) and high density lipoprotein cholesterol (HDL-C) in normal rats. The screening of numerous compounds has permitted the determination of the structural variations leading to optimal plasma lipid altering activity, indicating antiatherosclerotic potential. Among the compounds observed to be the most active, dimethyl alpha-(dimethoxyphosphinyl)-p-chlorobenzyl phosphate (20, SR-202, mifobate) was selected for further pharmacological and subsequent clinical development.</abstract><cop>Washington, DC</cop><pub>American Chemical Society</pub><pmid>3612689</pmid><doi>10.1021/jm00391a027</doi><tpages>8</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0022-2623 |
| ispartof | Journal of medicinal chemistry, 1987-08, Vol.30 (8), p.1426-1433 |
| issn | 0022-2623 1520-4804 |
| language | eng |
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| source | ACS Publications; MEDLINE |
| subjects | Animals Chemical Phenomena Chemistry Cholesterol, HDL - blood Diphosphonates - chemical synthesis Diphosphonates - pharmacology Exact sciences and technology Lipoproteins, HDL - blood Male Organic chemistry Organometalloidal and organometallic compounds P derivatives Phosphates - chemical synthesis Phosphates - pharmacology Preparations and properties Rats Rats, Inbred Strains Structure-Activity Relationship |
| title | gem-Diphosphonate and gem-phosphonate-phosphate compounds with specific high density lipoprotein inducing activity |
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