5,6-Diphenylpyridazine Derivatives as Acyl-CoA:Cholesterol Acyltransferase Inhibitors
Alkyl-5,6-diphenylpyridazine derivatives combining several main features of ACAT inhibitors, such as a long alkyl side chain linked to a heterocycle and the o-diphenyl system, were synthesized and tested. Moreover, modeling studies on representative terms were performed. Some compounds displayed ACA...
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| Veröffentlicht in: | Journal of medicinal chemistry 2001-11, Vol.44 (24), p.4292-4295 |
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| container_end_page | 4295 |
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| container_issue | 24 |
| container_start_page | 4292 |
| container_title | Journal of medicinal chemistry |
| container_volume | 44 |
| creator | Giovannoni, Maria Paola Piaz, Vittorio Dal Kwon, Byoung-Mog Kim, Mi-Kyung Kim, Young-Kook Toma, Lucio Barlocco, Daniela Bernini, Franco Canavesi, Monica |
| description | Alkyl-5,6-diphenylpyridazine derivatives combining several main features of ACAT inhibitors, such as a long alkyl side chain linked to a heterocycle and the o-diphenyl system, were synthesized and tested. Moreover, modeling studies on representative terms were performed. Some compounds displayed ACAT inhibition in the micromolar range, both on the enzyme isolated from rat liver microsomes and in cell-free homogenate of murine macrophages. |
| doi_str_mv | 10.1021/jm010807h |
| format | Article |
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Moreover, modeling studies on representative terms were performed. Some compounds displayed ACAT inhibition in the micromolar range, both on the enzyme isolated from rat liver microsomes and in cell-free homogenate of murine macrophages.</description><identifier>ISSN: 0022-2623</identifier><identifier>EISSN: 1520-4804</identifier><identifier>DOI: 10.1021/jm010807h</identifier><identifier>PMID: 11708931</identifier><identifier>CODEN: JMCMAR</identifier><language>eng</language><publisher>Washington, DC: American Chemical Society</publisher><subject>Animals ; Biological and medical sciences ; Cell-Free System ; Enzyme Inhibitors - chemical synthesis ; Enzyme Inhibitors - chemistry ; Enzyme Inhibitors - pharmacology ; General and cellular metabolism. Vitamins ; In Vitro Techniques ; Macrophages - drug effects ; Macrophages - enzymology ; Medical sciences ; Mice ; Microsomes, Liver - drug effects ; Microsomes, Liver - enzymology ; Models, Molecular ; Pharmacology. Drug treatments ; Pyridazines - chemical synthesis ; Pyridazines - chemistry ; Pyridazines - pharmacology ; Rats ; Sterol O-Acyltransferase - antagonists & inhibitors ; Structure-Activity Relationship</subject><ispartof>Journal of medicinal chemistry, 2001-11, Vol.44 (24), p.4292-4295</ispartof><rights>Copyright © 2001 American Chemical Society</rights><rights>2002 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-a379t-a9ab146c443d4e3a30e0eb8521810af6d5b91b608e51460f6549713785f003223</citedby><cites>FETCH-LOGICAL-a379t-a9ab146c443d4e3a30e0eb8521810af6d5b91b608e51460f6549713785f003223</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://pubs.acs.org/doi/pdf/10.1021/jm010807h$$EPDF$$P50$$Gacs$$H</linktopdf><linktohtml>$$Uhttps://pubs.acs.org/doi/10.1021/jm010807h$$EHTML$$P50$$Gacs$$H</linktohtml><link.rule.ids>314,780,784,2765,27076,27924,27925,56738,56788</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=14125424$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/11708931$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Giovannoni, Maria Paola</creatorcontrib><creatorcontrib>Piaz, Vittorio Dal</creatorcontrib><creatorcontrib>Kwon, Byoung-Mog</creatorcontrib><creatorcontrib>Kim, Mi-Kyung</creatorcontrib><creatorcontrib>Kim, Young-Kook</creatorcontrib><creatorcontrib>Toma, Lucio</creatorcontrib><creatorcontrib>Barlocco, Daniela</creatorcontrib><creatorcontrib>Bernini, Franco</creatorcontrib><creatorcontrib>Canavesi, Monica</creatorcontrib><title>5,6-Diphenylpyridazine Derivatives as Acyl-CoA:Cholesterol Acyltransferase Inhibitors</title><title>Journal of medicinal chemistry</title><addtitle>J. Med. Chem</addtitle><description>Alkyl-5,6-diphenylpyridazine derivatives combining several main features of ACAT inhibitors, such as a long alkyl side chain linked to a heterocycle and the o-diphenyl system, were synthesized and tested. Moreover, modeling studies on representative terms were performed. Some compounds displayed ACAT inhibition in the micromolar range, both on the enzyme isolated from rat liver microsomes and in cell-free homogenate of murine macrophages.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Cell-Free System</subject><subject>Enzyme Inhibitors - chemical synthesis</subject><subject>Enzyme Inhibitors - chemistry</subject><subject>Enzyme Inhibitors - pharmacology</subject><subject>General and cellular metabolism. Vitamins</subject><subject>In Vitro Techniques</subject><subject>Macrophages - drug effects</subject><subject>Macrophages - enzymology</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Microsomes, Liver - drug effects</subject><subject>Microsomes, Liver - enzymology</subject><subject>Models, Molecular</subject><subject>Pharmacology. Drug treatments</subject><subject>Pyridazines - chemical synthesis</subject><subject>Pyridazines - chemistry</subject><subject>Pyridazines - pharmacology</subject><subject>Rats</subject><subject>Sterol O-Acyltransferase - antagonists & inhibitors</subject><subject>Structure-Activity Relationship</subject><issn>0022-2623</issn><issn>1520-4804</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2001</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpt0E1v00AQgOEVAtFQOPAHUC4gIeEys1-2e4tcoJVaUaC9cFmNnbGywbHDrlMRfn2XJmounFbafTSafYV4jXCCIPHjcgUIBeSLJ2KCRkKmC9BPxQRAykxaqY7EixiXAKBQqufiCDGHolQ4Ebfmg83O_HrB_bZbb4Of01_f8_SMg7-j0d9xnFKczpptl1XD7LRaDB3HkcPQPVyOgfrYcqDI04t-4Ws_DiG-FM9a6iK_2p_H4vbzp5vqPLv8-uWiml1mpPJyzKikGrVttFZzzYoUMHBdGIkFArV2buoSawsFm8SgtUaXOaq8MG36ipTqWLzbzV2H4fcm7eVWPjbcddTzsIkul7KwiDbB9zvYhCHGwK1bB7-isHUI7l9D99gw2Tf7oZt6xfOD3EdL4O0eUGyoa1OCxseD0yiNljq5bOd8Cvbn8Z3CL2dzlRt3c_3D_bz6fv3N2MpdHeZSE91y2IQ-tfvPgvfAKpMA</recordid><startdate>20011122</startdate><enddate>20011122</enddate><creator>Giovannoni, Maria Paola</creator><creator>Piaz, Vittorio Dal</creator><creator>Kwon, Byoung-Mog</creator><creator>Kim, Mi-Kyung</creator><creator>Kim, Young-Kook</creator><creator>Toma, Lucio</creator><creator>Barlocco, Daniela</creator><creator>Bernini, Franco</creator><creator>Canavesi, Monica</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>20011122</creationdate><title>5,6-Diphenylpyridazine Derivatives as Acyl-CoA:Cholesterol Acyltransferase Inhibitors</title><author>Giovannoni, Maria Paola ; Piaz, Vittorio Dal ; Kwon, Byoung-Mog ; Kim, Mi-Kyung ; Kim, Young-Kook ; Toma, Lucio ; Barlocco, Daniela ; Bernini, Franco ; Canavesi, Monica</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-a379t-a9ab146c443d4e3a30e0eb8521810af6d5b91b608e51460f6549713785f003223</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2001</creationdate><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Cell-Free System</topic><topic>Enzyme Inhibitors - chemical synthesis</topic><topic>Enzyme Inhibitors - chemistry</topic><topic>Enzyme Inhibitors - pharmacology</topic><topic>General and cellular metabolism. Vitamins</topic><topic>In Vitro Techniques</topic><topic>Macrophages - drug effects</topic><topic>Macrophages - enzymology</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Microsomes, Liver - drug effects</topic><topic>Microsomes, Liver - enzymology</topic><topic>Models, Molecular</topic><topic>Pharmacology. Drug treatments</topic><topic>Pyridazines - chemical synthesis</topic><topic>Pyridazines - chemistry</topic><topic>Pyridazines - pharmacology</topic><topic>Rats</topic><topic>Sterol O-Acyltransferase - antagonists & inhibitors</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Giovannoni, Maria Paola</creatorcontrib><creatorcontrib>Piaz, Vittorio Dal</creatorcontrib><creatorcontrib>Kwon, Byoung-Mog</creatorcontrib><creatorcontrib>Kim, Mi-Kyung</creatorcontrib><creatorcontrib>Kim, Young-Kook</creatorcontrib><creatorcontrib>Toma, Lucio</creatorcontrib><creatorcontrib>Barlocco, Daniela</creatorcontrib><creatorcontrib>Bernini, Franco</creatorcontrib><creatorcontrib>Canavesi, Monica</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>Giovannoni, Maria Paola</au><au>Piaz, Vittorio Dal</au><au>Kwon, Byoung-Mog</au><au>Kim, Mi-Kyung</au><au>Kim, Young-Kook</au><au>Toma, Lucio</au><au>Barlocco, Daniela</au><au>Bernini, Franco</au><au>Canavesi, Monica</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>5,6-Diphenylpyridazine Derivatives as Acyl-CoA:Cholesterol Acyltransferase Inhibitors</atitle><jtitle>Journal of medicinal chemistry</jtitle><addtitle>J. Med. Chem</addtitle><date>2001-11-22</date><risdate>2001</risdate><volume>44</volume><issue>24</issue><spage>4292</spage><epage>4295</epage><pages>4292-4295</pages><issn>0022-2623</issn><eissn>1520-4804</eissn><coden>JMCMAR</coden><abstract>Alkyl-5,6-diphenylpyridazine derivatives combining several main features of ACAT inhibitors, such as a long alkyl side chain linked to a heterocycle and the o-diphenyl system, were synthesized and tested. Moreover, modeling studies on representative terms were performed. Some compounds displayed ACAT inhibition in the micromolar range, both on the enzyme isolated from rat liver microsomes and in cell-free homogenate of murine macrophages.</abstract><cop>Washington, DC</cop><pub>American Chemical Society</pub><pmid>11708931</pmid><doi>10.1021/jm010807h</doi><tpages>4</tpages></addata></record> |
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| ispartof | Journal of medicinal chemistry, 2001-11, Vol.44 (24), p.4292-4295 |
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| subjects | Animals Biological and medical sciences Cell-Free System Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology General and cellular metabolism. Vitamins In Vitro Techniques Macrophages - drug effects Macrophages - enzymology Medical sciences Mice Microsomes, Liver - drug effects Microsomes, Liver - enzymology Models, Molecular Pharmacology. Drug treatments Pyridazines - chemical synthesis Pyridazines - chemistry Pyridazines - pharmacology Rats Sterol O-Acyltransferase - antagonists & inhibitors Structure-Activity Relationship |
| title | 5,6-Diphenylpyridazine Derivatives as Acyl-CoA:Cholesterol Acyltransferase Inhibitors |
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