Fluorobenzamidrazone thrombin inhibitors: Influence of fluorine on enhancing oral absorption
LB30057 ( 1) is a selective and efficacious oral thrombin inhibitor. Fluorine-substitution on the phenylene ring of the benzamidrazone portion in both compound 1 and its derivatives gave, in many cases, enhanced oral absorption in rats while maintaining the intrinsic potency and selectivity. Compoun...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 1999-09, Vol.9 (17), p.2483-2486 |
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| container_end_page | 2486 |
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| container_issue | 17 |
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| container_title | Bioorganic & medicinal chemistry letters |
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| creator | Lee, Koo Jung, Won-Hyuk Hwang, Sang Yeul Lee, Sung-Hack |
| description | LB30057 (
1) is a selective and efficacious oral thrombin inhibitor. Fluorine-substitution on the phenylene ring of the benzamidrazone portion in both compound
1 and its derivatives gave, in many cases, enhanced oral absorption in rats while maintaining the intrinsic potency and selectivity. Compound
2 demonstrated a 3-fold increase in absorption. |
| doi_str_mv | 10.1016/S0960-894X(99)00412-6 |
| format | Article |
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1) is a selective and efficacious oral thrombin inhibitor. Fluorine-substitution on the phenylene ring of the benzamidrazone portion in both compound
1 and its derivatives gave, in many cases, enhanced oral absorption in rats while maintaining the intrinsic potency and selectivity. Compound
2 demonstrated a 3-fold increase in absorption.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/S0960-894X(99)00412-6</identifier><identifier>PMID: 10498193</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>Administration, Oral ; Animals ; Antithrombins - administration & dosage ; Antithrombins - chemistry ; Antithrombins - pharmacokinetics ; Benzamides - administration & dosage ; Benzamides - chemistry ; Benzamides - pharmacokinetics ; Biological and medical sciences ; Blood. Blood coagulation. Reticuloendothelial system ; Dogs ; Fluorine - chemistry ; Medical sciences ; Pharmacology. Drug treatments ; Rats</subject><ispartof>Bioorganic & medicinal chemistry letters, 1999-09, Vol.9 (17), p.2483-2486</ispartof><rights>1999</rights><rights>1999 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c456t-4521b0e9db0f55259d51a64a981856ec07f3008dadac89fa74ad548262253d393</citedby><cites>FETCH-LOGICAL-c456t-4521b0e9db0f55259d51a64a981856ec07f3008dadac89fa74ad548262253d393</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0960-894X(99)00412-6$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,777,781,3537,27905,27906,45976</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1953859$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/10498193$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Lee, Koo</creatorcontrib><creatorcontrib>Jung, Won-Hyuk</creatorcontrib><creatorcontrib>Hwang, Sang Yeul</creatorcontrib><creatorcontrib>Lee, Sung-Hack</creatorcontrib><title>Fluorobenzamidrazone thrombin inhibitors: Influence of fluorine on enhancing oral absorption</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>LB30057 (
1) is a selective and efficacious oral thrombin inhibitor. Fluorine-substitution on the phenylene ring of the benzamidrazone portion in both compound
1 and its derivatives gave, in many cases, enhanced oral absorption in rats while maintaining the intrinsic potency and selectivity. Compound
2 demonstrated a 3-fold increase in absorption.</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Antithrombins - administration & dosage</subject><subject>Antithrombins - chemistry</subject><subject>Antithrombins - pharmacokinetics</subject><subject>Benzamides - administration & dosage</subject><subject>Benzamides - chemistry</subject><subject>Benzamides - pharmacokinetics</subject><subject>Biological and medical sciences</subject><subject>Blood. Blood coagulation. Reticuloendothelial system</subject><subject>Dogs</subject><subject>Fluorine - chemistry</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Rats</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1999</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkM1rFDEYxoNY3HX1T1DmIKUepr6ZfGziRUpxbaHgQQUPQsjkw43MJNtkRuj-9Z3pLtZbT-_l9zzvww-hNxjOMWD-4RtIDrWQ9OeZlO8BKG5q_gwtMeW0JhTYc7T8hyzQy1L-AGAKlL5ACwxUCizJEv3adGPKqXVxr_tgs96n6Kphm1PfhliFuA1tGFIuH6vr6LvRReOq5Cs_x8KEpli5uNXRhPi7Sll3lW5LyrshpPgKnXjdFff6eFfox-bz98ur-ubrl-vLi5vaUMaHmrIGt-CkbcEz1jBpGdac6mmiYNwZWHsCIKy22gjp9Zpqy6hoeNMwYokkK3R66N3ldDu6Mqg-FOO6TkeXxqLWAEwQSSeQHUCTUynZebXLodf5TmFQs1b1oFXNzpSU6kGr4lPu7fHB2PbO_pc6eJyAd0dAF6M7n2ch5ZGTjAg2D_10wNxk429wWRUTZqU2ZGcGZVN4Ysk92ReVvg</recordid><startdate>19990906</startdate><enddate>19990906</enddate><creator>Lee, Koo</creator><creator>Jung, Won-Hyuk</creator><creator>Hwang, Sang Yeul</creator><creator>Lee, Sung-Hack</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>19990906</creationdate><title>Fluorobenzamidrazone thrombin inhibitors: Influence of fluorine on enhancing oral absorption</title><author>Lee, Koo ; Jung, Won-Hyuk ; Hwang, Sang Yeul ; Lee, Sung-Hack</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c456t-4521b0e9db0f55259d51a64a981856ec07f3008dadac89fa74ad548262253d393</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1999</creationdate><topic>Administration, Oral</topic><topic>Animals</topic><topic>Antithrombins - administration & dosage</topic><topic>Antithrombins - chemistry</topic><topic>Antithrombins - pharmacokinetics</topic><topic>Benzamides - administration & dosage</topic><topic>Benzamides - chemistry</topic><topic>Benzamides - pharmacokinetics</topic><topic>Biological and medical sciences</topic><topic>Blood. Blood coagulation. Reticuloendothelial system</topic><topic>Dogs</topic><topic>Fluorine - chemistry</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><topic>Rats</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Lee, Koo</creatorcontrib><creatorcontrib>Jung, Won-Hyuk</creatorcontrib><creatorcontrib>Hwang, Sang Yeul</creatorcontrib><creatorcontrib>Lee, Sung-Hack</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>Lee, Koo</au><au>Jung, Won-Hyuk</au><au>Hwang, Sang Yeul</au><au>Lee, Sung-Hack</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Fluorobenzamidrazone thrombin inhibitors: Influence of fluorine on enhancing oral absorption</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>1999-09-06</date><risdate>1999</risdate><volume>9</volume><issue>17</issue><spage>2483</spage><epage>2486</epage><pages>2483-2486</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>LB30057 (
1) is a selective and efficacious oral thrombin inhibitor. Fluorine-substitution on the phenylene ring of the benzamidrazone portion in both compound
1 and its derivatives gave, in many cases, enhanced oral absorption in rats while maintaining the intrinsic potency and selectivity. Compound
2 demonstrated a 3-fold increase in absorption.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>10498193</pmid><doi>10.1016/S0960-894X(99)00412-6</doi><tpages>4</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 1999-09, Vol.9 (17), p.2483-2486 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Administration, Oral Animals Antithrombins - administration & dosage Antithrombins - chemistry Antithrombins - pharmacokinetics Benzamides - administration & dosage Benzamides - chemistry Benzamides - pharmacokinetics Biological and medical sciences Blood. Blood coagulation. Reticuloendothelial system Dogs Fluorine - chemistry Medical sciences Pharmacology. Drug treatments Rats |
| title | Fluorobenzamidrazone thrombin inhibitors: Influence of fluorine on enhancing oral absorption |
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