The First Potent and Selective Non-Imidazole Human Histamine H4 Receptor Antagonists
Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10 l, which are the first potent and selective histamine...
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| Veröffentlicht in: | Journal of medicinal chemistry 2003-09, Vol.46 (19), p.3957-3960 |
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| container_end_page | 3960 |
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| container_issue | 19 |
| container_start_page | 3957 |
| container_title | Journal of medicinal chemistry |
| container_volume | 46 |
| creator | Jablonowski, Jill A Grice, Cheryl A Chai, Wenying Dvorak, Curt A Venable, Jennifer D Kwok, Annette K Ly, Kiev S Wei, Jianmei Baker, Sherry M Desai, Pragnya J Jiang, Wen Wilson, Sandy J Thurmond, Robin L Karlsson, Lars Edwards, James P Lovenberg, Timothy W Carruthers, Nicholas I |
| description | Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10 l, which are the first potent and selective histamine H4 receptor antagonists to be described. |
| doi_str_mv | 10.1021/jm0341047 |
| format | Article |
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Investigation of the SAR resulted in the discovery of novel compounds 10e and 10 l, which are the first potent and selective histamine H4 receptor antagonists to be described.</description><identifier>ISSN: 0022-2623</identifier><identifier>EISSN: 1520-4804</identifier><identifier>DOI: 10.1021/jm0341047</identifier><identifier>PMID: 12954048</identifier><identifier>CODEN: JMCMAR</identifier><language>eng</language><publisher>Washington, DC: American Chemical Society</publisher><subject>Animals ; Biological and medical sciences ; Cell Line ; Dose-Response Relationship, Drug ; Histamine Antagonists - chemistry ; Histamine Antagonists - metabolism ; Histamine Antagonists - pharmacology ; Humans ; Indoles - chemistry ; Indoles - metabolism ; Indoles - pharmacology ; Kinetics ; Ligands ; Medical sciences ; Miscellaneous ; Neurons - cytology ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Pharmacology. Drug treatments ; Piperazines - chemistry ; Piperazines - metabolism ; Piperazines - pharmacology ; Radioligand Assay ; Rats ; Receptors, Cell Surface - drug effects ; Receptors, Cell Surface - genetics ; Receptors, Cell Surface - metabolism ; Receptors, G-Protein-Coupled ; Receptors, Histamine ; Receptors, Histamine H4 ; Recombinant Proteins - drug effects ; Recombinant Proteins - genetics ; Recombinant Proteins - metabolism ; Structure-Activity Relationship ; Transfection</subject><ispartof>Journal of medicinal chemistry, 2003-09, Vol.46 (19), p.3957-3960</ispartof><rights>Copyright © 2003 American Chemical Society</rights><rights>2003 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://pubs.acs.org/doi/pdf/10.1021/jm0341047$$EPDF$$P50$$Gacs$$H</linktopdf><linktohtml>$$Uhttps://pubs.acs.org/doi/10.1021/jm0341047$$EHTML$$P50$$Gacs$$H</linktohtml><link.rule.ids>314,776,780,27055,27903,27904,56716,56766</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=15107730$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/12954048$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Jablonowski, Jill A</creatorcontrib><creatorcontrib>Grice, Cheryl A</creatorcontrib><creatorcontrib>Chai, Wenying</creatorcontrib><creatorcontrib>Dvorak, Curt A</creatorcontrib><creatorcontrib>Venable, Jennifer D</creatorcontrib><creatorcontrib>Kwok, Annette K</creatorcontrib><creatorcontrib>Ly, Kiev S</creatorcontrib><creatorcontrib>Wei, Jianmei</creatorcontrib><creatorcontrib>Baker, Sherry M</creatorcontrib><creatorcontrib>Desai, Pragnya J</creatorcontrib><creatorcontrib>Jiang, Wen</creatorcontrib><creatorcontrib>Wilson, Sandy J</creatorcontrib><creatorcontrib>Thurmond, Robin L</creatorcontrib><creatorcontrib>Karlsson, Lars</creatorcontrib><creatorcontrib>Edwards, James P</creatorcontrib><creatorcontrib>Lovenberg, Timothy W</creatorcontrib><creatorcontrib>Carruthers, Nicholas I</creatorcontrib><title>The First Potent and Selective Non-Imidazole Human Histamine H4 Receptor Antagonists</title><title>Journal of medicinal chemistry</title><addtitle>J. Med. Chem</addtitle><description>Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10 l, which are the first potent and selective histamine H4 receptor antagonists to be described.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Cell Line</subject><subject>Dose-Response Relationship, Drug</subject><subject>Histamine Antagonists - chemistry</subject><subject>Histamine Antagonists - metabolism</subject><subject>Histamine Antagonists - pharmacology</subject><subject>Humans</subject><subject>Indoles - chemistry</subject><subject>Indoles - metabolism</subject><subject>Indoles - pharmacology</subject><subject>Kinetics</subject><subject>Ligands</subject><subject>Medical sciences</subject><subject>Miscellaneous</subject><subject>Neurons - cytology</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>Pharmacology. Drug treatments</subject><subject>Piperazines - chemistry</subject><subject>Piperazines - metabolism</subject><subject>Piperazines - pharmacology</subject><subject>Radioligand Assay</subject><subject>Rats</subject><subject>Receptors, Cell Surface - drug effects</subject><subject>Receptors, Cell Surface - genetics</subject><subject>Receptors, Cell Surface - metabolism</subject><subject>Receptors, G-Protein-Coupled</subject><subject>Receptors, Histamine</subject><subject>Receptors, Histamine H4</subject><subject>Recombinant Proteins - drug effects</subject><subject>Recombinant Proteins - genetics</subject><subject>Recombinant Proteins - metabolism</subject><subject>Structure-Activity Relationship</subject><subject>Transfection</subject><issn>0022-2623</issn><issn>1520-4804</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2003</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkU9P3DAQxa2qqCzQQ79A5Ut7Sxn_SZwe6arbRVoBgkVCXKyxM2mzTZwldlDh0zeIBU6j0fvpaeY9xj4J-CZAiuNNB0oL0OYdm4lcQqZL0O_ZDEDKTBZS7bODGDcAoIRUH9i-kN9zDbqcsfX6D_FFM8TEL_pEIXEMFb-ilnxq7omf9SE77ZoKH_uW-HLsMPBlExN2TZh2zS_J0zb1Az8JCX_3YdLiEdursY30cTcP2fXi53q-zFbnv07nJ6sMpYSUCXCulFqaHEtpFJBAkZdovKwLU1DhyLgK0dUu19772gijHJRUey_BFZU6ZF-ffbdDfzdSTLZroqe2xUD9GK1RhYJClRP4eQeOrqPKboemw-HBvuQwAV92AEaPbT1g8E1843IBZrpw4rJnbnqT_r3qOPy1hVEmt-uLK3ur54vVzY9Lu3jzRR_tph-HMOVhBdin3uxrb-o_EiaF2Q</recordid><startdate>20030911</startdate><enddate>20030911</enddate><creator>Jablonowski, Jill A</creator><creator>Grice, Cheryl A</creator><creator>Chai, Wenying</creator><creator>Dvorak, Curt A</creator><creator>Venable, Jennifer D</creator><creator>Kwok, Annette K</creator><creator>Ly, Kiev S</creator><creator>Wei, Jianmei</creator><creator>Baker, Sherry M</creator><creator>Desai, Pragnya J</creator><creator>Jiang, Wen</creator><creator>Wilson, Sandy J</creator><creator>Thurmond, Robin L</creator><creator>Karlsson, Lars</creator><creator>Edwards, James P</creator><creator>Lovenberg, Timothy W</creator><creator>Carruthers, Nicholas I</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>7X8</scope></search><sort><creationdate>20030911</creationdate><title>The First Potent and Selective Non-Imidazole Human Histamine H4 Receptor Antagonists</title><author>Jablonowski, Jill A ; Grice, Cheryl A ; Chai, Wenying ; Dvorak, Curt A ; Venable, Jennifer D ; Kwok, Annette K ; Ly, Kiev S ; Wei, Jianmei ; Baker, Sherry M ; Desai, Pragnya J ; Jiang, Wen ; Wilson, Sandy J ; Thurmond, Robin L ; Karlsson, Lars ; Edwards, James P ; Lovenberg, Timothy W ; Carruthers, Nicholas I</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-a220t-10bb824275a82730e1a158a7c2f676e6be7bdaabfb54cccf7173b08efcc20b6d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2003</creationdate><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Cell Line</topic><topic>Dose-Response Relationship, Drug</topic><topic>Histamine Antagonists - chemistry</topic><topic>Histamine Antagonists - metabolism</topic><topic>Histamine Antagonists - pharmacology</topic><topic>Humans</topic><topic>Indoles - chemistry</topic><topic>Indoles - metabolism</topic><topic>Indoles - pharmacology</topic><topic>Kinetics</topic><topic>Ligands</topic><topic>Medical sciences</topic><topic>Miscellaneous</topic><topic>Neurons - cytology</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. Neurotransmission. Receptors</topic><topic>Pharmacology. Drug treatments</topic><topic>Piperazines - chemistry</topic><topic>Piperazines - metabolism</topic><topic>Piperazines - pharmacology</topic><topic>Radioligand Assay</topic><topic>Rats</topic><topic>Receptors, Cell Surface - drug effects</topic><topic>Receptors, Cell Surface - genetics</topic><topic>Receptors, Cell Surface - metabolism</topic><topic>Receptors, G-Protein-Coupled</topic><topic>Receptors, Histamine</topic><topic>Receptors, Histamine H4</topic><topic>Recombinant Proteins - drug effects</topic><topic>Recombinant Proteins - genetics</topic><topic>Recombinant Proteins - metabolism</topic><topic>Structure-Activity Relationship</topic><topic>Transfection</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Jablonowski, Jill A</creatorcontrib><creatorcontrib>Grice, Cheryl A</creatorcontrib><creatorcontrib>Chai, Wenying</creatorcontrib><creatorcontrib>Dvorak, Curt A</creatorcontrib><creatorcontrib>Venable, Jennifer D</creatorcontrib><creatorcontrib>Kwok, Annette K</creatorcontrib><creatorcontrib>Ly, Kiev S</creatorcontrib><creatorcontrib>Wei, Jianmei</creatorcontrib><creatorcontrib>Baker, Sherry M</creatorcontrib><creatorcontrib>Desai, Pragnya J</creatorcontrib><creatorcontrib>Jiang, Wen</creatorcontrib><creatorcontrib>Wilson, Sandy J</creatorcontrib><creatorcontrib>Thurmond, Robin L</creatorcontrib><creatorcontrib>Karlsson, Lars</creatorcontrib><creatorcontrib>Edwards, James P</creatorcontrib><creatorcontrib>Lovenberg, Timothy W</creatorcontrib><creatorcontrib>Carruthers, Nicholas I</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>MEDLINE - Academic</collection><jtitle>Journal of medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Jablonowski, Jill A</au><au>Grice, Cheryl A</au><au>Chai, Wenying</au><au>Dvorak, Curt A</au><au>Venable, Jennifer D</au><au>Kwok, Annette K</au><au>Ly, Kiev S</au><au>Wei, Jianmei</au><au>Baker, Sherry M</au><au>Desai, Pragnya J</au><au>Jiang, Wen</au><au>Wilson, Sandy J</au><au>Thurmond, Robin L</au><au>Karlsson, Lars</au><au>Edwards, James P</au><au>Lovenberg, Timothy W</au><au>Carruthers, Nicholas I</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The First Potent and Selective Non-Imidazole Human Histamine H4 Receptor Antagonists</atitle><jtitle>Journal of medicinal chemistry</jtitle><addtitle>J. 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| fulltext | fulltext |
| identifier | ISSN: 0022-2623 |
| ispartof | Journal of medicinal chemistry, 2003-09, Vol.46 (19), p.3957-3960 |
| issn | 0022-2623 1520-4804 |
| language | eng |
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| source | MEDLINE; ACS Publications |
| subjects | Animals Biological and medical sciences Cell Line Dose-Response Relationship, Drug Histamine Antagonists - chemistry Histamine Antagonists - metabolism Histamine Antagonists - pharmacology Humans Indoles - chemistry Indoles - metabolism Indoles - pharmacology Kinetics Ligands Medical sciences Miscellaneous Neurons - cytology Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Piperazines - chemistry Piperazines - metabolism Piperazines - pharmacology Radioligand Assay Rats Receptors, Cell Surface - drug effects Receptors, Cell Surface - genetics Receptors, Cell Surface - metabolism Receptors, G-Protein-Coupled Receptors, Histamine Receptors, Histamine H4 Recombinant Proteins - drug effects Recombinant Proteins - genetics Recombinant Proteins - metabolism Structure-Activity Relationship Transfection |
| title | The First Potent and Selective Non-Imidazole Human Histamine H4 Receptor Antagonists |
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