A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis
A novel p38 MAP kinase inhibitor structural class was discovered through selectivity screening. The rational analogue design, synthesis and structure-activity relationship of this series of bis-amide inhibitors is reported. The inhibition in vitro of human p38alpha enzyme activity and lipopolysaccha...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2004-11, Vol.14 (21), p.5383-5387 |
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| container_end_page | 5387 |
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| container_issue | 21 |
| container_start_page | 5383 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 14 |
| creator | BROWN, Dearg S BELFIELD, Andrew J BROWN, George R CAMPBELL, Douglas FOUBISTER, Alan MASTERS, David J PIKE, Kurt G SNELSON, Wendy L WELLS, Stuart L |
| description | A novel p38 MAP kinase inhibitor structural class was discovered through selectivity screening. The rational analogue design, synthesis and structure-activity relationship of this series of bis-amide inhibitors is reported. The inhibition in vitro of human p38alpha enzyme activity and lipopolysaccharide-induced tumour necrosis factor-alpha release is described for the series. The activity in vivo and pharmacokinetic properties are exemplified for the more potent analogues. |
| doi_str_mv | 10.1016/j.bmcl.2004.08.006 |
| format | Article |
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The rational analogue design, synthesis and structure-activity relationship of this series of bis-amide inhibitors is reported. The inhibition in vitro of human p38alpha enzyme activity and lipopolysaccharide-induced tumour necrosis factor-alpha release is described for the series. The activity in vivo and pharmacokinetic properties are exemplified for the more potent analogues.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2004.08.006</identifier><identifier>PMID: 15454231</identifier><language>eng</language><publisher>Oxford: Elsevier</publisher><subject>Amides - chemical synthesis ; Amides - pharmacokinetics ; Amides - pharmacology ; Animals ; Antirheumatic Agents - chemical synthesis ; Antirheumatic Agents - pharmacokinetics ; Antirheumatic Agents - pharmacology ; Arthritis, Rheumatoid - drug therapy ; Biological and medical sciences ; Bones, joints and connective tissue. Antiinflammatory agents ; Humans ; In Vitro Techniques ; Leukocytes, Mononuclear - drug effects ; Leukocytes, Mononuclear - metabolism ; Lipopolysaccharides - pharmacology ; Medical sciences ; Mice ; Mice, Inbred BALB C ; p38 Mitogen-Activated Protein Kinases - antagonists & inhibitors ; Pharmacology. 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The rational analogue design, synthesis and structure-activity relationship of this series of bis-amide inhibitors is reported. The inhibition in vitro of human p38alpha enzyme activity and lipopolysaccharide-induced tumour necrosis factor-alpha release is described for the series. The activity in vivo and pharmacokinetic properties are exemplified for the more potent analogues.</description><subject>Amides - chemical synthesis</subject><subject>Amides - pharmacokinetics</subject><subject>Amides - pharmacology</subject><subject>Animals</subject><subject>Antirheumatic Agents - chemical synthesis</subject><subject>Antirheumatic Agents - pharmacokinetics</subject><subject>Antirheumatic Agents - pharmacology</subject><subject>Arthritis, Rheumatoid - drug therapy</subject><subject>Biological and medical sciences</subject><subject>Bones, joints and connective tissue. Antiinflammatory agents</subject><subject>Humans</subject><subject>In Vitro Techniques</subject><subject>Leukocytes, Mononuclear - drug effects</subject><subject>Leukocytes, Mononuclear - metabolism</subject><subject>Lipopolysaccharides - pharmacology</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Mice, Inbred BALB C</subject><subject>p38 Mitogen-Activated Protein Kinases - antagonists & inhibitors</subject><subject>Pharmacology. Drug treatments</subject><subject>Rats</subject><subject>Structure-Activity Relationship</subject><subject>Time Factors</subject><subject>Tumor Necrosis Factor-alpha - antagonists & inhibitors</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2004</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkEtLxDAUhYMoOj7-gAvJRnetN83DdDmIL1B0oeAupO0Nk7FtxiQj-O_tMAOuLge-c-B-hJwzKBkwdb0sm6HtywpAlKBLALVHZkwoUXABcp_MoFZQ6Fp8HpHjlJYATIAQh-SISSFFxdmMmDkdww_2NGH0mGhwdMU1fZm_0S8_2oTUjwvf-Bxioi5EmhdIVyHjmL3taY5o8zCFTTEucD3YHHxHbcyL6LNPp-TA2T7h2e6ekI_7u_fbx-L59eHpdv5ctPyG54LVtRROd7Wqugac1Rw0gmw6oZiUUjnOwN20HCRDdLXsZMtEPeFKVlpwyU_I1XZ3FcP3GlM2g08t9r0dMayTUaqupNBsAqst2MaQUkRnVtEPNv4aBmaj1SzNRqvZaDWgzaR1Kl3s1tfNgN1_ZedxAi53gE2t7V20Y-vTP6eY0NNv_A8Y-oC2</recordid><startdate>20041101</startdate><enddate>20041101</enddate><creator>BROWN, Dearg S</creator><creator>BELFIELD, Andrew J</creator><creator>BROWN, George R</creator><creator>CAMPBELL, Douglas</creator><creator>FOUBISTER, Alan</creator><creator>MASTERS, David J</creator><creator>PIKE, Kurt G</creator><creator>SNELSON, Wendy L</creator><creator>WELLS, Stuart L</creator><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>20041101</creationdate><title>A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis</title><author>BROWN, Dearg S ; BELFIELD, Andrew J ; BROWN, George R ; CAMPBELL, Douglas ; FOUBISTER, Alan ; MASTERS, David J ; PIKE, Kurt G ; SNELSON, Wendy L ; WELLS, Stuart L</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c373t-19954f8d962db0fa8308e05bd4615556f310f7c3051eef95d5c149d9665284353</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2004</creationdate><topic>Amides - chemical synthesis</topic><topic>Amides - pharmacokinetics</topic><topic>Amides - pharmacology</topic><topic>Animals</topic><topic>Antirheumatic Agents - chemical synthesis</topic><topic>Antirheumatic Agents - pharmacokinetics</topic><topic>Antirheumatic Agents - pharmacology</topic><topic>Arthritis, Rheumatoid - drug therapy</topic><topic>Biological and medical sciences</topic><topic>Bones, joints and connective tissue. 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Drug treatments</topic><topic>Rats</topic><topic>Structure-Activity Relationship</topic><topic>Time Factors</topic><topic>Tumor Necrosis Factor-alpha - antagonists & inhibitors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>BROWN, Dearg S</creatorcontrib><creatorcontrib>BELFIELD, Andrew J</creatorcontrib><creatorcontrib>BROWN, George R</creatorcontrib><creatorcontrib>CAMPBELL, Douglas</creatorcontrib><creatorcontrib>FOUBISTER, Alan</creatorcontrib><creatorcontrib>MASTERS, David J</creatorcontrib><creatorcontrib>PIKE, Kurt G</creatorcontrib><creatorcontrib>SNELSON, Wendy L</creatorcontrib><creatorcontrib>WELLS, Stuart L</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>BROWN, Dearg S</au><au>BELFIELD, Andrew J</au><au>BROWN, George R</au><au>CAMPBELL, Douglas</au><au>FOUBISTER, Alan</au><au>MASTERS, David J</au><au>PIKE, Kurt G</au><au>SNELSON, Wendy L</au><au>WELLS, Stuart L</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2004-11-01</date><risdate>2004</risdate><volume>14</volume><issue>21</issue><spage>5383</spage><epage>5387</epage><pages>5383-5387</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>A novel p38 MAP kinase inhibitor structural class was discovered through selectivity screening. The rational analogue design, synthesis and structure-activity relationship of this series of bis-amide inhibitors is reported. The inhibition in vitro of human p38alpha enzyme activity and lipopolysaccharide-induced tumour necrosis factor-alpha release is described for the series. The activity in vivo and pharmacokinetic properties are exemplified for the more potent analogues.</abstract><cop>Oxford</cop><pub>Elsevier</pub><pmid>15454231</pmid><doi>10.1016/j.bmcl.2004.08.006</doi><tpages>5</tpages><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
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| ispartof | Bioorganic & medicinal chemistry letters, 2004-11, Vol.14 (21), p.5383-5387 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Amides - chemical synthesis Amides - pharmacokinetics Amides - pharmacology Animals Antirheumatic Agents - chemical synthesis Antirheumatic Agents - pharmacokinetics Antirheumatic Agents - pharmacology Arthritis, Rheumatoid - drug therapy Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Humans In Vitro Techniques Leukocytes, Mononuclear - drug effects Leukocytes, Mononuclear - metabolism Lipopolysaccharides - pharmacology Medical sciences Mice Mice, Inbred BALB C p38 Mitogen-Activated Protein Kinases - antagonists & inhibitors Pharmacology. Drug treatments Rats Structure-Activity Relationship Time Factors Tumor Necrosis Factor-alpha - antagonists & inhibitors |
| title | A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis |
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