Discovery and evaluation of N-(triazin-1,3,5-yl) phenylalanine derivatives as VLA-4 integrin antagonists
SAR studies aimed at improving the rate of clearance of a series of VLA-4 integrin antagonists by the introduction of a 1,3,5-triazine as an amide isostere are described. A series of triazinyl derivatives, such as 4, that block the interaction of VLA-4 integrin with VCAM-1 are described.
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2002-06, Vol.12 (12), p.1591-1594 |
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| container_end_page | 1594 |
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| container_issue | 12 |
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| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 12 |
| creator | Porter, John R. Archibald, Sarah C. Brown, Julien A. Childs, Kirstie Critchley, David Head, John C. Hutchinson, Brian Parton, Ted A.H. Robinson, Martyn K. Shock, Anthony Warrellow, Graham J. Zomaya, Alex |
| description | SAR studies aimed at improving the rate of clearance of a series of VLA-4 integrin antagonists by the introduction of a 1,3,5-triazine as an amide isostere are described.
A series of triazinyl derivatives, such as
4, that block the interaction of VLA-4 integrin with VCAM-1 are described. |
| doi_str_mv | 10.1016/S0960-894X(02)00237-8 |
| format | Article |
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A series of triazinyl derivatives, such as
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Drug treatments</subject><subject>Phenylalanine - analogs & derivatives</subject><subject>Phenylalanine - chemistry</subject><subject>Phenylalanine - pharmacology</subject><subject>Structure-Activity Relationship</subject><subject>Triazines - chemistry</subject><subject>Triazines - pharmacology</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2002</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1vEzEQhi0EoqHwE0C-gFqphvH6a31CVfmUIjhQIW6W451tjTbe1N6sFH49ThPRI6e5PO_MvA8hLzm85cD1ux9gNbDWyl9n0JwDNMKw9hFZcKklExLUY7L4h5yQZ6X8BuASpHxKTngDwiptF-T2QyxhnDHvqE8dxdkPWz_FMdGxp9_Y2ZSj_xMT4xfiQrHdcE43t5h2gx98iglphznONTBjob7Qn8tLJmlME97kmOrKyd-MKZapPCdPej8UfHGcp-T608frqy9s-f3z16vLJQvC8onx0PSdwaAliJVRbYceOfamtUYE7LSy0DdN8Mq0WvF2Fcyq08DBcgsNKnFK3hzWbvJ4t8UyuXUtiEN9F8dtcYYbXdu3FVQHMOSxlIy92-S49nnnOLi9YXdv2O31OWjcvWG3z706Htiu1tg9pI5KK_D6CPgS_NBnn0IsD5zQRksuK_f-wGG1MUfMroSIqZaMGcPkujH-55W_lhqX3A</recordid><startdate>20020617</startdate><enddate>20020617</enddate><creator>Porter, John R.</creator><creator>Archibald, Sarah C.</creator><creator>Brown, Julien A.</creator><creator>Childs, Kirstie</creator><creator>Critchley, David</creator><creator>Head, John C.</creator><creator>Hutchinson, Brian</creator><creator>Parton, Ted A.H.</creator><creator>Robinson, Martyn K.</creator><creator>Shock, Anthony</creator><creator>Warrellow, Graham J.</creator><creator>Zomaya, Alex</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>20020617</creationdate><title>Discovery and evaluation of N-(triazin-1,3,5-yl) phenylalanine derivatives as VLA-4 integrin antagonists</title><author>Porter, John R. ; Archibald, Sarah C. ; Brown, Julien A. ; Childs, Kirstie ; Critchley, David ; Head, John C. ; Hutchinson, Brian ; Parton, Ted A.H. ; Robinson, Martyn K. ; Shock, Anthony ; Warrellow, Graham J. ; Zomaya, Alex</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c391t-1c2fd7ec6403b758deae1ef78973ced6590f22ca5786518bc7bd601091902e53</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2002</creationdate><topic>Biological and medical sciences</topic><topic>Bones, joints and connective tissue. 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| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2002-06, Vol.12 (12), p.1591-1594 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Integrin alpha4beta1 - antagonists & inhibitors Medical sciences Pharmacology. Drug treatments Phenylalanine - analogs & derivatives Phenylalanine - chemistry Phenylalanine - pharmacology Structure-Activity Relationship Triazines - chemistry Triazines - pharmacology |
| title | Discovery and evaluation of N-(triazin-1,3,5-yl) phenylalanine derivatives as VLA-4 integrin antagonists |
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