2-Aminothiazole based P2Y1 antagonists as novel antiplatelet agents
ADP receptors, P2Y1 and P2Y12 have been recognized as potential targets for antithrombotic drugs. A series of P2Y1 antagonists that contain 2-aminothiazoles as urea surrogates were discovered. Extensive SAR of the thiazole ring is described. The most potent compound 7j showed good P2Y1 binding (Ki=1...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2013-07, Vol.23 (14), p.4206-4209 |
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| container_end_page | 4209 |
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| container_issue | 14 |
| container_start_page | 4206 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 23 |
| creator | Pi, Zulan Sutton, James Lloyd, John Hua, Ji Price, Laura Wu, Qimin Chang, Ming Zheng, Joanna Rehfuss, Robert Huang, Christine S. Wexler, Ruth R. Lam, Patrick Y.S. |
| description | ADP receptors, P2Y1 and P2Y12 have been recognized as potential targets for antithrombotic drugs. A series of P2Y1 antagonists that contain 2-aminothiazoles as urea surrogates were discovered. Extensive SAR of the thiazole ring is described. The most potent compound 7j showed good P2Y1 binding (Ki=12nM), moderate antagonism of platelet aggregation (PA IC50=5.2μM) and acceptable PK in rats. |
| doi_str_mv | 10.1016/j.bmcl.2013.05.025 |
| format | Article |
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The most potent compound 7j showed good P2Y1 binding (Ki=12nM), moderate antagonism of platelet aggregation (PA IC50=5.2μM) and acceptable PK in rats.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2013.05.025</identifier><language>eng</language><publisher>Elsevier Ltd</publisher><subject>adenosine diphosphate ; Aminothiazole as urea surrogates ; Antagonism ; antagonists ; Antithrombotic ; chemistry ; drugs ; P2Y1 antagonists ; Platelet aggregation ; rats ; receptors ; urea</subject><ispartof>Bioorganic & medicinal chemistry letters, 2013-07, Vol.23 (14), p.4206-4209</ispartof><rights>2013 Elsevier Ltd</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c272t-7128a3a8981887521c85e2a054f5647ec1d7798ed551781021ae1e1e8a81fc293</citedby><cites>FETCH-LOGICAL-c272t-7128a3a8981887521c85e2a054f5647ec1d7798ed551781021ae1e1e8a81fc293</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0960894X13006112$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids></links><search><creatorcontrib>Pi, Zulan</creatorcontrib><creatorcontrib>Sutton, James</creatorcontrib><creatorcontrib>Lloyd, John</creatorcontrib><creatorcontrib>Hua, Ji</creatorcontrib><creatorcontrib>Price, Laura</creatorcontrib><creatorcontrib>Wu, Qimin</creatorcontrib><creatorcontrib>Chang, Ming</creatorcontrib><creatorcontrib>Zheng, Joanna</creatorcontrib><creatorcontrib>Rehfuss, Robert</creatorcontrib><creatorcontrib>Huang, Christine S.</creatorcontrib><creatorcontrib>Wexler, Ruth R.</creatorcontrib><creatorcontrib>Lam, Patrick Y.S.</creatorcontrib><title>2-Aminothiazole based P2Y1 antagonists as novel antiplatelet agents</title><title>Bioorganic & medicinal chemistry letters</title><description>ADP receptors, P2Y1 and P2Y12 have been recognized as potential targets for antithrombotic drugs. A series of P2Y1 antagonists that contain 2-aminothiazoles as urea surrogates were discovered. Extensive SAR of the thiazole ring is described. The most potent compound 7j showed good P2Y1 binding (Ki=12nM), moderate antagonism of platelet aggregation (PA IC50=5.2μM) and acceptable PK in rats.</description><subject>adenosine diphosphate</subject><subject>Aminothiazole as urea surrogates</subject><subject>Antagonism</subject><subject>antagonists</subject><subject>Antithrombotic</subject><subject>chemistry</subject><subject>drugs</subject><subject>P2Y1 antagonists</subject><subject>Platelet aggregation</subject><subject>rats</subject><subject>receptors</subject><subject>urea</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2013</creationdate><recordtype>article</recordtype><recordid>eNp9kEFr3DAQhUVJoJu0f6CX-tiLnRlZsmXoJSxJGwgk0ATSk5jI460W29pY2oX019fu5hzmMDB8783ME-ILQoGA1cW2eB5cX0jAsgBdgNQfxApVpfJSgT4RK2gqyE2jnj6Ksxi3AKhAqZVYy_xy8GNIfzz9DT1nzxS5ze7lb8xoTLQJo48pZhSzMRy4X4Z-11PinlNGGx5T_CROO-ojf37r5-Lx-uph_TO_vftxs768zZ2sZcprlIZKMo1BY2ot0RnNkkCrTleqZodtXTeGW62xNggSiXEuQwY7J5vyXHw7-u6m8LLnmOzgo-O-p5HDPlrUALWuGqlnVB5RN4UYJ-7sbvIDTa8WwS6J2a1dErNLYha0hf-ir0dRR8HSZvLRPv6agdkWSynVcsH3I8HzmwfPk43O8-i49RO7ZNvg31vwD2zPe9g</recordid><startdate>20130715</startdate><enddate>20130715</enddate><creator>Pi, Zulan</creator><creator>Sutton, James</creator><creator>Lloyd, John</creator><creator>Hua, Ji</creator><creator>Price, Laura</creator><creator>Wu, Qimin</creator><creator>Chang, Ming</creator><creator>Zheng, Joanna</creator><creator>Rehfuss, Robert</creator><creator>Huang, Christine S.</creator><creator>Wexler, Ruth R.</creator><creator>Lam, Patrick Y.S.</creator><general>Elsevier Ltd</general><scope>FBQ</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope></search><sort><creationdate>20130715</creationdate><title>2-Aminothiazole based P2Y1 antagonists as novel antiplatelet agents</title><author>Pi, Zulan ; Sutton, James ; Lloyd, John ; Hua, Ji ; Price, Laura ; Wu, Qimin ; Chang, Ming ; Zheng, Joanna ; Rehfuss, Robert ; Huang, Christine S. ; Wexler, Ruth R. ; Lam, Patrick Y.S.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c272t-7128a3a8981887521c85e2a054f5647ec1d7798ed551781021ae1e1e8a81fc293</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2013</creationdate><topic>adenosine diphosphate</topic><topic>Aminothiazole as urea surrogates</topic><topic>Antagonism</topic><topic>antagonists</topic><topic>Antithrombotic</topic><topic>chemistry</topic><topic>drugs</topic><topic>P2Y1 antagonists</topic><topic>Platelet aggregation</topic><topic>rats</topic><topic>receptors</topic><topic>urea</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Pi, Zulan</creatorcontrib><creatorcontrib>Sutton, James</creatorcontrib><creatorcontrib>Lloyd, John</creatorcontrib><creatorcontrib>Hua, Ji</creatorcontrib><creatorcontrib>Price, Laura</creatorcontrib><creatorcontrib>Wu, Qimin</creatorcontrib><creatorcontrib>Chang, Ming</creatorcontrib><creatorcontrib>Zheng, Joanna</creatorcontrib><creatorcontrib>Rehfuss, Robert</creatorcontrib><creatorcontrib>Huang, Christine S.</creatorcontrib><creatorcontrib>Wexler, Ruth R.</creatorcontrib><creatorcontrib>Lam, Patrick Y.S.</creatorcontrib><collection>AGRIS</collection><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Pi, Zulan</au><au>Sutton, James</au><au>Lloyd, John</au><au>Hua, Ji</au><au>Price, Laura</au><au>Wu, Qimin</au><au>Chang, Ming</au><au>Zheng, Joanna</au><au>Rehfuss, Robert</au><au>Huang, Christine S.</au><au>Wexler, Ruth R.</au><au>Lam, Patrick Y.S.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>2-Aminothiazole based P2Y1 antagonists as novel antiplatelet agents</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><date>2013-07-15</date><risdate>2013</risdate><volume>23</volume><issue>14</issue><spage>4206</spage><epage>4209</epage><pages>4206-4209</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>ADP receptors, P2Y1 and P2Y12 have been recognized as potential targets for antithrombotic drugs. A series of P2Y1 antagonists that contain 2-aminothiazoles as urea surrogates were discovered. Extensive SAR of the thiazole ring is described. The most potent compound 7j showed good P2Y1 binding (Ki=12nM), moderate antagonism of platelet aggregation (PA IC50=5.2μM) and acceptable PK in rats.</abstract><pub>Elsevier Ltd</pub><doi>10.1016/j.bmcl.2013.05.025</doi><tpages>4</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2013-07, Vol.23 (14), p.4206-4209 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | Elsevier ScienceDirect Journals |
| subjects | adenosine diphosphate Aminothiazole as urea surrogates Antagonism antagonists Antithrombotic chemistry drugs P2Y1 antagonists Platelet aggregation rats receptors urea |
| title | 2-Aminothiazole based P2Y1 antagonists as novel antiplatelet agents |
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