Discovery of 5-Arylsulfonamido-3- (pyrrolidin-2-ylmethyl)-1H-indole Derivatives as Potent, Selective 5-HT6 Receptor Agonists and Antagonists
5-Arylsulfonylamido-3-(pyrrolidin-2-ylmethyl)-1H-indoles have been identified as high-affinity 5-HT6 receptor ligands. Within this class, several of the (R)-enantiomers were potent agonists having EC50 values of 1 nM or less and functioning as full agonists while the (S)-enantiomers displayed modera...
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| Veröffentlicht in: | Journal of medicinal chemistry 2005-01, Vol.48 (2), p.353-356 |
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| container_end_page | 356 |
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| container_issue | 2 |
| container_start_page | 353 |
| container_title | Journal of medicinal chemistry |
| container_volume | 48 |
| creator | Cole, Derek C Lennox, William J Lombardi, Sabrina Ellingboe, John W Bernotas, Ronald C Tawa, Gregory J Mazandarani, Hossein Smith, Deborah L Zhang, Guoming Coupet, Joseph Schechter, Lee E |
| description | 5-Arylsulfonylamido-3-(pyrrolidin-2-ylmethyl)-1H-indoles have been identified as high-affinity 5-HT6 receptor ligands. Within this class, several of the (R)-enantiomers were potent agonists having EC50 values of 1 nM or less and functioning as full agonists while the (S)-enantiomers displayed moderate antagonist activity. |
| doi_str_mv | 10.1021/jm049243i |
| format | Article |
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Within this class, several of the (R)-enantiomers were potent agonists having EC50 values of 1 nM or less and functioning as full agonists while the (S)-enantiomers displayed moderate antagonist activity.</description><subject>Cyclic AMP - agonists</subject><subject>Cyclic AMP - antagonists & inhibitors</subject><subject>Cyclic AMP - biosynthesis</subject><subject>HeLa Cells</subject><subject>Humans</subject><subject>Indoles - chemical synthesis</subject><subject>Indoles - chemistry</subject><subject>Indoles - pharmacology</subject><subject>Pyrrolidines - chemical synthesis</subject><subject>Pyrrolidines - chemistry</subject><subject>Pyrrolidines - pharmacology</subject><subject>Receptors, Serotonin - drug effects</subject><subject>Stereoisomerism</subject><subject>Structure-Activity Relationship</subject><subject>Sulfonamides - chemical synthesis</subject><subject>Sulfonamides - chemistry</subject><subject>Sulfonamides - pharmacology</subject><issn>0022-2623</issn><issn>1520-4804</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2005</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo9kdtuEzEQhi0EoqHlghdAvgGBhMGHPXgvox5I1dJWNAjuLMc7C06962B7I_YdeGgcJfRqTp9-zfyD0CtGPzLK2ad1T4uGF8I-QTNWckoKSYunaEYp54RXXByhFzGuKaWCcfEcHbGyKqUs5Az9PbPR-C2ECfsOl2QeJhdH1_lB97b1RBD8bjOF4J1t7UA4mVwP6dfk3hO2IHZovQN8BsFudbJbiFhHfOcTDOkDvgcHZtfNuotlhb-CgU3yAc9_-sHGlOGhxfMh6UN9gp512kV4eYjH6NvF-fJ0Qa5vP1-ezq-J5nWdiC5ygK5jQsvGSGYkrERVUFMJvqqhgUaIoqvaTvOighpWIPPl1Ggp2pwZcYze7nU3wf8eISbVZxfAOT2AH6OqalE2lMoMvj6A46qHVm2C7XWY1H__MkD2QF4f_jzOdXjYidSlWt7dK_rlpiq_31ypH5l_s-e1iWrtxzDkOxWjavdH9fhH8Q9iiozz</recordid><startdate>20050127</startdate><enddate>20050127</enddate><creator>Cole, Derek C</creator><creator>Lennox, William J</creator><creator>Lombardi, Sabrina</creator><creator>Ellingboe, John W</creator><creator>Bernotas, Ronald C</creator><creator>Tawa, Gregory J</creator><creator>Mazandarani, Hossein</creator><creator>Smith, Deborah L</creator><creator>Zhang, Guoming</creator><creator>Coupet, Joseph</creator><creator>Schechter, Lee E</creator><general>American Chemical Society</general><scope>BSCLL</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>20050127</creationdate><title>Discovery of 5-Arylsulfonamido-3- (pyrrolidin-2-ylmethyl)-1H-indole Derivatives as Potent, Selective 5-HT6 Receptor Agonists and Antagonists</title><author>Cole, Derek C ; 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Med. Chem</addtitle><date>2005-01-27</date><risdate>2005</risdate><volume>48</volume><issue>2</issue><spage>353</spage><epage>356</epage><pages>353-356</pages><issn>0022-2623</issn><eissn>1520-4804</eissn><abstract>5-Arylsulfonylamido-3-(pyrrolidin-2-ylmethyl)-1H-indoles have been identified as high-affinity 5-HT6 receptor ligands. Within this class, several of the (R)-enantiomers were potent agonists having EC50 values of 1 nM or less and functioning as full agonists while the (S)-enantiomers displayed moderate antagonist activity.</abstract><cop>United States</cop><pub>American Chemical Society</pub><pmid>15658848</pmid><doi>10.1021/jm049243i</doi><tpages>4</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0022-2623 |
| ispartof | Journal of medicinal chemistry, 2005-01, Vol.48 (2), p.353-356 |
| issn | 0022-2623 1520-4804 |
| language | eng |
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| source | ACS Publications; MEDLINE |
| subjects | Cyclic AMP - agonists Cyclic AMP - antagonists & inhibitors Cyclic AMP - biosynthesis HeLa Cells Humans Indoles - chemical synthesis Indoles - chemistry Indoles - pharmacology Pyrrolidines - chemical synthesis Pyrrolidines - chemistry Pyrrolidines - pharmacology Receptors, Serotonin - drug effects Stereoisomerism Structure-Activity Relationship Sulfonamides - chemical synthesis Sulfonamides - chemistry Sulfonamides - pharmacology |
| title | Discovery of 5-Arylsulfonamido-3- (pyrrolidin-2-ylmethyl)-1H-indole Derivatives as Potent, Selective 5-HT6 Receptor Agonists and Antagonists |
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