Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules
We sought to design dual pharmacology bronchodilators targeting both the M 3 muscarinic acetylcholine and beta-2 adrenergic (β 2) receptors by applying our multivalent approach to drug discovery. Herein, we describe our initial discovery and the SAR of the first such compounds with matched potencies...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2011-03, Vol.21 (5), p.1354-1358 |
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| container_end_page | 1358 |
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| container_issue | 5 |
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| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 21 |
| creator | Hughes, Adam D. Chin, Kay H. Dunham, Sarah L. Jasper, Jeffrey R. King, Kristin E. Lee, Tae Weon Mammen, Mathai Martin, Jerri Steinfeld, Tod |
| description | We sought to design dual pharmacology bronchodilators targeting both the M
3 muscarinic acetylcholine and beta-2 adrenergic (β
2) receptors by applying our multivalent approach to drug discovery. Herein, we describe our initial discovery and the SAR of the first such compounds with matched potencies at both receptors. |
| doi_str_mv | 10.1016/j.bmcl.2011.01.043 |
| format | Article |
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3 muscarinic acetylcholine and beta-2 adrenergic (β
2) receptors by applying our multivalent approach to drug discovery. Herein, we describe our initial discovery and the SAR of the first such compounds with matched potencies at both receptors.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2011.01.043</identifier><identifier>PMID: 21310610</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>acetylcholine ; Adrenergic beta-2 Receptor Agonists - chemical synthesis ; Adrenergic beta-2 Receptor Agonists - chemistry ; Adrenergic beta-2 Receptor Agonists - pharmacology ; agonists ; antagonists ; Beta 2 adrenoceptor agonist ; Biological and medical sciences ; Bronchodilator ; Bronchodilator Agents - chemical synthesis ; Bronchodilator Agents - chemistry ; Bronchodilator Agents - pharmacology ; bronchodilators ; Catecholaminergic system ; chemistry ; Cholinergic system ; COPD ; Drug Design ; Dual pharmacology ; Humans ; Inhaled ; LABA ; LAMA ; MABA ; Medical sciences ; Molecular Structure ; Multivalent approach ; Muscarinic acetylcholine receptor antagonist ; Muscarinic Antagonists - chemical synthesis ; Muscarinic Antagonists - chemistry ; Muscarinic Antagonists - pharmacology ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; pharmacology ; Pharmacology. Drug treatments ; receptors ; Receptors, Adrenergic, beta-2 - chemistry ; Receptors, Muscarinic - chemistry ; Respiratory system ; Structure-Activity Relationship</subject><ispartof>Bioorganic & medicinal chemistry letters, 2011-03, Vol.21 (5), p.1354-1358</ispartof><rights>2011</rights><rights>2015 INIST-CNRS</rights><rights>Copyright © 2011. Published by Elsevier Ltd.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c441t-fadeeda0caa97c105a24da6bd2581453496cfe85d6c8c06e0644f0dbfb39f973</citedby><cites>FETCH-LOGICAL-c441t-fadeeda0caa97c105a24da6bd2581453496cfe85d6c8c06e0644f0dbfb39f973</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmcl.2011.01.043$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=23919103$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/21310610$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Hughes, Adam D.</creatorcontrib><creatorcontrib>Chin, Kay H.</creatorcontrib><creatorcontrib>Dunham, Sarah L.</creatorcontrib><creatorcontrib>Jasper, Jeffrey R.</creatorcontrib><creatorcontrib>King, Kristin E.</creatorcontrib><creatorcontrib>Lee, Tae Weon</creatorcontrib><creatorcontrib>Mammen, Mathai</creatorcontrib><creatorcontrib>Martin, Jerri</creatorcontrib><creatorcontrib>Steinfeld, Tod</creatorcontrib><title>Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>We sought to design dual pharmacology bronchodilators targeting both the M
3 muscarinic acetylcholine and beta-2 adrenergic (β
2) receptors by applying our multivalent approach to drug discovery. Herein, we describe our initial discovery and the SAR of the first such compounds with matched potencies at both receptors.</description><subject>acetylcholine</subject><subject>Adrenergic beta-2 Receptor Agonists - chemical synthesis</subject><subject>Adrenergic beta-2 Receptor Agonists - chemistry</subject><subject>Adrenergic beta-2 Receptor Agonists - pharmacology</subject><subject>agonists</subject><subject>antagonists</subject><subject>Beta 2 adrenoceptor agonist</subject><subject>Biological and medical sciences</subject><subject>Bronchodilator</subject><subject>Bronchodilator Agents - chemical synthesis</subject><subject>Bronchodilator Agents - chemistry</subject><subject>Bronchodilator Agents - pharmacology</subject><subject>bronchodilators</subject><subject>Catecholaminergic system</subject><subject>chemistry</subject><subject>Cholinergic system</subject><subject>COPD</subject><subject>Drug Design</subject><subject>Dual pharmacology</subject><subject>Humans</subject><subject>Inhaled</subject><subject>LABA</subject><subject>LAMA</subject><subject>MABA</subject><subject>Medical sciences</subject><subject>Molecular Structure</subject><subject>Multivalent approach</subject><subject>Muscarinic acetylcholine receptor antagonist</subject><subject>Muscarinic Antagonists - chemical synthesis</subject><subject>Muscarinic Antagonists - chemistry</subject><subject>Muscarinic Antagonists - pharmacology</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>pharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>receptors</subject><subject>Receptors, Adrenergic, beta-2 - chemistry</subject><subject>Receptors, Muscarinic - chemistry</subject><subject>Respiratory system</subject><subject>Structure-Activity Relationship</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2011</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkU2LFDEQhhtR3HH1D3jQXEQ99FjppHu6wcu4fsKKB1fwFqqTymyGdGc26V4Y8MebYWb1plCQQJ56K8lTFE85LDnw5s122Q_aLyvgfAm5pLhXLLhsZCkk1PeLBXQNlG0nf54Vj1LaAnAJUj4sziouODQcFsWv9y7pcEtxz4Jlw5w0Rjc6zVDTtPf6Ong3EoukaTeFyHCccBNGl6a8NaynCVnF0EQawx1yOn_1df1u_ZqZGT3bXWMcUAcfNns2BE969pQeFw8s-kRPTut5cfXxw9XF5_Ly26cvF-vLUkvJp9KiITIIGrFbaQ41VtJg05uqbrmshewabamtTaNbDQ1BI6UF09tedLZbifPi5TF2F8PNTGlSQ340eY8jhTmpDla8boG3_yXbWlRV1XaQyepI6hhSimTVLroB415xUAc7aqsOdtTBjoJcUuSmZ6f4uR_I_Gm505GBFycAswhvI47apb-c6HiXscw9P3IWg8JNzMyP73lSnRULKeUh6e2RoPyvt46iStrRqMm47HJSJrh_3fQ3hu-4qQ</recordid><startdate>20110301</startdate><enddate>20110301</enddate><creator>Hughes, Adam D.</creator><creator>Chin, Kay H.</creator><creator>Dunham, Sarah L.</creator><creator>Jasper, Jeffrey R.</creator><creator>King, Kristin E.</creator><creator>Lee, Tae Weon</creator><creator>Mammen, Mathai</creator><creator>Martin, Jerri</creator><creator>Steinfeld, Tod</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>FBQ</scope><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><scope>7QO</scope><scope>7TK</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope></search><sort><creationdate>20110301</creationdate><title>Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules</title><author>Hughes, Adam D. ; Chin, Kay H. ; Dunham, Sarah L. ; Jasper, Jeffrey R. ; King, Kristin E. ; Lee, Tae Weon ; Mammen, Mathai ; Martin, Jerri ; Steinfeld, Tod</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c441t-fadeeda0caa97c105a24da6bd2581453496cfe85d6c8c06e0644f0dbfb39f973</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2011</creationdate><topic>acetylcholine</topic><topic>Adrenergic beta-2 Receptor Agonists - chemical synthesis</topic><topic>Adrenergic beta-2 Receptor Agonists - chemistry</topic><topic>Adrenergic beta-2 Receptor Agonists - pharmacology</topic><topic>agonists</topic><topic>antagonists</topic><topic>Beta 2 adrenoceptor agonist</topic><topic>Biological and medical sciences</topic><topic>Bronchodilator</topic><topic>Bronchodilator Agents - chemical synthesis</topic><topic>Bronchodilator Agents - chemistry</topic><topic>Bronchodilator Agents - pharmacology</topic><topic>bronchodilators</topic><topic>Catecholaminergic system</topic><topic>chemistry</topic><topic>Cholinergic system</topic><topic>COPD</topic><topic>Drug Design</topic><topic>Dual pharmacology</topic><topic>Humans</topic><topic>Inhaled</topic><topic>LABA</topic><topic>LAMA</topic><topic>MABA</topic><topic>Medical sciences</topic><topic>Molecular Structure</topic><topic>Multivalent approach</topic><topic>Muscarinic acetylcholine receptor antagonist</topic><topic>Muscarinic Antagonists - chemical synthesis</topic><topic>Muscarinic Antagonists - chemistry</topic><topic>Muscarinic Antagonists - pharmacology</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. Neurotransmission. Receptors</topic><topic>pharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>receptors</topic><topic>Receptors, Adrenergic, beta-2 - chemistry</topic><topic>Receptors, Muscarinic - chemistry</topic><topic>Respiratory system</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Hughes, Adam D.</creatorcontrib><creatorcontrib>Chin, Kay H.</creatorcontrib><creatorcontrib>Dunham, Sarah L.</creatorcontrib><creatorcontrib>Jasper, Jeffrey R.</creatorcontrib><creatorcontrib>King, Kristin E.</creatorcontrib><creatorcontrib>Lee, Tae Weon</creatorcontrib><creatorcontrib>Mammen, Mathai</creatorcontrib><creatorcontrib>Martin, Jerri</creatorcontrib><creatorcontrib>Steinfeld, Tod</creatorcontrib><collection>AGRIS</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>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>Biotechnology Research Abstracts</collection><collection>Neurosciences 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>Hughes, Adam D.</au><au>Chin, Kay H.</au><au>Dunham, Sarah L.</au><au>Jasper, Jeffrey R.</au><au>King, Kristin E.</au><au>Lee, Tae Weon</au><au>Mammen, Mathai</au><au>Martin, Jerri</au><au>Steinfeld, Tod</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2011-03-01</date><risdate>2011</risdate><volume>21</volume><issue>5</issue><spage>1354</spage><epage>1358</epage><pages>1354-1358</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>We sought to design dual pharmacology bronchodilators targeting both the M
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2) receptors by applying our multivalent approach to drug discovery. Herein, we describe our initial discovery and the SAR of the first such compounds with matched potencies at both receptors.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>21310610</pmid><doi>10.1016/j.bmcl.2011.01.043</doi><tpages>5</tpages></addata></record> |
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| ispartof | Bioorganic & medicinal chemistry letters, 2011-03, Vol.21 (5), p.1354-1358 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | acetylcholine Adrenergic beta-2 Receptor Agonists - chemical synthesis Adrenergic beta-2 Receptor Agonists - chemistry Adrenergic beta-2 Receptor Agonists - pharmacology agonists antagonists Beta 2 adrenoceptor agonist Biological and medical sciences Bronchodilator Bronchodilator Agents - chemical synthesis Bronchodilator Agents - chemistry Bronchodilator Agents - pharmacology bronchodilators Catecholaminergic system chemistry Cholinergic system COPD Drug Design Dual pharmacology Humans Inhaled LABA LAMA MABA Medical sciences Molecular Structure Multivalent approach Muscarinic acetylcholine receptor antagonist Muscarinic Antagonists - chemical synthesis Muscarinic Antagonists - chemistry Muscarinic Antagonists - pharmacology Neuropharmacology Neurotransmitters. Neurotransmission. Receptors pharmacology Pharmacology. Drug treatments receptors Receptors, Adrenergic, beta-2 - chemistry Receptors, Muscarinic - chemistry Respiratory system Structure-Activity Relationship |
| title | Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules |
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