Structure–activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor
[Display omitted] A series of cyclohexylpiperazines was synthesized as potent and selective antagonists of the human MC4 receptor. Compound 14t displayed binding affinity ( K i) of 4.2 and 1100 nM at MC4R and MC3R, respectively.
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2005-07, Vol.15 (14), p.3434-3438 |
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| container_end_page | 3438 |
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| container_issue | 14 |
| container_start_page | 3434 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 15 |
| creator | Tran, Joseph A. Pontillo, Joseph Arellano, Melissa Fleck, Beth A. Tucci, Fabio C. Marinkovic, Dragan Chen, Caroline W. Saunders, John Foster, Alan C. Chen, Chen |
| description | [Display omitted]
A series of cyclohexylpiperazines was synthesized as potent and selective antagonists of the human MC4 receptor. Compound
14t displayed binding affinity (
K
i) of 4.2 and 1100
nM at MC4R and MC3R, respectively. |
| doi_str_mv | 10.1016/j.bmcl.2005.05.017 |
| format | Article |
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A series of cyclohexylpiperazines was synthesized as potent and selective antagonists of the human MC4 receptor. Compound
14t displayed binding affinity (
K
i) of 4.2 and 1100
nM at MC4R and MC3R, respectively.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2005.05.017</identifier><identifier>PMID: 15950470</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>Amides - chemistry ; Antagonist ; Binding, Competitive ; Biological and medical sciences ; Cyclohexylpiperazine ; Humans ; Medical sciences ; Melanocortin-4 receptor ; Molecular Conformation ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems ; Pharmacology. Drug treatments ; Piperidines - chemical synthesis ; Piperidines - chemistry ; Piperidines - pharmacology ; Receptor, Melanocortin, Type 3 - antagonists & inhibitors ; Receptor, Melanocortin, Type 4 - antagonists & inhibitors ; Structure-Activity Relationship</subject><ispartof>Bioorganic & medicinal chemistry letters, 2005-07, Vol.15 (14), p.3434-3438</ispartof><rights>2005 Elsevier Ltd</rights><rights>2005 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c384t-2d6932e2f8a4e3a48d792184376a61aa93252345d4990053189c818750cec77c3</citedby><cites>FETCH-LOGICAL-c384t-2d6932e2f8a4e3a48d792184376a61aa93252345d4990053189c818750cec77c3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0960894X0500572X$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27903,27904,65309</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=16903902$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/15950470$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Tran, Joseph A.</creatorcontrib><creatorcontrib>Pontillo, Joseph</creatorcontrib><creatorcontrib>Arellano, Melissa</creatorcontrib><creatorcontrib>Fleck, Beth A.</creatorcontrib><creatorcontrib>Tucci, Fabio C.</creatorcontrib><creatorcontrib>Marinkovic, Dragan</creatorcontrib><creatorcontrib>Chen, Caroline W.</creatorcontrib><creatorcontrib>Saunders, John</creatorcontrib><creatorcontrib>Foster, Alan C.</creatorcontrib><creatorcontrib>Chen, Chen</creatorcontrib><title>Structure–activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>[Display omitted]
A series of cyclohexylpiperazines was synthesized as potent and selective antagonists of the human MC4 receptor. Compound
14t displayed binding affinity (
K
i) of 4.2 and 1100
nM at MC4R and MC3R, respectively.</description><subject>Amides - chemistry</subject><subject>Antagonist</subject><subject>Binding, Competitive</subject><subject>Biological and medical sciences</subject><subject>Cyclohexylpiperazine</subject><subject>Humans</subject><subject>Medical sciences</subject><subject>Melanocortin-4 receptor</subject><subject>Molecular Conformation</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems</subject><subject>Pharmacology. Drug treatments</subject><subject>Piperidines - chemical synthesis</subject><subject>Piperidines - chemistry</subject><subject>Piperidines - pharmacology</subject><subject>Receptor, Melanocortin, Type 3 - antagonists & inhibitors</subject><subject>Receptor, Melanocortin, Type 4 - antagonists & inhibitors</subject><subject>Structure-Activity Relationship</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2005</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kc2KFDEQx4Mo7rj6Ah6kL3rrMemkOx3wIsv6AQseVPAWMtXVOzV0d9okvTg330HwAX0S087A3oQiKap-9cG_GHsu-FZw0bw-bHcjDNuK83q7mtAP2EaoRpVS8foh23DT8LI16tsFexLjgXOhuFKP2YWoTc2V5hv2-3MKC6Ql4J-fvxwkuqN0LAIOLpGf4p7mwveFKyIGwrj6cITB7_HHcZhpztGOppzYoQs03RZuKtxIHRZxfWDvKAdiDid36yeK6V-PtMdiv4wZHvOkyYMPiaZS5cGAc_LhKXvUuyHis_N_yb6-u_5y9aG8-fT-49XbmxJkq1JZdY2RFVZ96xRKp9pOm0q0SurGNcK5nKwrqepOGZNVkqI10IpW1xwQtAZ5yV6d-s7Bf18wJjtSBBzyUuiXaBttGq1klcHqBELwMQbs7RxodOFoBbfrNezBrtew6zXsakLnohfn7stuxO6-5Cx_Bl6eARfBDX1wE1C85xrDpeHr9DcnDrMWd4TBRiCcADvKiiXbefrfHn8BfsqrpA</recordid><startdate>20050715</startdate><enddate>20050715</enddate><creator>Tran, Joseph A.</creator><creator>Pontillo, Joseph</creator><creator>Arellano, Melissa</creator><creator>Fleck, Beth A.</creator><creator>Tucci, Fabio C.</creator><creator>Marinkovic, Dragan</creator><creator>Chen, Caroline W.</creator><creator>Saunders, John</creator><creator>Foster, Alan C.</creator><creator>Chen, Chen</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>20050715</creationdate><title>Structure–activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor</title><author>Tran, Joseph A. ; Pontillo, Joseph ; Arellano, Melissa ; Fleck, Beth A. ; Tucci, Fabio C. ; Marinkovic, Dragan ; Chen, Caroline W. ; Saunders, John ; Foster, Alan C. ; Chen, Chen</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c384t-2d6932e2f8a4e3a48d792184376a61aa93252345d4990053189c818750cec77c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2005</creationdate><topic>Amides - chemistry</topic><topic>Antagonist</topic><topic>Binding, Competitive</topic><topic>Biological and medical sciences</topic><topic>Cyclohexylpiperazine</topic><topic>Humans</topic><topic>Medical sciences</topic><topic>Melanocortin-4 receptor</topic><topic>Molecular Conformation</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. Neurotransmission. Receptors</topic><topic>Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems</topic><topic>Pharmacology. Drug treatments</topic><topic>Piperidines - chemical synthesis</topic><topic>Piperidines - chemistry</topic><topic>Piperidines - pharmacology</topic><topic>Receptor, Melanocortin, Type 3 - antagonists & inhibitors</topic><topic>Receptor, Melanocortin, Type 4 - antagonists & inhibitors</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Tran, Joseph A.</creatorcontrib><creatorcontrib>Pontillo, Joseph</creatorcontrib><creatorcontrib>Arellano, Melissa</creatorcontrib><creatorcontrib>Fleck, Beth A.</creatorcontrib><creatorcontrib>Tucci, Fabio C.</creatorcontrib><creatorcontrib>Marinkovic, Dragan</creatorcontrib><creatorcontrib>Chen, Caroline W.</creatorcontrib><creatorcontrib>Saunders, John</creatorcontrib><creatorcontrib>Foster, Alan C.</creatorcontrib><creatorcontrib>Chen, Chen</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>Tran, Joseph A.</au><au>Pontillo, Joseph</au><au>Arellano, Melissa</au><au>Fleck, Beth A.</au><au>Tucci, Fabio C.</au><au>Marinkovic, Dragan</au><au>Chen, Caroline W.</au><au>Saunders, John</au><au>Foster, Alan C.</au><au>Chen, Chen</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Structure–activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2005-07-15</date><risdate>2005</risdate><volume>15</volume><issue>14</issue><spage>3434</spage><epage>3438</epage><pages>3434-3438</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>[Display omitted]
A series of cyclohexylpiperazines was synthesized as potent and selective antagonists of the human MC4 receptor. Compound
14t displayed binding affinity (
K
i) of 4.2 and 1100
nM at MC4R and MC3R, respectively.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>15950470</pmid><doi>10.1016/j.bmcl.2005.05.017</doi><tpages>5</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2005-07, Vol.15 (14), p.3434-3438 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Amides - chemistry Antagonist Binding, Competitive Biological and medical sciences Cyclohexylpiperazine Humans Medical sciences Melanocortin-4 receptor Molecular Conformation Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - chemistry Piperidines - pharmacology Receptor, Melanocortin, Type 3 - antagonists & inhibitors Receptor, Melanocortin, Type 4 - antagonists & inhibitors Structure-Activity Relationship |
| title | Structure–activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor |
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