Synthesis and biological activity of fluoro-substituted pyrrolo[2,3-d]pyrimidines: The development of potential positron emission tomography imaging agents for the corticotropin-releasing hormone type 1 receptor
A series of fluoro-substituted 4-(dialkylamino)pyrrolo[2,3-d]pyrimidines was synthesized and their binding affinity for corticotropin-releasing hormone type 1 receptor (CRHR1) was investigated. Compounds 11a and 11b possessed very high CRHR1 affinity (Ki=3.5, 0.91 nM, respectively). They are promisi...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2000-04, Vol.10 (8), p.707-710 |
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| container_title | Bioorganic & medicinal chemistry letters |
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| creator | HSIN, L.-W WEBSTER, E. L CHROUSOS, G. P GOLD, P. W ECKELMAN, W. C CONTOREGGI, C RICE, K. C |
| description | A series of fluoro-substituted 4-(dialkylamino)pyrrolo[2,3-d]pyrimidines was synthesized and their binding affinity for corticotropin-releasing hormone type 1 receptor (CRHR1) was investigated. Compounds 11a and 11b possessed very high CRHR1 affinity (Ki=3.5, 0.91 nM, respectively). They are promising candidates for the development of 18F-containing nonpeptide PET radioligands for CRHR1. |
| doi_str_mv | 10.1016/s0960-894x(00)00071-8 |
| format | Article |
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They are promising candidates for the development of 18F-containing nonpeptide PET radioligands for CRHR1.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/s0960-894x(00)00071-8</identifier><identifier>PMID: 10782669</identifier><language>eng</language><publisher>Oxford: Elsevier</publisher><subject>Animals ; Biological and medical sciences ; Cerebellum - metabolism ; Contrast Media - chemical synthesis ; Contrast Media - metabolism ; Contrast Media - pharmacology ; Fluorine - chemistry ; Medical sciences ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems ; Pharmacology. Drug treatments ; Pyrimidines - chemical synthesis ; Pyrimidines - metabolism ; Pyrimidines - pharmacology ; Pyrroles - chemistry ; Radioligand Assay ; Rats ; Receptors, Corticotropin-Releasing Hormone - metabolism ; Tomography, Emission-Computed</subject><ispartof>Bioorganic & medicinal chemistry letters, 2000-04, Vol.10 (8), p.707-710</ispartof><rights>2000 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c400t-e274970251e2f39e49213a412662d81def6e496bf02a834db311660542a637ab3</citedby><cites>FETCH-LOGICAL-c400t-e274970251e2f39e49213a412662d81def6e496bf02a834db311660542a637ab3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27901,27902</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1341358$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/10782669$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>HSIN, L.-W</creatorcontrib><creatorcontrib>WEBSTER, E. 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They are promising candidates for the development of 18F-containing nonpeptide PET radioligands for CRHR1.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Cerebellum - metabolism</subject><subject>Contrast Media - chemical synthesis</subject><subject>Contrast Media - metabolism</subject><subject>Contrast Media - pharmacology</subject><subject>Fluorine - chemistry</subject><subject>Medical sciences</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>Pyrimidines - chemical synthesis</subject><subject>Pyrimidines - metabolism</subject><subject>Pyrimidines - pharmacology</subject><subject>Pyrroles - chemistry</subject><subject>Radioligand Assay</subject><subject>Rats</subject><subject>Receptors, Corticotropin-Releasing Hormone - metabolism</subject><subject>Tomography, Emission-Computed</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2000</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpNkduK1TAUhoMoznb0EZRciChYXTk0bb2TwRMMeDEjCCIlbVf3jrRJJkkH-5y-kKl7i15lJXz_SrI-Qh4zeMWAqdcRGgVF3cifzwFeAEDFivoO2TGpZCEklHfJ7i_y9Yw8iPEHAJMg5X1yxqCquVLNjvy6Wm06YDSRajvQzrjJ7U2vJ6r7ZG5NWqkb6TgtLrgiLl1MJi0JB-rXEDL7jb8UxfA978xsBmMxvqHXB6QD3uLk_Iw2bQ28S7kyua130aTgLMXZxGhykdzs9kH7w0rNrPfG7qneZzrS0QWaH0d7F5LpXY55Y4uAE-q4YQcXZmeRptUjZTRgjz658JDcG_UU8dFpPSdf3r-7vvhYXH7-8Oni7WXRS4BUIK9kUwEvGfJRNCgbzoSWLA-GDzUbcFT5THUjcF0LOXSCMaWglFwrUelOnJNnx74-uJsFY2rzl3qcJm3RLbGtGJQ8hzJYHsE-uBgDjq3P49JhbRm0m832alPVbqpagPaPzbbOuSenC5ZuxuG_1FFfBp6eAB2zszFo25v4jxOSibIWvwFMJa55</recordid><startdate>20000417</startdate><enddate>20000417</enddate><creator>HSIN, L.-W</creator><creator>WEBSTER, E. 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Drug treatments</topic><topic>Pyrimidines - chemical synthesis</topic><topic>Pyrimidines - metabolism</topic><topic>Pyrimidines - pharmacology</topic><topic>Pyrroles - chemistry</topic><topic>Radioligand Assay</topic><topic>Rats</topic><topic>Receptors, Corticotropin-Releasing Hormone - metabolism</topic><topic>Tomography, Emission-Computed</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>HSIN, L.-W</creatorcontrib><creatorcontrib>WEBSTER, E. L</creatorcontrib><creatorcontrib>CHROUSOS, G. P</creatorcontrib><creatorcontrib>GOLD, P. W</creatorcontrib><creatorcontrib>ECKELMAN, W. C</creatorcontrib><creatorcontrib>CONTOREGGI, C</creatorcontrib><creatorcontrib>RICE, K. 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| subjects | Animals Biological and medical sciences Cerebellum - metabolism Contrast Media - chemical synthesis Contrast Media - metabolism Contrast Media - pharmacology Fluorine - chemistry Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Pyrimidines - chemical synthesis Pyrimidines - metabolism Pyrimidines - pharmacology Pyrroles - chemistry Radioligand Assay Rats Receptors, Corticotropin-Releasing Hormone - metabolism Tomography, Emission-Computed |
| title | Synthesis and biological activity of fluoro-substituted pyrrolo[2,3-d]pyrimidines: The development of potential positron emission tomography imaging agents for the corticotropin-releasing hormone type 1 receptor |
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