Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists
A series of 3-phenylpyrazolo[1,5- a]pyrimidines was prepared and found to have affinity for the human CRF-1 receptor. The 3-dimensional structure of one of the most potent analogs in this series, 10d, was determined by X-ray crystallography and suggests the spatial requirements for potent CRF-1 rece...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 1998-08, Vol.8 (16), p.2067-2070 |
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| container_title | Bioorganic & medicinal chemistry letters |
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| creator | Wustrow, David J. Capiris, Thomas Rubin, Ronald Knobelsdorf, James A. Akunne, Hyacinth Davis, M.Duff MacKenzie, Robert Pugsley, Thomas A. Zoski, Kim T. Heffner, Thomas G. Wise, Lawrence D. |
| description | A series of 3-phenylpyrazolo[1,5-
a]pyrimidines was prepared and found to have affinity for the human CRF-1 receptor. The 3-dimensional structure of one of the most potent analogs in this series,
10d, was determined by X-ray crystallography and suggests the spatial requirements for potent CRF-1 receptor binding affinity in this series.
A series of 3-phenylpyrazolo[1,5-a]pyrimidines was prepared and found to have affinity for the human CRF-1 receptor. The X-ray structure of one of the most potent analogs suggests the spatial requirements for potent CRF-1 receptor binding affinity in this series. |
| doi_str_mv | 10.1016/S0960-894X(98)00372-2 |
| format | Article |
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a]pyrimidines was prepared and found to have affinity for the human CRF-1 receptor. The 3-dimensional structure of one of the most potent analogs in this series,
10d, was determined by X-ray crystallography and suggests the spatial requirements for potent CRF-1 receptor binding affinity in this series.
A series of 3-phenylpyrazolo[1,5-a]pyrimidines was prepared and found to have affinity for the human CRF-1 receptor. The X-ray structure of one of the most potent analogs suggests the spatial requirements for potent CRF-1 receptor binding affinity in this series.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/S0960-894X(98)00372-2</identifier><identifier>PMID: 9873487</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>Biological and medical sciences ; Corticotropin-Releasing Hormone - antagonists & inhibitors ; Crystallography, X-Ray ; Drug Design ; Humans ; Kinetics ; Medical sciences ; Models, Molecular ; Molecular Conformation ; Molecular Structure ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems ; Pharmacology. Drug treatments ; Pyrazoles - chemical synthesis ; Pyrazoles - chemistry ; Pyrazoles - pharmacology ; Pyrimidines - chemical synthesis ; Pyrimidines - chemistry ; Pyrimidines - pharmacology ; Receptors, Corticotropin-Releasing Hormone - antagonists & inhibitors ; Structure-Activity Relationship</subject><ispartof>Bioorganic & medicinal chemistry letters, 1998-08, Vol.8 (16), p.2067-2070</ispartof><rights>1998</rights><rights>1998 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c389t-58bf9f6da0f75a7612735757516a26360a6986753dc2d1130b5716226200a3613</citedby><cites>FETCH-LOGICAL-c389t-58bf9f6da0f75a7612735757516a26360a6986753dc2d1130b5716226200a3613</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0960894X98003722$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=2366936$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9873487$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Wustrow, David J.</creatorcontrib><creatorcontrib>Capiris, Thomas</creatorcontrib><creatorcontrib>Rubin, Ronald</creatorcontrib><creatorcontrib>Knobelsdorf, James A.</creatorcontrib><creatorcontrib>Akunne, Hyacinth</creatorcontrib><creatorcontrib>Davis, M.Duff</creatorcontrib><creatorcontrib>MacKenzie, Robert</creatorcontrib><creatorcontrib>Pugsley, Thomas A.</creatorcontrib><creatorcontrib>Zoski, Kim T.</creatorcontrib><creatorcontrib>Heffner, Thomas G.</creatorcontrib><creatorcontrib>Wise, Lawrence D.</creatorcontrib><title>Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>A series of 3-phenylpyrazolo[1,5-
a]pyrimidines was prepared and found to have affinity for the human CRF-1 receptor. The 3-dimensional structure of one of the most potent analogs in this series,
10d, was determined by X-ray crystallography and suggests the spatial requirements for potent CRF-1 receptor binding affinity in this series.
A series of 3-phenylpyrazolo[1,5-a]pyrimidines was prepared and found to have affinity for the human CRF-1 receptor. The X-ray structure of one of the most potent analogs suggests the spatial requirements for potent CRF-1 receptor binding affinity in this series.</description><subject>Biological and medical sciences</subject><subject>Corticotropin-Releasing Hormone - antagonists & inhibitors</subject><subject>Crystallography, X-Ray</subject><subject>Drug Design</subject><subject>Humans</subject><subject>Kinetics</subject><subject>Medical sciences</subject><subject>Models, Molecular</subject><subject>Molecular Conformation</subject><subject>Molecular Structure</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>Pyrazoles - chemical synthesis</subject><subject>Pyrazoles - chemistry</subject><subject>Pyrazoles - pharmacology</subject><subject>Pyrimidines - chemical synthesis</subject><subject>Pyrimidines - chemistry</subject><subject>Pyrimidines - pharmacology</subject><subject>Receptors, Corticotropin-Releasing Hormone - antagonists & inhibitors</subject><subject>Structure-Activity Relationship</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1998</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkFtLwzAUgIMoc05_wmAPIgpWc-tJ8yQynAoDxQsIIiFLU4l0bU06Yf56s63sVc7DeTjfuX0IDQm-IJjA5TOWgJNM8rdTmZ1hzARN6A7qEw48YRynu6i_RfbRQQhfGBOOOe-hnswE45noI_649Pq3Lut3cp4m-qNZejd3uavsaPw0ScjIW2ObtvYjXbX6s65caMMh2it0GexRlwfodXLzMr5Lpg-39-PraWJYJtskzWaFLCDXuBCpFkCoYKmIQUBTYIA1yAxEynJDc0IYnqWCAKVAMdYMCBugk83cxtffCxtaNXfB2LLUla0XQYEk8ds4dYDSDWh8HYK3hWriG9ovFcFqZUutbamVCiUztbalaOwbdgsWs7nNt12dnlg_7uo6GF0WXlfGhS1GGYBkELGrDWajjB9nvQrG2crY3EV9rcpr988hf96ng3k</recordid><startdate>19980818</startdate><enddate>19980818</enddate><creator>Wustrow, David J.</creator><creator>Capiris, Thomas</creator><creator>Rubin, Ronald</creator><creator>Knobelsdorf, James A.</creator><creator>Akunne, Hyacinth</creator><creator>Davis, M.Duff</creator><creator>MacKenzie, Robert</creator><creator>Pugsley, Thomas A.</creator><creator>Zoski, Kim T.</creator><creator>Heffner, Thomas G.</creator><creator>Wise, Lawrence D.</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>19980818</creationdate><title>Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists</title><author>Wustrow, David J. ; Capiris, Thomas ; Rubin, Ronald ; Knobelsdorf, James A. ; Akunne, Hyacinth ; Davis, M.Duff ; MacKenzie, Robert ; Pugsley, Thomas A. ; Zoski, Kim T. ; Heffner, Thomas G. ; Wise, Lawrence D.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c389t-58bf9f6da0f75a7612735757516a26360a6986753dc2d1130b5716226200a3613</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1998</creationdate><topic>Biological and medical sciences</topic><topic>Corticotropin-Releasing Hormone - antagonists & inhibitors</topic><topic>Crystallography, X-Ray</topic><topic>Drug Design</topic><topic>Humans</topic><topic>Kinetics</topic><topic>Medical sciences</topic><topic>Models, Molecular</topic><topic>Molecular Conformation</topic><topic>Molecular Structure</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>Pyrazoles - chemical synthesis</topic><topic>Pyrazoles - chemistry</topic><topic>Pyrazoles - pharmacology</topic><topic>Pyrimidines - chemical synthesis</topic><topic>Pyrimidines - chemistry</topic><topic>Pyrimidines - pharmacology</topic><topic>Receptors, Corticotropin-Releasing Hormone - antagonists & inhibitors</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Wustrow, David J.</creatorcontrib><creatorcontrib>Capiris, Thomas</creatorcontrib><creatorcontrib>Rubin, Ronald</creatorcontrib><creatorcontrib>Knobelsdorf, James A.</creatorcontrib><creatorcontrib>Akunne, Hyacinth</creatorcontrib><creatorcontrib>Davis, M.Duff</creatorcontrib><creatorcontrib>MacKenzie, Robert</creatorcontrib><creatorcontrib>Pugsley, Thomas A.</creatorcontrib><creatorcontrib>Zoski, Kim T.</creatorcontrib><creatorcontrib>Heffner, Thomas G.</creatorcontrib><creatorcontrib>Wise, Lawrence D.</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>Wustrow, David J.</au><au>Capiris, Thomas</au><au>Rubin, Ronald</au><au>Knobelsdorf, James A.</au><au>Akunne, Hyacinth</au><au>Davis, M.Duff</au><au>MacKenzie, Robert</au><au>Pugsley, Thomas A.</au><au>Zoski, Kim T.</au><au>Heffner, Thomas G.</au><au>Wise, Lawrence D.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>1998-08-18</date><risdate>1998</risdate><volume>8</volume><issue>16</issue><spage>2067</spage><epage>2070</epage><pages>2067-2070</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>A series of 3-phenylpyrazolo[1,5-
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10d, was determined by X-ray crystallography and suggests the spatial requirements for potent CRF-1 receptor binding affinity in this series.
A series of 3-phenylpyrazolo[1,5-a]pyrimidines was prepared and found to have affinity for the human CRF-1 receptor. The X-ray structure of one of the most potent analogs suggests the spatial requirements for potent CRF-1 receptor binding affinity in this series.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>9873487</pmid><doi>10.1016/S0960-894X(98)00372-2</doi><tpages>4</tpages></addata></record> |
| fulltext | fulltext |
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| ispartof | Bioorganic & medicinal chemistry letters, 1998-08, Vol.8 (16), p.2067-2070 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Biological and medical sciences Corticotropin-Releasing Hormone - antagonists & inhibitors Crystallography, X-Ray Drug Design Humans Kinetics Medical sciences Models, Molecular Molecular Conformation Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Pyrazoles - chemical synthesis Pyrazoles - chemistry Pyrazoles - pharmacology Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Receptors, Corticotropin-Releasing Hormone - antagonists & inhibitors Structure-Activity Relationship |
| title | Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists |
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