Synthesis and evaluation of imidazo[1,5- a]pyrazines as corticotropin releasing hormone receptor ligands
A novel series of imidazo[1,5- a]pyrazines was synthesized and evaluated as corticotropin releasing hormone (CRH) receptor ligands. SAR studies focused primarily on dialkylamino side chain optimization. SAR of the aryl and small alkyl substituents was also explored. A novel series of imidazo[1,5- a]...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2002-02, Vol.12 (3), p.291-294 |
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container_issue | 3 |
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container_title | Bioorganic & medicinal chemistry letters |
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creator | Hartz, Richard A. Gilligan, Paul J. Nanda, Kausik K. Tebben, Andrew J. Fitzgerald, Larry W. Miller, Keith |
description | A novel series of imidazo[1,5-
a]pyrazines was synthesized and evaluated as corticotropin releasing hormone (CRH) receptor ligands. SAR studies focused primarily on dialkylamino side chain optimization. SAR of the aryl and small alkyl substituents was also explored.
A novel series of imidazo[1,5-
a]pyrazines was synthesized and evaluated as corticotropin releasing hormone (CRH) receptor ligands. |
doi_str_mv | 10.1016/S0960-894X(01)00741-7 |
format | Article |
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a]pyrazines was synthesized and evaluated as corticotropin releasing hormone (CRH) receptor ligands. SAR studies focused primarily on dialkylamino side chain optimization. SAR of the aryl and small alkyl substituents was also explored.
A novel series of imidazo[1,5-
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a]pyrazines was synthesized and evaluated as corticotropin releasing hormone (CRH) receptor ligands. SAR studies focused primarily on dialkylamino side chain optimization. SAR of the aryl and small alkyl substituents was also explored.
A novel series of imidazo[1,5-
a]pyrazines was synthesized and evaluated as corticotropin releasing hormone (CRH) receptor ligands.</description><subject>Alkylation</subject><subject>Animals</subject><subject>Binding, Competitive - drug effects</subject><subject>Biological and medical sciences</subject><subject>Imidazoles - chemical synthesis</subject><subject>Imidazoles - pharmacology</subject><subject>In Vitro Techniques</subject><subject>Indicators and Reagents</subject><subject>Ligands</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>Prefrontal Cortex - metabolism</subject><subject>Pyrazines - chemical synthesis</subject><subject>Pyrazines - pharmacology</subject><subject>Rats</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>2002</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkFFrFDEQx4Mo9qx-BCUvioKrM5tkN_skUloVCj5UQRAJuWS2F9lN1mSvcP307vUO--jTwPD7_2f4MfYc4R0CNu-voGug0p388RrwDUArsWofsBXKRlZCgnrIVv-QE_aklN8AKEHKx-wEUaNsNazY5moX5w2VULiNntONHbZ2Diny1PMwBm9v0098qypuf027bG9DpAUt3KU8B5fmnKYQeaaBbAnxmm9SHlOkZeNomlPmQ7hemstT9qi3Q6Fnx3nKvl-cfzv7XF1-_fTl7ONl5aRq50oJ7KGulatd3fYktBTgaqFQKKsasN3aou7qNTovO-XXynnlJGoQTV177cQpe3XonXL6s6UymzEUR8NgI6VtMS1KVFrrBVQH0OVUSqbeTDmMNu8MgtkrNneKzd6fATR3ik275F4cD2zXI_n71NHpArw8ArY4O_TZRhfKPSekxhb3RR8OHC06bgJlU1yg6MiHRd5sfAr_eeUvSPCZXg</recordid><startdate>20020211</startdate><enddate>20020211</enddate><creator>Hartz, Richard A.</creator><creator>Gilligan, Paul J.</creator><creator>Nanda, Kausik K.</creator><creator>Tebben, Andrew J.</creator><creator>Fitzgerald, Larry W.</creator><creator>Miller, Keith</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>20020211</creationdate><title>Synthesis and evaluation of imidazo[1,5- a]pyrazines as corticotropin releasing hormone receptor ligands</title><author>Hartz, Richard A. ; Gilligan, Paul J. ; Nanda, Kausik K. ; Tebben, Andrew J. ; Fitzgerald, Larry W. ; Miller, Keith</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c457t-531f0225c2c27fe38430c235135a560a9ba1892b1cd495db5cd5c41803622d8c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2002</creationdate><topic>Alkylation</topic><topic>Animals</topic><topic>Binding, Competitive - drug effects</topic><topic>Biological and medical sciences</topic><topic>Imidazoles - chemical synthesis</topic><topic>Imidazoles - pharmacology</topic><topic>In Vitro Techniques</topic><topic>Indicators and Reagents</topic><topic>Ligands</topic><topic>Medical sciences</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>Prefrontal Cortex - metabolism</topic><topic>Pyrazines - chemical synthesis</topic><topic>Pyrazines - pharmacology</topic><topic>Rats</topic><topic>Receptors, Corticotropin-Releasing Hormone - antagonists & inhibitors</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Hartz, Richard A.</creatorcontrib><creatorcontrib>Gilligan, Paul J.</creatorcontrib><creatorcontrib>Nanda, Kausik K.</creatorcontrib><creatorcontrib>Tebben, Andrew J.</creatorcontrib><creatorcontrib>Fitzgerald, Larry W.</creatorcontrib><creatorcontrib>Miller, Keith</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>Hartz, Richard A.</au><au>Gilligan, Paul J.</au><au>Nanda, Kausik K.</au><au>Tebben, Andrew J.</au><au>Fitzgerald, Larry W.</au><au>Miller, Keith</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and evaluation of imidazo[1,5- a]pyrazines as corticotropin releasing hormone receptor ligands</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2002-02-11</date><risdate>2002</risdate><volume>12</volume><issue>3</issue><spage>291</spage><epage>294</epage><pages>291-294</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>A novel series of imidazo[1,5-
a]pyrazines was synthesized and evaluated as corticotropin releasing hormone (CRH) receptor ligands. SAR studies focused primarily on dialkylamino side chain optimization. SAR of the aryl and small alkyl substituents was also explored.
A novel series of imidazo[1,5-
a]pyrazines was synthesized and evaluated as corticotropin releasing hormone (CRH) receptor ligands.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>11814780</pmid><doi>10.1016/S0960-894X(01)00741-7</doi><tpages>4</tpages></addata></record> |
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subjects | Alkylation Animals Binding, Competitive - drug effects Biological and medical sciences Imidazoles - chemical synthesis Imidazoles - pharmacology In Vitro Techniques Indicators and Reagents Ligands Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Prefrontal Cortex - metabolism Pyrazines - chemical synthesis Pyrazines - pharmacology Rats Receptors, Corticotropin-Releasing Hormone - antagonists & inhibitors Structure-Activity Relationship |
title | Synthesis and evaluation of imidazo[1,5- a]pyrazines as corticotropin releasing hormone receptor ligands |
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