{"id":"https://openalex.org/W2005135546","doi":"https://doi.org/10.1021/jm00387a031","title":"Synthesis and pharmacological evaluation of .gamma.-aminobutyric acid analogs. New ligand for GABAB sites","display_name":"Synthesis and pharmacological evaluation of .gamma.-aminobutyric acid analogs. New ligand for GABAB sites","publication_year":1987,"publication_date":"1987-04-01","ids":{"openalex":"https://openalex.org/W2005135546","doi":"https://doi.org/10.1021/jm00387a031","mag":"2005135546","pmid":"https://pubmed.ncbi.nlm.nih.gov/3031294"},"language":"en","primary_location":{"id":"doi:10.1021/jm00387a031","doi":"https://doi.org/10.1021/jm00387a031","is_oa":false,"landing_page_url":"https://doi.org/10.1021/jm00387a031","pdf_url":null,"source":{"id":"https://openalex.org/S162030435","display_name":"Journal of Medicinal Chemistry","issn_l":"0022-2623","issn":["0022-2623","1520-4804"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-a","jufo-3","ki-jl-2","medline","norway-2","poland-200","russia-white-list-1","vabb-shw"],"host_organization":"https://openalex.org/P4310320006","host_organization_name":"American Chemical Society","host_organization_lineage":["https://openalex.org/P4310320006"],"host_organization_lineage_names":["American Chemical Society"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of Medicinal Chemistry","raw_type":"journal-article"},"volume":null,"type":"article","is_traditional":true,"indexed_in":["crossref","pubmed"],"open_access":{"is_oa":false,"oa_status":"closed","oa_url":null,"any_repository_has_fulltext":false},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5109956088","display_name":"Pascal Berthelot","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Pascal Berthelot","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5105987040","display_name":"Claude Vaccher","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Claude Vaccher","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5072172890","display_name":"Amir Musadad","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Amir Musadad","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5062800640","display_name":"Nathalie Flouquet","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Nathalie Flouquet","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5079558090","display_name":"Michel Debaert","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Michel Debaert","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"last","author":{"id":"https://openalex.org/A5109991141","display_name":"M. Luyckx","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Michel Luyckx","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]}],"institutions":[],"countries_distinct_count":0,"institutions_distinct_count":0,"corresponding_author_ids":[],"corresponding_institution_ids":[],"apc_list":{"value":4500,"currency":"USD","value_usd":4500},"apc_paid":null,"fwci":0.756,"has_fulltext":false,"cited_by_count":56,"citation_normalized_percentile":{"value":0.62523282,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":88,"max":96},"biblio":{"volume":"30","issue":"4","first_page":"743","last_page":"746"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T10077","display_name":"Neuroscience and Neuropharmacology Research","score":0.9380000233650208,"subfield":{"id":"https://openalex.org/subfields/2804","display_name":"Cellular and Molecular Neuroscience"},"field":{"id":"https://openalex.org/fields/28","display_name":"Neuroscience"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},"topics":[{"id":"https://openalex.org/T10077","display_name":"Neuroscience and Neuropharmacology Research","score":0.9380000233650208,"subfield":{"id":"https://openalex.org/subfields/2804","display_name":"Cellular and Molecular Neuroscience"},"field":{"id":"https://openalex.org/fields/28","display_name":"Neuroscience"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},{"id":"https://openalex.org/T11178","display_name":"Receptor Mechanisms and Signaling","score":0.031199999153614044,"subfield":{"id":"https://openalex.org/subfields/1312","display_name":"Molecular Biology"},"field":{"id":"https://openalex.org/fields/13","display_name":"Biochemistry, Genetics and Molecular Biology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},{"id":"https://openalex.org/T10274","display_name":"Heterocyclic Compound Synthesis and Bioactivity","score":0.012299999594688416,"subfield":{"id":"https://openalex.org/subfields/1605","display_name":"Organic Chemistry"},"field":{"id":"https://openalex.org/fields/16","display_name":"Chemistry"},"domain":{"id":"https://openalex.org/domains/3","display_name":"Physical Sciences"}}],"keywords":[{"id":"https://openalex.org/keywords/gaba-analogues","display_name":"GABA analogues","score":0.7749999761581421},{"id":"https://openalex.org/keywords/gabab-receptors","display_name":"GABAB receptors","score":0.8849999904632568},{"id":"https://openalex.org/keywords/baclofen","display_name":"baclofen","score":0.8579999804496765},{"id":"https://openalex.org/keywords/structure-activity-relationship","display_name":"structure-activity relationship","score":0.671999990940094},{"id":"https://openalex.org/keywords/benzofuran-derivatives","display_name":"benzofuran derivatives","score":0.890999972820282},{"id":"https://openalex.org/keywords/gaba-receptor-agonists","display_name":"GABA agonists","score":0.652999997138977},{"id":"https://openalex.org/keywords/receptor-ligands","display_name":"receptor ligands","score":0.628000020980835},{"id":"https://openalex.org/keywords/racemic-compounds","display_name":"racemic compounds","score":0.45899999141693115}],"concepts":[{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.9327268600463867},{"id":"https://openalex.org/C116569031","wikidata":"https://www.wikidata.org/wiki/Q899107","display_name":"Ligand (biochemistry)","level":3,"score":0.5773403644561768},{"id":"https://openalex.org/C101027131","wikidata":"https://www.wikidata.org/wiki/Q305671","display_name":"GABAB receptor","level":4,"score":0.49181583523750305},{"id":"https://openalex.org/C2777771985","wikidata":"https://www.wikidata.org/wiki/Q210021","display_name":"gamma-Aminobutyric acid","level":3,"score":0.4755905866622925},{"id":"https://openalex.org/C21951064","wikidata":"https://www.wikidata.org/wiki/Q899212","display_name":"Combinatorial chemistry","level":1,"score":0.42160624265670776},{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.38932159543037415},{"id":"https://openalex.org/C71240020","wikidata":"https://www.wikidata.org/wiki/Q186011","display_name":"Stereochemistry","level":1,"score":0.3596641421318054},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.3024142384529114},{"id":"https://openalex.org/C2778938600","wikidata":"https://www.wikidata.org/wiki/Q389934","display_name":"Agonist","level":3,"score":0.15147918462753296},{"id":"https://openalex.org/C170493617","wikidata":"https://www.wikidata.org/wiki/Q208467","display_name":"Receptor","level":2,"score":0.13913494348526},{"id":"https://openalex.org/C71924100","wikidata":"https://www.wikidata.org/wiki/Q11190","display_name":"Medicine","level":0,"score":0.0}],"mesh":[{"descriptor_ui":"D000818","descriptor_name":"Animals","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D001418","descriptor_name":"Baclofen","qualifier_ui":"Q000031","qualifier_name":"analogs & derivatives","is_major_topic":true},{"descriptor_ui":"D001418","descriptor_name":"Baclofen","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":false},{"descriptor_ui":"D001418","descriptor_name":"Baclofen","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D001418","descriptor_name":"Baclofen","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D002540","descriptor_name":"Cerebral Cortex","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D005680","descriptor_name":"gamma-Aminobutyric Acid","qualifier_ui":"Q000031","qualifier_name":"analogs & derivatives","is_major_topic":true},{"descriptor_ui":"D005680","descriptor_name":"gamma-Aminobutyric Acid","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":false},{"descriptor_ui":"D005680","descriptor_name":"gamma-Aminobutyric Acid","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D005680","descriptor_name":"gamma-Aminobutyric Acid","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D008297","descriptor_name":"Male","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D011919","descriptor_name":"Rats, Inbred Strains","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D011963","descriptor_name":"Receptors, GABA-A","qualifier_ui":"Q000187","qualifier_name":"drug effects","is_major_topic":true},{"descriptor_ui":"D011963","descriptor_name":"Receptors, GABA-A","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D013237","descriptor_name":"Stereoisomerism","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D013329","descriptor_name":"Structure-Activity Relationship","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D018080","descriptor_name":"Receptors, GABA-B","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D051381","descriptor_name":"Rats","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false}],"locations_count":2,"locations":[{"id":"doi:10.1021/jm00387a031","doi":"https://doi.org/10.1021/jm00387a031","is_oa":false,"landing_page_url":"https://doi.org/10.1021/jm00387a031","pdf_url":null,"source":{"id":"https://openalex.org/S162030435","display_name":"Journal of Medicinal Chemistry","issn_l":"0022-2623","issn":["0022-2623","1520-4804"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-a","jufo-3","ki-jl-2","medline","norway-2","poland-200","russia-white-list-1","vabb-shw"],"host_organization":"https://openalex.org/P4310320006","host_organization_name":"American Chemical Society","host_organization_lineage":["https://openalex.org/P4310320006"],"host_organization_lineage_names":["American Chemical Society"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of Medicinal Chemistry","raw_type":"journal-article"},{"id":"pmid:3031294","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/3031294","pdf_url":null,"source":{"id":"https://openalex.org/S4306525036","display_name":"PubMed","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I1299303238","host_organization_name":"National Institutes of Health","host_organization_lineage":["https://openalex.org/I1299303238"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of medicinal chemistry","raw_type":"Comparative Study"}],"best_oa_location":null,"sustainable_development_goals":[{"display_name":"Good health and well-being","id":"https://metadata.un.org/sdg/3","score":0.4043000042438507}],"study_designs":[],"awards":[],"funders":[],"has_content":{"pdf":false,"grobid_xml":false},"content_urls":null,"referenced_works_count":0,"referenced_works":[],"related_works":["https://openalex.org/W1974927854","https://openalex.org/W2950945213","https://openalex.org/W1998097979","https://openalex.org/W2951908880","https://openalex.org/W4412252583","https://openalex.org/W2415181284","https://openalex.org/W2007312469","https://openalex.org/W2017774566","https://openalex.org/W1996729572","https://openalex.org/W4408782422"],"abstract_inverted_index":{"Baclofen":[0],"(beta-p-chlorophenyl-GABA)":[1],"is":[2],"the":[3,8,14,38,55,64,70],"only":[4],"selective":[5],"agonist":[6],"for":[7,37,51,69],"bicuculline-insensitive":[9],"GABAB":[10,39,76],"receptor.":[11,40,77],"We":[12],"report":[13],"synthesis":[15],"of":[16,47,58,66],"new":[17,50],"GABA":[18],"analogues":[19],"and":[20,30,54],"baclofen":[21],"analogues.":[22],"In":[23],"vitro,":[24],"two":[25],"compounds,":[26],"4-amino-3-benzo[b]furan-2-ylbutanoic":[27],"acid":[28,32],"(9g)":[29],"4-amino-3-(5-methoxybenzo[b]furan-2-yl)butanoic":[31],"(9h),":[33],"showed":[34],"an":[35,67],"affinity":[36],"The":[41],"results":[42],"obtained":[43],"with":[44,73],"racemic":[45],"compounds":[46],"benzofuran":[48],"structure,":[49],"this":[52],"series,":[53],"surprising":[56],"inactivity":[57],"compound":[59],"3a":[60],"(4-amino-3-(4-hydroxyphenyl)butanoic":[61],"acid)":[62],"permit":[63],"proposal":[65],"hypothesis":[68],"structure-activity":[71],"relationships":[72],"regard":[74],"to":[75]},"counts_by_year":[{"year":2026,"cited_by_count":1},{"year":2025,"cited_by_count":1},{"year":2024,"cited_by_count":2},{"year":2019,"cited_by_count":1},{"year":2016,"cited_by_count":1},{"year":2015,"cited_by_count":2}],"updated_date":"2026-11-04T10:54:05.112534","created_date":"2016-06-24T00:00:00"}
