{"id":"https://openalex.org/W1978105661","doi":"https://doi.org/10.1021/jm900796p","title":"Identification of Novel Indanylsulfonamide Guanylhydrazones as Potent 5-HT6Serotonin Receptor Antagonists","display_name":"Identification of Novel Indanylsulfonamide Guanylhydrazones as Potent 5-HT6Serotonin Receptor Antagonists","publication_year":2009,"publication_date":"2009-09-09","ids":{"openalex":"https://openalex.org/W1978105661","doi":"https://doi.org/10.1021/jm900796p","mag":"1978105661","pmid":"https://pubmed.ncbi.nlm.nih.gov/19739674"},"language":"en","primary_location":{"id":"doi:10.1021/jm900796p","doi":"https://doi.org/10.1021/jm900796p","is_oa":false,"landing_page_url":"https://doi.org/10.1021/jm900796p","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/A5078490873","display_name":"Neus Mesquida","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I71999127","display_name":"Universitat de Barcelona","ror":"https://ror.org/021018s57","country_code":"ES","type":"education","lineage":["https://openalex.org/I71999127"]}],"countries":["ES"],"is_corresponding":true,"raw_author_name":"Neus Mesquida","raw_affiliation_strings":["Laboratori de Qu\u00edmica Org\u00e0nica, Departament de Farmacologia i Qu\u00edmica Terap\u00e8utica, Facultat de Farm\u00e0cia, Universitat de Barcelona, Avda. Joan XXIII s/n, 08028 Barcelona, Spain"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Laboratori de Qu\u00edmica Org\u00e0nica, Departament de Farmacologia i Qu\u00edmica Terap\u00e8utica, Facultat de Farm\u00e0cia, Universitat de Barcelona, Avda. Joan XXIII s/n, 08028 Barcelona, Spain","institution_ids":["https://openalex.org/I71999127"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5020351764","display_name":"Sara L\u00f3pez-P\u00e9rez","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I71999127","display_name":"Universitat de Barcelona","ror":"https://ror.org/021018s57","country_code":"ES","type":"education","lineage":["https://openalex.org/I71999127"]}],"countries":["ES"],"is_corresponding":false,"raw_author_name":"Sara L\u00f3pez-P\u00e9rez","raw_affiliation_strings":["Laboratori de Qu\u00edmica Org\u00e0nica, Departament de Farmacologia i Qu\u00edmica Terap\u00e8utica, Facultat de Farm\u00e0cia, Universitat de Barcelona, Avda. Joan XXIII s/n, 08028 Barcelona, Spain"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Laboratori de Qu\u00edmica Org\u00e0nica, Departament de Farmacologia i Qu\u00edmica Terap\u00e8utica, Facultat de Farm\u00e0cia, Universitat de Barcelona, Avda. Joan XXIII s/n, 08028 Barcelona, Spain","institution_ids":["https://openalex.org/I71999127"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5068035815","display_name":"Immaculada Dinar\u00e8s","orcid":"https://orcid.org/0000-0002-8637-2598","observed_orcids":["https://orcid.org/0000-0002-8637-2598"]},"institutions":[{"id":"https://openalex.org/I71999127","display_name":"Universitat de Barcelona","ror":"https://ror.org/021018s57","country_code":"ES","type":"education","lineage":["https://openalex.org/I71999127"]}],"countries":["ES"],"is_corresponding":false,"raw_author_name":"Immaculada Dinar\u00e8s","raw_affiliation_strings":["Laboratori de Qu\u00edmica Org\u00e0nica, Departament de Farmacologia i Qu\u00edmica Terap\u00e8utica, Facultat de Farm\u00e0cia, Universitat de Barcelona, Avda. Joan XXIII s/n, 08028 Barcelona, Spain"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Laboratori de Qu\u00edmica Org\u00e0nica, Departament de Farmacologia i Qu\u00edmica Terap\u00e8utica, Facultat de Farm\u00e0cia, Universitat de Barcelona, Avda. Joan XXIII s/n, 08028 Barcelona, Spain","institution_ids":["https://openalex.org/I71999127"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5103854440","display_name":"Jordi Frigola","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210162160","display_name":"Esteve (Spain)","ror":"https://ror.org/04yns5a36","country_code":"ES","type":"company","lineage":["https://openalex.org/I4210162160"]}],"countries":["ES"],"is_corresponding":false,"raw_author_name":"Jordi Frigola","raw_affiliation_strings":["ESTEVE, Av. Mare de D\u00e9u de Montserrat 221, 08041 Barcelona, Spain"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"ESTEVE, Av. Mare de D\u00e9u de Montserrat 221, 08041 Barcelona, Spain","institution_ids":["https://openalex.org/I4210162160"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5065739569","display_name":"Ramon Merc\u00e8","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210162160","display_name":"Esteve (Spain)","ror":"https://ror.org/04yns5a36","country_code":"ES","type":"company","lineage":["https://openalex.org/I4210162160"]}],"countries":["ES"],"is_corresponding":false,"raw_author_name":"Ramon Merc\u00e8","raw_affiliation_strings":["ESTEVE, Av. Mare de D\u00e9u de Montserrat 221, 08041 Barcelona, Spain"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"ESTEVE, Av. Mare de D\u00e9u de Montserrat 221, 08041 Barcelona, Spain","institution_ids":["https://openalex.org/I4210162160"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5109117260","display_name":"J\u00f6rg Holenz","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210162160","display_name":"Esteve (Spain)","ror":"https://ror.org/04yns5a36","country_code":"ES","type":"company","lineage":["https://openalex.org/I4210162160"]}],"countries":["ES"],"is_corresponding":false,"raw_author_name":"J\u00f6rg Holenz","raw_affiliation_strings":["ESTEVE, Av. Mare de D\u00e9u de Montserrat 221, 08041 Barcelona, Spain"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"ESTEVE, Av. Mare de D\u00e9u de Montserrat 221, 08041 Barcelona, Spain","institution_ids":["https://openalex.org/I4210162160"]}]},{"author_position":"middle","author":{"id":null,"display_name":"Raquel P\u00e9rez","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210162160","display_name":"Esteve (Spain)","ror":"https://ror.org/04yns5a36","country_code":"ES","type":"company","lineage":["https://openalex.org/I4210162160"]}],"countries":["ES"],"is_corresponding":false,"raw_author_name":"Raquel P\u00e9rez","raw_affiliation_strings":["ESTEVE, Av. Mare de D\u00e9u de Montserrat 221, 08041 Barcelona, Spain"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"ESTEVE, Av. Mare de D\u00e9u de Montserrat 221, 08041 Barcelona, Spain","institution_ids":["https://openalex.org/I4210162160"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5079313086","display_name":"Javier Burgue\u00f1o","orcid":"https://orcid.org/0000-0001-8938-8299","observed_orcids":["https://orcid.org/0000-0001-8938-8299"]},"institutions":[{"id":"https://openalex.org/I4210162160","display_name":"Esteve (Spain)","ror":"https://ror.org/04yns5a36","country_code":"ES","type":"company","lineage":["https://openalex.org/I4210162160"]}],"countries":["ES"],"is_corresponding":false,"raw_author_name":"Javier Burgue\u00f1o","raw_affiliation_strings":["ESTEVE, Av. Mare de D\u00e9u de Montserrat 221, 08041 Barcelona, Spain"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"ESTEVE, Av. Mare de D\u00e9u de Montserrat 221, 08041 Barcelona, Spain","institution_ids":["https://openalex.org/I4210162160"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5043906877","display_name":"Ermitas Alcalde","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I71999127","display_name":"Universitat de Barcelona","ror":"https://ror.org/021018s57","country_code":"ES","type":"education","lineage":["https://openalex.org/I71999127"]}],"countries":["ES"],"is_corresponding":true,"raw_author_name":"Ermitas Alcalde","raw_affiliation_strings":["Laboratori de Qu\u00edmica Org\u00e0nica, Departament de Farmacologia i Qu\u00edmica Terap\u00e8utica, Facultat de Farm\u00e0cia, Universitat de Barcelona, Avda. Joan XXIII s/n, 08028 Barcelona, Spain"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Laboratori de Qu\u00edmica Org\u00e0nica, Departament de Farmacologia i Qu\u00edmica Terap\u00e8utica, Facultat de Farm\u00e0cia, Universitat de Barcelona, Avda. Joan XXIII s/n, 08028 Barcelona, Spain","institution_ids":["https://openalex.org/I71999127"]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":2,"corresponding_author_ids":["https://openalex.org/A5043906877","https://openalex.org/A5078490873"],"corresponding_institution_ids":["https://openalex.org/I71999127"],"apc_list":{"value":4500,"currency":"USD","value_usd":4500},"apc_paid":null,"fwci":0.3296,"has_fulltext":false,"cited_by_count":12,"citation_normalized_percentile":{"value":0.52355701,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":88,"max":97},"biblio":{"volume":"52","issue":"19","first_page":"6153","last_page":"6157"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T11178","display_name":"Receptor Mechanisms and Signaling","score":0.5054000020027161,"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"}},"topics":[{"id":"https://openalex.org/T11178","display_name":"Receptor Mechanisms and Signaling","score":0.5054000020027161,"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/T10056","display_name":"Neurotransmitter Receptor Influence on Behavior","score":0.3285999894142151,"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/T10274","display_name":"Heterocyclic Compound Synthesis and Bioactivity","score":0.05860000103712082,"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/5-ht6-receptor-antagonists","display_name":"5-HT6 receptor antagonists","score":0.8920000195503235},{"id":"https://openalex.org/keywords/guanylhydrazones","display_name":"guanylhydrazones","score":0.828000009059906},{"id":"https://openalex.org/keywords/serotonin-receptor-antagonists","display_name":"serotonin antagonists","score":0.5839999914169312},{"id":"https://openalex.org/keywords/receptor-binding-affinity","display_name":"receptor binding affinity","score":0.7229999899864197},{"id":"https://openalex.org/keywords/structure-activity-relationship","display_name":"structure-activity relationship","score":0.6470000147819519}],"concepts":[{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.9312342405319214},{"id":"https://openalex.org/C2775864247","wikidata":"https://www.wikidata.org/wiki/Q167934","display_name":"Serotonin","level":3,"score":0.6847761869430542},{"id":"https://openalex.org/C71240020","wikidata":"https://www.wikidata.org/wiki/Q186011","display_name":"Stereochemistry","level":1,"score":0.6532604098320007},{"id":"https://openalex.org/C2776568683","wikidata":"https://www.wikidata.org/wiki/Q23005640","display_name":"Moiety","level":2,"score":0.6497681140899658},{"id":"https://openalex.org/C170493617","wikidata":"https://www.wikidata.org/wiki/Q208467","display_name":"Receptor","level":2,"score":0.6152790784835815},{"id":"https://openalex.org/C53910766","wikidata":"https://www.wikidata.org/wiki/Q238516","display_name":"5-HT receptor","level":4,"score":0.6090421676635742},{"id":"https://openalex.org/C2781039511","wikidata":"https://www.wikidata.org/wiki/Q3208529","display_name":"Sulfonamide","level":2,"score":0.5856143236160278},{"id":"https://openalex.org/C2910276969","wikidata":"https://www.wikidata.org/wiki/Q7455047","display_name":"Serotonin Antagonists","level":5,"score":0.5764162540435791},{"id":"https://openalex.org/C3018795828","wikidata":"https://www.wikidata.org/wiki/Q899107","display_name":"Binding affinities","level":3,"score":0.537999153137207},{"id":"https://openalex.org/C2780283098","wikidata":"https://www.wikidata.org/wiki/Q4688960","display_name":"Affinities","level":2,"score":0.5367677211761475},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.1934485137462616}],"mesh":[{"descriptor_ui":"D006157","descriptor_name":"Guanosine Monophosphate","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D006157","descriptor_name":"Guanosine Monophosphate","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D006801","descriptor_name":"Humans","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D006835","descriptor_name":"Hydrazones","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":false},{"descriptor_ui":"D006835","descriptor_name":"Hydrazones","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":true},{"descriptor_ui":"D007192","descriptor_name":"Indenes","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D011485","descriptor_name":"Protein Binding","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D011985","descriptor_name":"Receptors, Serotonin","qualifier_ui":"Q000187","qualifier_name":"drug effects","is_major_topic":true},{"descriptor_ui":"D012702","descriptor_name":"Serotonin Antagonists","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D013329","descriptor_name":"Structure-Activity Relationship","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D013449","descriptor_name":"Sulfonamides","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D013449","descriptor_name":"Sulfonamides","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D020128","descriptor_name":"Inhibitory Concentration 50","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false}],"locations_count":2,"locations":[{"id":"doi:10.1021/jm900796p","doi":"https://doi.org/10.1021/jm900796p","is_oa":false,"landing_page_url":"https://doi.org/10.1021/jm900796p","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:19739674","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/19739674","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":"Journal Article"}],"best_oa_location":null,"sustainable_development_goals":[{"id":"https://metadata.un.org/sdg/3","display_name":"Good health and well-being","score":0.4000000059604645}],"study_designs":[],"awards":[],"funders":[],"has_content":{"grobid_xml":false,"pdf":false},"content_urls":null,"referenced_works_count":31,"referenced_works":["https://openalex.org/W1964511337","https://openalex.org/W1967874875","https://openalex.org/W1968006674","https://openalex.org/W1972615247","https://openalex.org/W1973177864","https://openalex.org/W1974496422","https://openalex.org/W1976125276","https://openalex.org/W1997337458","https://openalex.org/W2004116204","https://openalex.org/W2016552887","https://openalex.org/W2019214891","https://openalex.org/W2022514673","https://openalex.org/W2026823702","https://openalex.org/W2032277387","https://openalex.org/W2040985862","https://openalex.org/W2043746918","https://openalex.org/W2043813981","https://openalex.org/W2045712137","https://openalex.org/W2045906370","https://openalex.org/W2048159519","https://openalex.org/W2051038048","https://openalex.org/W2056038991","https://openalex.org/W2062174853","https://openalex.org/W2072398405","https://openalex.org/W2088735650","https://openalex.org/W2137076561","https://openalex.org/W2262188647","https://openalex.org/W2398650533","https://openalex.org/W4211248987","https://openalex.org/W4252764178","https://openalex.org/W4407034851"],"related_works":["https://openalex.org/W2066118774","https://openalex.org/W2179204391","https://openalex.org/W2045906370","https://openalex.org/W2008730137","https://openalex.org/W2064446575","https://openalex.org/W1986967268","https://openalex.org/W2070473876","https://openalex.org/W2952068036","https://openalex.org/W1968006674","https://openalex.org/W2072398405"],"abstract_inverted_index":{"Changing":[0],"the":[1,6,20,25,28,42,51],"N,N-(dimethylamino)ethyl":[2],"side":[3],"chain":[4],"in":[5,50],"N-[3-(aminoethyl)inden-5-yl]sulfonamide":[7],"5-HT(6)":[8,43],"serotonin":[9],"receptor":[10],"agonists":[11],"1":[12],"by":[13],"a":[14],"conformationally":[15],"rigid":[16],"guanylhydrazone":[17],"moiety":[18],"at":[19,41],"indene":[21],"3-position":[22],"led":[23],"to":[24],"identification":[26],"of":[27],"title":[29],"indanylguanylhydrazones":[30],"6,":[31],"which":[32],"exhibited":[33],"excellent":[34],"binding":[35],"affinities":[36],"and":[37,47,62],"an":[38],"antagonistic":[39],"response":[40],"receptor,":[44],"with":[45],"K(i)":[46],"IC(50)":[48,58],"values":[49],"nanomolar":[52],"range":[53],"(K(i)":[54],">or=":[55,59],"1.2":[56],"nM,":[57,61],"47":[60],"I(max)":[63],"<or=":[64],"173%).":[65]},"counts_by_year":[{"year":2025,"cited_by_count":1},{"year":2024,"cited_by_count":1},{"year":2017,"cited_by_count":1},{"year":2015,"cited_by_count":4},{"year":2014,"cited_by_count":1}],"updated_date":"2026-11-08T12:12:28.789561","created_date":"2016-06-24T00:00:00"}