{"id":"https://openalex.org/W2094844576","doi":"https://doi.org/10.1016/j.bmcl.2009.05.101","title":"Synthesis, structure\u2013activity relationships, and biological profiles of a dihydrobenzoxathiin class of histamine H3 receptor inverse agonists","display_name":"Synthesis, structure\u2013activity relationships, and biological profiles of a dihydrobenzoxathiin class of histamine H3 receptor inverse agonists","publication_year":2009,"publication_date":"2009-05-31","ids":{"openalex":"https://openalex.org/W2094844576","doi":"https://doi.org/10.1016/j.bmcl.2009.05.101","mag":"2094844576","pmid":"https://pubmed.ncbi.nlm.nih.gov/19520574"},"language":"en","primary_location":{"id":"doi:10.1016/j.bmcl.2009.05.101","doi":"https://doi.org/10.1016/j.bmcl.2009.05.101","is_oa":false,"landing_page_url":"https://doi.org/10.1016/j.bmcl.2009.05.101","pdf_url":null,"source":{"id":"https://openalex.org/S30970080","display_name":"Bioorganic & Medicinal Chemistry Letters","issn_l":"0960-894X","issn":["0960-894X","1464-3405"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-b","jufo-1","ki-jl-1","medline","norway-1","poland-70","russia-white-list-2","vabb-shw"],"host_organization":"https://openalex.org/P4310320990","host_organization_name":"Elsevier BV","host_organization_lineage":["https://openalex.org/P4310320990"],"host_organization_lineage_names":["Elsevier BV"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Bioorganic & Medicinal Chemistry Letters","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/A5089301917","display_name":"Takahide Sasaki","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Takahide Sasaki","raw_affiliation_strings":["Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5008683011","display_name":"Toshiyuki Takahashi","orcid":"https://orcid.org/0000-0003-1627-8624","observed_orcids":["https://orcid.org/0000-0003-1627-8624"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Toshiyuki Takahashi","raw_affiliation_strings":["Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5112649901","display_name":"Tsuyoshi Nagase","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Tsuyoshi Nagase","raw_affiliation_strings":["Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan","institution_ids":[]}]},{"author_position":"middle","author":{"id":null,"display_name":"Takashi Mizutani","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Takashi Mizutani","raw_affiliation_strings":["Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5102976681","display_name":"Sayaka Ito","orcid":"https://orcid.org/0000-0003-1992-8661","observed_orcids":["https://orcid.org/0000-0003-1992-8661"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Sayaka Ito","raw_affiliation_strings":["Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5007001095","display_name":"Yuko Mitobe","orcid":"https://orcid.org/0000-0001-8897-8561","observed_orcids":["https://orcid.org/0000-0001-8897-8561"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Yuko Mitobe","raw_affiliation_strings":["Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5108484968","display_name":"Yasuhisa Miyamoto","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Yasuhisa Miyamoto","raw_affiliation_strings":["Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5002341540","display_name":"Maki Kanesaka","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Maki Kanesaka","raw_affiliation_strings":["Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5057428545","display_name":"Ryo Yoshimoto","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Ryo Yoshimoto","raw_affiliation_strings":["Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5103586620","display_name":"Takeshi Tanaka","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Takeshi Tanaka","raw_affiliation_strings":["Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5067022912","display_name":"Norihiro Takenaga","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Norihiro Takenaga","raw_affiliation_strings":["Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5040795360","display_name":"Shigeru Tokita","orcid":"https://orcid.org/0000-0003-0916-2199","observed_orcids":["https://orcid.org/0000-0003-0916-2199"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Shigeru Tokita","raw_affiliation_strings":["Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan","institution_ids":[]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5111593751","display_name":"Nagaaki Sato","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":true,"raw_author_name":"Nagaaki Sato","raw_affiliation_strings":["Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan","institution_ids":[]}]}],"institutions":[],"countries_distinct_count":0,"institutions_distinct_count":0,"corresponding_author_ids":["https://openalex.org/A5111593751"],"corresponding_institution_ids":[],"apc_list":{"value":3880,"currency":"USD","value_usd":3880},"apc_paid":null,"fwci":0.1377,"has_fulltext":false,"cited_by_count":10,"citation_normalized_percentile":{"value":0.50768854,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":88,"max":96},"biblio":{"volume":"19","issue":"15","first_page":"4232","last_page":"4236"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T11346","display_name":"Mast cells and histamine","score":0.5497999787330627,"subfield":{"id":"https://openalex.org/subfields/2403","display_name":"Immunology"},"field":{"id":"https://openalex.org/fields/24","display_name":"Immunology and Microbiology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},"topics":[{"id":"https://openalex.org/T11346","display_name":"Mast cells and histamine","score":0.5497999787330627,"subfield":{"id":"https://openalex.org/subfields/2403","display_name":"Immunology"},"field":{"id":"https://openalex.org/fields/24","display_name":"Immunology and Microbiology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},{"id":"https://openalex.org/T10274","display_name":"Heterocyclic Compound Synthesis and Bioactivity","score":0.10360000282526016,"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"}},{"id":"https://openalex.org/T11178","display_name":"Receptor Mechanisms and Signaling","score":0.09589999914169312,"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"}}],"keywords":[{"id":"https://openalex.org/keywords/histamine-h3-receptor","display_name":"histamine H3 receptor","score":0.9620000123977661},{"id":"https://openalex.org/keywords/inverse-agonists","display_name":"inverse agonists","score":0.9950000047683716},{"id":"https://openalex.org/keywords/structure-activity-relationship","display_name":"structure-activity relationship","score":0.9559999704360962},{"id":"https://openalex.org/keywords/pyrrolidine-derivatives","display_name":"pyrrolidine derivatives","score":0.8119999766349792},{"id":"https://openalex.org/keywords/brain-penetration","display_name":"brain penetration","score":0.7170000076293945},{"id":"https://openalex.org/keywords/pharmacokinetics","display_name":"pharmacokinetics","score":0.9750000238418579}],"concepts":[{"id":"https://openalex.org/C63180777","wikidata":"https://www.wikidata.org/wiki/Q288395","display_name":"Histamine H3 receptor","level":4,"score":0.9550900459289551},{"id":"https://openalex.org/C89951826","wikidata":"https://www.wikidata.org/wiki/Q1671731","display_name":"Inverse agonist","level":4,"score":0.8994172811508179},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.8760404586791992},{"id":"https://openalex.org/C1122143","wikidata":"https://www.wikidata.org/wiki/Q61233","display_name":"Histamine","level":2,"score":0.8335351943969727},{"id":"https://openalex.org/C2778938600","wikidata":"https://www.wikidata.org/wiki/Q389934","display_name":"Agonist","level":3,"score":0.7229684591293335},{"id":"https://openalex.org/C170493617","wikidata":"https://www.wikidata.org/wiki/Q208467","display_name":"Receptor","level":2,"score":0.5613012313842773},{"id":"https://openalex.org/C112705442","wikidata":"https://www.wikidata.org/wiki/Q323936","display_name":"Pharmacokinetics","level":2,"score":0.46426156163215637},{"id":"https://openalex.org/C71240020","wikidata":"https://www.wikidata.org/wiki/Q186011","display_name":"Stereochemistry","level":1,"score":0.4642072319984436},{"id":"https://openalex.org/C2778851528","wikidata":"https://www.wikidata.org/wiki/Q408898","display_name":"Pyrrolidine","level":2,"score":0.4585966169834137},{"id":"https://openalex.org/C114373084","wikidata":"https://www.wikidata.org/wiki/Q273499","display_name":"Chemical synthesis","level":3,"score":0.4468718469142914},{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.438377320766449},{"id":"https://openalex.org/C2777056448","wikidata":"https://www.wikidata.org/wiki/Q285166","display_name":"Oral administration","level":2,"score":0.43654438853263855},{"id":"https://openalex.org/C202751555","wikidata":"https://www.wikidata.org/wiki/Q221681","display_name":"In vitro","level":2,"score":0.2831951975822449},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.2502995431423187},{"id":"https://openalex.org/C71924100","wikidata":"https://www.wikidata.org/wiki/Q11190","display_name":"Medicine","level":0,"score":0.0}],"mesh":[{"descriptor_ui":"D000072237","descriptor_name":"ERG1 Potassium Channel","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D000284","descriptor_name":"Administration, Oral","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D000818","descriptor_name":"Animals","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D001921","descriptor_name":"Brain","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D002626","descriptor_name":"Chemistry, Pharmaceutical","qualifier_ui":"Q000379","qualifier_name":"methods","is_major_topic":true},{"descriptor_ui":"D006801","descriptor_name":"Humans","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D008956","descriptor_name":"Models, Chemical","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D010075","descriptor_name":"Oxathiins","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":true},{"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":"D015195","descriptor_name":"Drug Design","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D017207","descriptor_name":"Rats, Sprague-Dawley","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D018100","descriptor_name":"Receptors, Histamine H3","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":true},{"descriptor_ui":"D020128","descriptor_name":"Inhibitory Concentration 50","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},{"descriptor_ui":"D051638","descriptor_name":"Ether-A-Go-Go Potassium Channels","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false}],"locations_count":2,"locations":[{"id":"doi:10.1016/j.bmcl.2009.05.101","doi":"https://doi.org/10.1016/j.bmcl.2009.05.101","is_oa":false,"landing_page_url":"https://doi.org/10.1016/j.bmcl.2009.05.101","pdf_url":null,"source":{"id":"https://openalex.org/S30970080","display_name":"Bioorganic & Medicinal Chemistry Letters","issn_l":"0960-894X","issn":["0960-894X","1464-3405"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-b","jufo-1","ki-jl-1","medline","norway-1","poland-70","russia-white-list-2","vabb-shw"],"host_organization":"https://openalex.org/P4310320990","host_organization_name":"Elsevier BV","host_organization_lineage":["https://openalex.org/P4310320990"],"host_organization_lineage_names":["Elsevier BV"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Bioorganic & Medicinal Chemistry Letters","raw_type":"journal-article"},{"id":"pmid:19520574","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/19520574","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":"Bioorganic & medicinal chemistry letters","raw_type":"Journal Article"}],"best_oa_location":null,"sustainable_development_goals":[{"display_name":"Good health and well-being","id":"https://metadata.un.org/sdg/3","score":0.6240000128746033}],"study_designs":[],"awards":[],"funders":[],"has_content":{"pdf":false,"grobid_xml":false},"content_urls":null,"referenced_works_count":38,"referenced_works":["https://openalex.org/W1571956553","https://openalex.org/W1586404244","https://openalex.org/W1919779618","https://openalex.org/W1970311780","https://openalex.org/W1990471091","https://openalex.org/W1992282620","https://openalex.org/W1993068126","https://openalex.org/W2003089715","https://openalex.org/W2008838316","https://openalex.org/W2016079923","https://openalex.org/W2016934701","https://openalex.org/W2018597141","https://openalex.org/W2033702340","https://openalex.org/W2034697832","https://openalex.org/W2041722434","https://openalex.org/W2046818662","https://openalex.org/W2059191263","https://openalex.org/W2060204812","https://openalex.org/W2061409645","https://openalex.org/W2070678202","https://openalex.org/W2073821618","https://openalex.org/W2075962215","https://openalex.org/W2076514006","https://openalex.org/W2077687762","https://openalex.org/W2078855866","https://openalex.org/W2085596664","https://openalex.org/W2091020918","https://openalex.org/W2096162880","https://openalex.org/W2102773142","https://openalex.org/W2129233012","https://openalex.org/W2130900903","https://openalex.org/W2131894174","https://openalex.org/W2133232647","https://openalex.org/W2137534575","https://openalex.org/W2139335899","https://openalex.org/W2165663580","https://openalex.org/W2167169197","https://openalex.org/W3022526165"],"related_works":["https://openalex.org/W1992282620","https://openalex.org/W2078855866","https://openalex.org/W2019696218","https://openalex.org/W2055769195","https://openalex.org/W2324683287","https://openalex.org/W1987580387","https://openalex.org/W2016934701","https://openalex.org/W2087446502","https://openalex.org/W2075962215","https://openalex.org/W2142079565"],"abstract_inverted_index":null,"counts_by_year":[{"year":2023,"cited_by_count":1},{"year":2020,"cited_by_count":2},{"year":2018,"cited_by_count":1},{"year":2017,"cited_by_count":2},{"year":2016,"cited_by_count":2}],"updated_date":"2026-11-04T10:54:05.112534","created_date":"2016-06-24T00:00:00"}