{"id":"https://openalex.org/W2949879563","doi":"https://doi.org/10.3987/com-95-s91","title":"New Approach to the Imidazolutidine Moiety of MK-996","display_name":"New Approach to the Imidazolutidine Moiety of MK-996","publication_year":1996,"publication_date":"1996-01-01","ids":{"openalex":"https://openalex.org/W2949879563","doi":"https://doi.org/10.3987/com-95-s91","mag":"2949879563"},"language":"en","primary_location":{"id":"doi:10.3987/com-95-s91","doi":"https://doi.org/10.3987/com-95-s91","is_oa":true,"landing_page_url":"https://doi.org/10.3987/com-95-s91","pdf_url":null,"source":{"id":"https://openalex.org/S27298842","display_name":"Heterocycles","issn_l":"0385-5414","issn":["0385-5414","1881-0942"],"is_oa":true,"is_in_doaj":false,"is_core":true,"listed_in":["cwts-core","jufo-1","norway-1","poland-40","russia-white-list-4"],"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":"HETEROCYCLES","raw_type":"journal-article"},"volume":null,"type":"article","indexed_in":["crossref"],"open_access":{"is_oa":true,"oa_status":"diamond","oa_url":"https://doi.org/10.3987/com-95-s91","any_repository_has_fulltext":false},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5015397568","display_name":"Chris H. Senanayake","orcid":"https://orcid.org/0009-0009-3170-0687","observed_orcids":["https://orcid.org/0009-0009-3170-0687"]},"institutions":[{"id":"https://openalex.org/I1285764155","display_name":"Merck & Co., Inc., Rahway, NJ, USA (United States)","ror":"https://ror.org/02891sr49","country_code":"US","type":"company","lineage":["https://openalex.org/I1285764155"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Chris H. Senanayake","raw_affiliation_strings":["Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA","institution_ids":["https://openalex.org/I1285764155"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5042103099","display_name":"Laura E. Fredenburgh","orcid":"https://orcid.org/0000-0002-7447-6453","observed_orcids":["https://orcid.org/0000-0002-7447-6453"]},"institutions":[{"id":"https://openalex.org/I1285764155","display_name":"Merck & Co., Inc., Rahway, NJ, USA (United States)","ror":"https://ror.org/02891sr49","country_code":"US","type":"company","lineage":["https://openalex.org/I1285764155"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Laura E. Fredenburgh","raw_affiliation_strings":["Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA","institution_ids":["https://openalex.org/I1285764155"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5082528423","display_name":"Robert A. Reamer","orcid":"https://orcid.org/0000-0003-3371-2429","observed_orcids":["https://orcid.org/0000-0003-3371-2429"]},"institutions":[{"id":"https://openalex.org/I1285764155","display_name":"Merck & Co., Inc., Rahway, NJ, USA (United States)","ror":"https://ror.org/02891sr49","country_code":"US","type":"company","lineage":["https://openalex.org/I1285764155"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Robert A. Reamer","raw_affiliation_strings":["Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA","institution_ids":["https://openalex.org/I1285764155"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5100626177","display_name":"Liu Ji","orcid":"https://orcid.org/0000-0002-2528-2839","observed_orcids":["https://orcid.org/0000-0002-2528-2839"]},"institutions":[{"id":"https://openalex.org/I1285764155","display_name":"Merck & Co., Inc., Rahway, NJ, USA (United States)","ror":"https://ror.org/02891sr49","country_code":"US","type":"company","lineage":["https://openalex.org/I1285764155"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Ji Liu","raw_affiliation_strings":["Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA","institution_ids":["https://openalex.org/I1285764155"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5007910071","display_name":"F. E. ROBERTS","orcid":"https://orcid.org/0000-0002-2054-8933","observed_orcids":["https://orcid.org/0000-0002-2054-8933"]},"institutions":[{"id":"https://openalex.org/I1285764155","display_name":"Merck & Co., Inc., Rahway, NJ, USA (United States)","ror":"https://ror.org/02891sr49","country_code":"US","type":"company","lineage":["https://openalex.org/I1285764155"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"F. Edward Roberts","raw_affiliation_strings":["Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA","institution_ids":["https://openalex.org/I1285764155"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5097187271","display_name":"Guy Humphery","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I1285764155","display_name":"Merck & Co., Inc., Rahway, NJ, USA (United States)","ror":"https://ror.org/02891sr49","country_code":"US","type":"company","lineage":["https://openalex.org/I1285764155"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Guy Humphery","raw_affiliation_strings":["Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA","institution_ids":["https://openalex.org/I1285764155"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5074826873","display_name":"Andrew S. Thompson","orcid":"https://orcid.org/0009-0004-2715-4891","observed_orcids":["https://orcid.org/0009-0004-2715-4891"]},"institutions":[{"id":"https://openalex.org/I1285764155","display_name":"Merck & Co., Inc., Rahway, NJ, USA (United States)","ror":"https://ror.org/02891sr49","country_code":"US","type":"company","lineage":["https://openalex.org/I1285764155"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Andrew S. Thompson","raw_affiliation_strings":["Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA","institution_ids":["https://openalex.org/I1285764155"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5049859356","display_name":"Robert D. Larsen","orcid":"https://orcid.org/0000-0002-9697-4955","observed_orcids":["https://orcid.org/0000-0002-9697-4955"]},"institutions":[{"id":"https://openalex.org/I1285764155","display_name":"Merck & Co., Inc., Rahway, NJ, USA (United States)","ror":"https://ror.org/02891sr49","country_code":"US","type":"company","lineage":["https://openalex.org/I1285764155"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Robert D. Larsen","raw_affiliation_strings":["Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA","institution_ids":["https://openalex.org/I1285764155"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5084108294","display_name":"Thomas R. Verhoeven","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I1285764155","display_name":"Merck & Co., Inc., Rahway, NJ, USA (United States)","ror":"https://ror.org/02891sr49","country_code":"US","type":"company","lineage":["https://openalex.org/I1285764155"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Thomas R. Verhoeven","raw_affiliation_strings":["Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA","institution_ids":["https://openalex.org/I1285764155"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5084347682","display_name":"Paul J. Reider","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I1285764155","display_name":"Merck & Co., Inc., Rahway, NJ, USA (United States)","ror":"https://ror.org/02891sr49","country_code":"US","type":"company","lineage":["https://openalex.org/I1285764155"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Paul J. Reider","raw_affiliation_strings":["Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA","institution_ids":["https://openalex.org/I1285764155"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5097102836","display_name":"Ichiro Sinkai","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I1285764155","display_name":"Merck & Co., Inc., Rahway, NJ, USA (United States)","ror":"https://ror.org/02891sr49","country_code":"US","type":"company","lineage":["https://openalex.org/I1285764155"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Ichiro Sinkai","raw_affiliation_strings":["Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Process Research, Merck Research Laboratories, Division of Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA","institution_ids":["https://openalex.org/I1285764155"]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":1,"corresponding_author_ids":[],"corresponding_institution_ids":["https://openalex.org/I1285764155"],"apc_list":null,"apc_paid":null,"fwci":0.5994,"has_fulltext":false,"cited_by_count":15,"citation_normalized_percentile":{"value":0.64360047,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":88,"max":94},"biblio":{"volume":"42","issue":"2","first_page":"821","last_page":"821"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T14459","display_name":"Synthesis and Reactions of Organic Compounds","score":0.4133000075817108,"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"}},"topics":[{"id":"https://openalex.org/T14459","display_name":"Synthesis and Reactions of Organic Compounds","score":0.4133000075817108,"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/T11001","display_name":"Renin-Angiotensin System Studies","score":0.28760001063346863,"subfield":{"id":"https://openalex.org/subfields/2705","display_name":"Cardiology and Cardiovascular Medicine"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}},{"id":"https://openalex.org/T13649","display_name":"Advanced Synthetic Organic Chemistry","score":0.10859999805688858,"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/malonamide","display_name":"malonamide","score":0.5329999923706055},{"id":"https://openalex.org/keywords/acetylacetone","display_name":"acetylacetone","score":0.9350000023841858},{"id":"https://openalex.org/keywords/regioselective-synthesis","display_name":"regioselective synthesis","score":0.9330000281333923},{"id":"https://openalex.org/keywords/renin-angiotensin-system","display_name":"renin-angiotensin system","score":0.9089999794960022},{"id":"https://openalex.org/keywords/angiotensin-ii-receptor-antagonism","display_name":"angiotensin II receptor antagonism","score":0.8610000014305115},{"id":"https://openalex.org/keywords/angiotensin-ii-type-1-receptor","display_name":"angiotensin II type 1 receptor","score":0.8519999980926514},{"id":"https://openalex.org/keywords/hypertension","display_name":"hypertension","score":0.6620000004768372},{"id":"https://openalex.org/keywords/ace-inhibitors","display_name":"ACE inhibitors","score":0.7459999918937683}],"concepts":[{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.9592489004135132},{"id":"https://openalex.org/C2776568683","wikidata":"https://www.wikidata.org/wiki/Q23005640","display_name":"Moiety","level":2,"score":0.861498236656189},{"id":"https://openalex.org/C71240020","wikidata":"https://www.wikidata.org/wiki/Q186011","display_name":"Stereochemistry","level":1,"score":0.5324640870094299},{"id":"https://openalex.org/C21951064","wikidata":"https://www.wikidata.org/wiki/Q899212","display_name":"Combinatorial chemistry","level":1,"score":0.3552819490432739}],"mesh":[],"locations_count":1,"locations":[{"id":"doi:10.3987/com-95-s91","doi":"https://doi.org/10.3987/com-95-s91","is_oa":true,"landing_page_url":"https://doi.org/10.3987/com-95-s91","pdf_url":null,"source":{"id":"https://openalex.org/S27298842","display_name":"Heterocycles","issn_l":"0385-5414","issn":["0385-5414","1881-0942"],"is_oa":true,"is_in_doaj":false,"is_core":true,"listed_in":["cwts-core","jufo-1","norway-1","poland-40","russia-white-list-4"],"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":"HETEROCYCLES","raw_type":"journal-article"}],"best_oa_location":{"id":"doi:10.3987/com-95-s91","doi":"https://doi.org/10.3987/com-95-s91","is_oa":true,"landing_page_url":"https://doi.org/10.3987/com-95-s91","pdf_url":null,"source":{"id":"https://openalex.org/S27298842","display_name":"Heterocycles","issn_l":"0385-5414","issn":["0385-5414","1881-0942"],"is_oa":true,"is_in_doaj":false,"is_core":true,"listed_in":["cwts-core","jufo-1","norway-1","poland-40","russia-white-list-4"],"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":"HETEROCYCLES","raw_type":"journal-article"},"sustainable_development_goals":[{"display_name":"Good health and well-being","id":"https://metadata.un.org/sdg/3","score":0.8560000061988831}],"study_designs":[],"awards":[],"funders":[],"has_content":{"grobid_xml":false,"pdf":false},"content_urls":null,"referenced_works_count":0,"referenced_works":[],"related_works":["https://openalex.org/W1997274592","https://openalex.org/W174152796","https://openalex.org/W2005374073","https://openalex.org/W7052966118","https://openalex.org/W2952795355","https://openalex.org/W1978806597","https://openalex.org/W2952682160","https://openalex.org/W6998005028","https://openalex.org/W2046232235","https://openalex.org/W2312995831"],"abstract_inverted_index":{"A":[0],"highly":[1],"effective,":[2],"regio-selective":[3],"synthesis":[4],"of":[5,40,78,83],"imidawlutidine":[6],"(1)":[7],"is":[8,21,55,81],"described":[9],"starting":[10],"from":[11],"readily":[12],"available":[13],"malonamamidine":[14],"hydrochloride":[15],"and":[16,35,44],"2,4pentanedione.The":[17],"renin-angiotensin":[18],"system":[19],"(RAS)":[20],"a":[22,33,56,94],"crucial":[23],"mechanism":[24],"that":[25,48,60,70],"regulate":[26],"blood":[27],"pressure":[28],"in":[29],"~~o":[30],"r":[31],"m":[32],"l":[34],"pathophysiological":[36],"states.'This":[37],"cascade":[38],"consists":[39],"two":[41],"enzymes,":[42],"renin":[43],"angiotensin-convening":[45],"enzyme":[46],"(ACE),":[47],"convert":[49],"angiotensinogen":[50],"to":[51,92],"angiotensin":[52,85],"I1":[53],"(AII).2A11":[54],"powerful":[57],"arterial":[58],"vasoconsaictor":[59],"exerts":[61],"its":[62],"action":[63],"by":[64],"interacting":[65],"with":[66],"specific":[67],"receptors":[68],"(AT1)":[69],"are":[71],"present":[72],"on":[73],"cell":[74],"membranes.One":[75],"possible":[76],"mode":[77],"controlling":[79],"hypertension":[80],"antagonisim":[82],"the":[84],"11":[86],"receptor3":[87],"Recently,":[88],"MK-9964":[89],"was":[90],"discovered":[91],"be":[93],"potent,":[95],"nonpeptidic,":[96],"orally":[97],"active":[98],"AT1-selective":[99],"All":[100],"antagonist.":[101]},"counts_by_year":[{"year":2022,"cited_by_count":1},{"year":2021,"cited_by_count":1},{"year":2019,"cited_by_count":1},{"year":2017,"cited_by_count":1},{"year":2012,"cited_by_count":1}],"updated_date":"2026-10-01T08:54:57.152042","created_date":"2019-06-27T00:00:00"}