{"id":"https://openalex.org/W2584460023","doi":null,"title":"The synthesis and biological evaluation of a novel class of butyrylcholinesterase inhibitors using isosorbide as a building block","display_name":"The synthesis and biological evaluation of a novel class of butyrylcholinesterase inhibitors using isosorbide as a building block","publication_year":2007,"publication_date":"2007-01-01","ids":{"openalex":"https://openalex.org/W2584460023","mag":"2584460023"},"language":"en","primary_location":{"id":"pmh:http://www.rian.ie/133235/","doi":null,"is_oa":false,"landing_page_url":"http://hdl.handle.net/2262/77951","pdf_url":null,"source":{"id":"https://openalex.org/S4306400033","display_name":"Arrow@dit (Dublin Institute of Technology)","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I4210144925","host_organization_name":"Technological University Dublin","host_organization_lineage":["https://openalex.org/I4210144925"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"submittedVersion","is_accepted":false,"is_published":false,"raw_source_name":"Gerald Dillon, 'The synthesis and biological evaluation of a novel class of butyrylcholinesterase inhibitors using isosorbide as a building block', [thesis], Trinity College (Dublin, Ireland). School of Pharmacy &amp; Pharmaceutical Sciences, 2007, pp 297","raw_type":"Doctoral thesis"},"volume":null,"type":"dissertation","is_traditional":true,"indexed_in":[],"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/A5049547436","display_name":"Gerald Patrick Dillon","orcid":"https://orcid.org/0000-0001-7544-6339","observed_orcids":["https://orcid.org/0000-0001-7544-6339"]},"institutions":[],"countries":[],"is_corresponding":true,"raw_author_name":"Gerald Patrick Dillon","raw_affiliation_strings":[],"raw_orcid":"https://orcid.org/0000-0001-7544-6339","affiliations":[]}],"institutions":[],"countries_distinct_count":0,"institutions_distinct_count":0,"corresponding_author_ids":["https://openalex.org/A5049547436"],"corresponding_institution_ids":[],"apc_list":null,"apc_paid":null,"fwci":null,"has_fulltext":false,"cited_by_count":1,"citation_normalized_percentile":null,"cited_by_percentile_year":null,"biblio":{"volume":null,"issue":null,"first_page":null,"last_page":null},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T12023","display_name":"Cholinesterase and Neurodegenerative Diseases","score":1.0,"subfield":{"id":"https://openalex.org/subfields/2736","display_name":"Pharmacology (medical)"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}},"topics":[{"id":"https://openalex.org/T12023","display_name":"Cholinesterase and Neurodegenerative Diseases","score":1.0,"subfield":{"id":"https://openalex.org/subfields/2736","display_name":"Pharmacology (medical)"},"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/T12412","display_name":"Enzyme function and inhibition","score":0.0,"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":0.0,"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/butyrylcholinesterase-inhibitors","display_name":"butyrylcholinesterase inhibitors","score":0.9900000095367432},{"id":"https://openalex.org/keywords/carbamate-inhibitors","display_name":"carbamate inhibitors","score":0.6769999861717224},{"id":"https://openalex.org/keywords/acetylcholinesterase","display_name":"acetylcholinesterase","score":0.828000009059906},{"id":"https://openalex.org/keywords/alzheimer-s-disease","display_name":"Alzheimer's disease","score":0.9610000252723694},{"id":"https://openalex.org/keywords/enzyme-inhibition","display_name":"enzyme inhibition","score":0.7279999852180481},{"id":"https://openalex.org/keywords/structure-activity-relationship","display_name":"structure-activity relationship","score":0.6100000143051147},{"id":"https://openalex.org/keywords/benzyl-substitution","display_name":"benzyl substitution","score":0.4320000112056732},{"id":"https://openalex.org/keywords/cholinesterase-inhibitors","display_name":"cholinesterase inhibitors","score":0.5260000228881836},{"id":"https://openalex.org/keywords/drug-design","display_name":"drug design","score":0.3580000102519989}],"concepts":[{"id":"https://openalex.org/C2779101902","wikidata":"https://www.wikidata.org/wiki/Q22679015","display_name":"Butyrylcholinesterase","level":5,"score":0.7695791721343994},{"id":"https://openalex.org/C2777210771","wikidata":"https://www.wikidata.org/wiki/Q4927124","display_name":"Block (permutation group theory)","level":2,"score":0.6232120394706726},{"id":"https://openalex.org/C2778949068","wikidata":"https://www.wikidata.org/wiki/Q179748","display_name":"Isosorbide dinitrate","level":2,"score":0.5992403030395508},{"id":"https://openalex.org/C2777212361","wikidata":"https://www.wikidata.org/wiki/Q5127848","display_name":"Class (philosophy)","level":2,"score":0.560638427734375},{"id":"https://openalex.org/C2776915459","wikidata":"https://www.wikidata.org/wiki/Q1243800","display_name":"Isosorbide","level":2,"score":0.43859851360321045},{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.37467920780181885},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.36310505867004395},{"id":"https://openalex.org/C71924100","wikidata":"https://www.wikidata.org/wiki/Q11190","display_name":"Medicine","level":0,"score":0.3352842926979065},{"id":"https://openalex.org/C41008148","wikidata":"https://www.wikidata.org/wiki/Q21198","display_name":"Computer science","level":0,"score":0.24778667092323303},{"id":"https://openalex.org/C126322002","wikidata":"https://www.wikidata.org/wiki/Q11180","display_name":"Internal medicine","level":1,"score":0.2340070903301239},{"id":"https://openalex.org/C33923547","wikidata":"https://www.wikidata.org/wiki/Q395","display_name":"Mathematics","level":0,"score":0.1941136121749878},{"id":"https://openalex.org/C178790620","wikidata":"https://www.wikidata.org/wiki/Q11351","display_name":"Organic chemistry","level":1,"score":0.19194239377975464},{"id":"https://openalex.org/C154945302","wikidata":"https://www.wikidata.org/wiki/Q11660","display_name":"Artificial intelligence","level":1,"score":0.11416590213775635},{"id":"https://openalex.org/C181199279","wikidata":"https://www.wikidata.org/wiki/Q8047","display_name":"Enzyme","level":2,"score":0.07081344723701477},{"id":"https://openalex.org/C2778816929","wikidata":"https://www.wikidata.org/wiki/Q22676679","display_name":"Acetylcholinesterase","level":3,"score":0.05476534366607666},{"id":"https://openalex.org/C2779059548","wikidata":"https://www.wikidata.org/wiki/Q383701","display_name":"Ach\u00e9","level":4,"score":0.0},{"id":"https://openalex.org/C2524010","wikidata":"https://www.wikidata.org/wiki/Q8087","display_name":"Geometry","level":1,"score":0.0}],"mesh":[],"locations_count":2,"locations":[{"id":"pmh:http://www.rian.ie/133235/","doi":null,"is_oa":false,"landing_page_url":"http://hdl.handle.net/2262/77951","pdf_url":null,"source":{"id":"https://openalex.org/S4306400033","display_name":"Arrow@dit (Dublin Institute of Technology)","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I4210144925","host_organization_name":"Technological University Dublin","host_organization_lineage":["https://openalex.org/I4210144925"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"submittedVersion","is_accepted":false,"is_published":false,"raw_source_name":"Gerald Dillon, 'The synthesis and biological evaluation of a novel class of butyrylcholinesterase inhibitors using isosorbide as a building block', [thesis], Trinity College (Dublin, Ireland). School of Pharmacy &amp; Pharmaceutical Sciences, 2007, pp 297","raw_type":"Doctoral thesis"},{"id":"mag:2584460023","doi":null,"is_oa":false,"landing_page_url":"http://www.tara.tcd.ie/handle/2262/77951","pdf_url":null,"source":null,"license":null,"license_id":null,"version":null,"is_accepted":false,"is_published":false,"raw_source_name":null,"raw_type":null}],"best_oa_location":null,"sustainable_development_goals":[{"id":"https://metadata.un.org/sdg/3","score":0.428600013256073,"display_name":"Good health and well-being"}],"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/W2588748646","https://openalex.org/W1983368608","https://openalex.org/W2590177070","https://openalex.org/W3196602412","https://openalex.org/W3004925615","https://openalex.org/W7056519648","https://openalex.org/W4404590776","https://openalex.org/W2131754369","https://openalex.org/W1988410641","https://openalex.org/W2950259598"],"abstract_inverted_index":{"The":[0,143,347],"aim":[1],"of":[2,13,31,55,84,94,98,112,117,127,131,141,145,158,171,176,191,212,220,226,250,258,271,291,301,314,325,329,355,363,369,383],"this":[3,118,350],"project":[4],"was":[5,150,182,333,339],"to":[6,26,209,231,287],"synthesise":[7],"and":[8,25,48,62,173,188,216,235,269,281,312,366,376,385],"optimise":[9],"a":[10,22,74,105,168,203,242,336,353,361],"novel":[11,278],"class":[12],"cholinesterase":[14],"inhibitors":[15,149,190,290,368],"using":[16],"the":[17,28,79,81,91,110,125,128,139,153,198,218,221,256,267,294,310,323,340,372],"simple":[18],"sugar,":[19],"isosorbide,":[20,330],"as":[21,87,135,232,331],"building":[23],"block":[24],"assess":[27],"inhibitory":[29],"activity":[30],"these":[32,177],"compounds":[33,178,227,374],"in":[34,78,279,284,321,345,349],"vitro.":[35],"Cholinesterases":[36],"are":[37,52,120,160],"enzymes":[38],"that":[39,71,155,185,335],"can":[40],"hydrolyse":[41],"choline":[42,49],"esters":[43],"into":[44],"their":[45],"respective":[46],"acid":[47],"portions.":[50],"There":[51],"two":[53],"types":[54],"cholinesterases,":[56],"namely,":[57],"acetylcholinesterase":[58],"(AChE)":[59],"[E.C.":[60],"3.1.1.7]":[61],"butyrylcholinesterase":[63],"(BuChE)":[64],"[B.C.":[65],"3.1.1.8].":[66],"While":[67],"it":[68,332],"is":[69,207],"known":[70],"AChE":[72],"has":[73],"specific":[75],"biological":[76,82,129],"role":[77,130],"body,":[80],"function":[83],"BuChE":[85,108,132,163,192,215],"is,":[86],"yet,":[88],"unclear.":[89],"In":[90],"last":[92],"number":[93],"years,":[95],"several":[96],"lines":[97],"medical":[99],"research":[100],"have":[101],"independently":[102],"reported":[103],"upon":[104],"link":[106],"associating":[107],"with":[109,164,202,214,293,318,371],"onset":[111],"Alzheimer\u2019s":[113],"disease":[114],"(AD).":[115],"Inhibitors":[116],"enzyme":[119],"therefore":[121,183],"highly":[122,186,364],"desirable":[123],"for":[124,138,179,304,343,381],"elucidation":[126],"but":[133],"also,":[134],"potential":[136],"therapeutics":[137],"treatment":[140],"AD.":[142],"design":[144],"huBuChE":[146,370,382],"(human":[147],"butyrylcholinesterase)":[148],"based":[151],"on":[152,255,309],"discovery":[154],"2-ester":[156,200],"derivatives":[157],"isosorbide":[159],"hydrolysed":[161],"by":[162,196],"exceptional":[165],"rapidity,":[166],"demonstrating":[167],"high":[169],"level":[170],"affinity":[172],"molecular":[174],"recognition":[175],"BuChE.":[180],"It":[181],"proposed":[184],"potent":[187,365],"selective":[189,367],"could":[193],"be":[194,210,288],"synthesised":[195],"replacing":[197],"vulnerable":[199],"group":[201,233,236,247,259,315,342],"carbamate":[204,243,338],"group,":[205],"which":[206,239,275,282,359],"understood":[208],"capable":[211],"interacting":[213],"causing":[217],"inhibition":[219,344],"enzyme.":[222],"Two":[223],"initial":[224],"families":[225],"were":[228,276],"synthesised,":[229],"referred":[230],"1":[234,316],"2":[237,253,260],"compounds,":[238,274,358],"possessed":[240],"either":[241],"or":[244],"'reversed":[245,261],"carbamate'":[246,262],"at":[248,327],"position-2":[249],"isosorbide.":[251],"Chapter":[252,306],"focuses":[254,308],"development":[257],"compounds.":[263],"This":[264],"chapter":[265,351],"describes":[266],"synthesis":[268,311],"evaluation":[270,313],"17":[272],"test":[273,357],"completely":[277],"structure":[280],"transpired,":[283],"some":[285],"cases,":[286],"moderate":[289],"huBuChE,":[292],"lead":[295,373],"compound":[296],"106":[297],"having":[298,378],"an":[299],"IC50":[300,379],"1.5":[302],"[iM":[303],"huBuChE.":[305],"3":[307],"carbamates,":[317],"particular":[319],"emphasis":[320],"optimising":[322],"type":[324],"substitution":[326],"position-5":[328],"found":[334],"benzyl":[337],"optimum":[341],"position-2.":[346],"work":[348],"produced":[352],"total":[354],"29":[356],"includes":[360],"range":[362],"121":[375],"124":[377],"values":[380],"5.77":[384],"12.33":[386],"nM":[387],"respectively.":[388]},"counts_by_year":[{"year":2019,"cited_by_count":1}],"updated_date":"2026-11-09T13:22:03.289127","created_date":"2017-02-10T00:00:00"}
