{"id":"https://openalex.org/W652297349","doi":null,"title":"Design and synthesis of aspartyl protease inhibitors : Targeting HIV-1 and malaria plasmepsin I and II","display_name":"Design and synthesis of aspartyl protease inhibitors : Targeting HIV-1 and malaria plasmepsin I and II","publication_year":2003,"publication_date":"2003-01-01","ids":{"openalex":"https://openalex.org/W652297349","mag":"652297349"},"language":"en","primary_location":{"id":"pmh:oai:DiVA.org:uu-3288","doi":null,"is_oa":true,"landing_page_url":"http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-3288","pdf_url":null,"source":{"id":"https://openalex.org/S4306402042","display_name":"Uppsala University Publications (Uppsala University)","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I123387679","host_organization_name":"Uppsala University","host_organization_lineage":["https://openalex.org/I123387679"],"host_organization_lineage_names":[],"type":"repository"},"license":"other-oa","license_id":"https://openalex.org/licenses/other-oa","version":"submittedVersion","is_accepted":false,"is_published":false,"raw_source_name":"","raw_type":"info:eu-repo/semantics/doctoralThesis"},"volume":null,"type":"dissertation","is_traditional":true,"indexed_in":[],"open_access":{"is_oa":true,"oa_status":"green","oa_url":"http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-3288","any_repository_has_fulltext":true},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5066930684","display_name":"Daniel N\u00f6teberg","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":true,"raw_author_name":"Daniel N\u00f6teberg","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]}],"institutions":[],"countries_distinct_count":0,"institutions_distinct_count":0,"corresponding_author_ids":["https://openalex.org/A5066930684"],"corresponding_institution_ids":[],"apc_list":null,"apc_paid":null,"fwci":null,"has_fulltext":false,"cited_by_count":0,"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/T10620","display_name":"Protease and Inhibitor Mechanisms","score":0.6395999789237976,"subfield":{"id":"https://openalex.org/subfields/1306","display_name":"Cancer Research"},"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/T10620","display_name":"Protease and Inhibitor Mechanisms","score":0.6395999789237976,"subfield":{"id":"https://openalex.org/subfields/1306","display_name":"Cancer Research"},"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/T10911","display_name":"Chemical Synthesis and Analysis","score":0.2946999967098236,"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/T10526","display_name":"HIV/AIDS drug development and treatment","score":0.009800000116229057,"subfield":{"id":"https://openalex.org/subfields/2725","display_name":"Infectious Diseases"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}}],"keywords":[{"id":"https://openalex.org/keywords/aspartyl-protease-inhibitors","display_name":"aspartyl protease inhibitors","score":0.9909999966621399},{"id":"https://openalex.org/keywords/hiv-1-protease-inhibitors","display_name":"HIV-1 protease inhibitors","score":0.9169999957084656},{"id":"https://openalex.org/keywords/plasmepsin-ii","display_name":"plasmepsin II","score":1.0},{"id":"https://openalex.org/keywords/malaria","display_name":"malaria","score":0.625},{"id":"https://openalex.org/keywords/peptidomimetics","display_name":"peptidomimetics","score":0.9010000228881836},{"id":"https://openalex.org/keywords/anthranilic-acid","display_name":"anthranilic acid","score":0.8709999918937683},{"id":"https://openalex.org/keywords/cathepsin-d","display_name":"cathepsin D","score":0.8700000047683716},{"id":"https://openalex.org/keywords/structure-activity-relationship","display_name":"structure-activity relationship","score":0.6830000281333923},{"id":"https://openalex.org/keywords/hemoglobin-degradation","display_name":"hemoglobin degradation","score":0.4480000138282776},{"id":"https://openalex.org/keywords/tertiary-amines","display_name":"tertiary amines","score":0.4050000011920929}],"concepts":[{"id":"https://openalex.org/C2776714187","wikidata":"https://www.wikidata.org/wiki/Q212410","display_name":"Protease","level":3,"score":0.6371972560882568},{"id":"https://openalex.org/C2778048844","wikidata":"https://www.wikidata.org/wiki/Q12156","display_name":"Malaria","level":2,"score":0.6110100746154785},{"id":"https://openalex.org/C159047783","wikidata":"https://www.wikidata.org/wiki/Q7215","display_name":"Virology","level":1,"score":0.5425328612327576},{"id":"https://openalex.org/C3013748606","wikidata":"https://www.wikidata.org/wiki/Q15787","display_name":"Human immunodeficiency virus (HIV)","level":2,"score":0.49709370732307434},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.3865845501422882},{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.34351807832717896},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.3263133764266968},{"id":"https://openalex.org/C181199279","wikidata":"https://www.wikidata.org/wiki/Q8047","display_name":"Enzyme","level":2,"score":0.27680736780166626},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.2732517123222351},{"id":"https://openalex.org/C203014093","wikidata":"https://www.wikidata.org/wiki/Q101929","display_name":"Immunology","level":1,"score":0.1775299608707428}],"mesh":[],"locations_count":2,"locations":[{"id":"pmh:oai:DiVA.org:uu-3288","doi":null,"is_oa":true,"landing_page_url":"http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-3288","pdf_url":null,"source":{"id":"https://openalex.org/S4306402042","display_name":"Uppsala University Publications (Uppsala University)","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I123387679","host_organization_name":"Uppsala University","host_organization_lineage":["https://openalex.org/I123387679"],"host_organization_lineage_names":[],"type":"repository"},"license":"other-oa","license_id":"https://openalex.org/licenses/other-oa","version":"submittedVersion","is_accepted":false,"is_published":false,"raw_source_name":"","raw_type":"info:eu-repo/semantics/doctoralThesis"},{"id":"mag:652297349","doi":null,"is_oa":false,"landing_page_url":"http://uu.diva-portal.org/smash/get/diva2:162323/FULLTEXT01","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":{"id":"pmh:oai:DiVA.org:uu-3288","doi":null,"is_oa":true,"landing_page_url":"http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-3288","pdf_url":null,"source":{"id":"https://openalex.org/S4306402042","display_name":"Uppsala University Publications (Uppsala University)","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I123387679","host_organization_name":"Uppsala University","host_organization_lineage":["https://openalex.org/I123387679"],"host_organization_lineage_names":[],"type":"repository"},"license":"other-oa","license_id":"https://openalex.org/licenses/other-oa","version":"submittedVersion","is_accepted":false,"is_published":false,"raw_source_name":"","raw_type":"info:eu-repo/semantics/doctoralThesis"},"sustainable_development_goals":[{"display_name":"Good health and well-being","score":0.46810001134872437,"id":"https://metadata.un.org/sdg/3"}],"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/W2085364947","https://openalex.org/W7072013984","https://openalex.org/W1999308385","https://openalex.org/W2057862446","https://openalex.org/W2013520316","https://openalex.org/W2021881285","https://openalex.org/W2114742412","https://openalex.org/W2513285393","https://openalex.org/W2134418875","https://openalex.org/W2076427899"],"abstract_inverted_index":{"Aspartyl":[0],"proteases":[1,48,162],"can":[2],"generally":[3],"be":[4,301,343,398],"inhibited":[5],"by":[6],"peptide":[7,12,22,175],"mimics":[8,176],"containing":[9],"an":[10,84,88],"uncleavable":[11],"bond":[13,23],"isostere":[14,24],"at":[15,253],"the":[16,26,41,46,60,77,110,120,127,136,154,160,178,191,198,201,205,219,227,230,241,246,258,278,304,308,311,316,319,324,353,366,373,382,394],"proposed":[17],"cleavage":[18],"site.":[19],"One":[20],"such":[21],"is":[25,74,141,153,208,348],"hydroxyethylamine":[27,179],"moiety,":[28],"which":[29,103,222,347],"in":[30,37,164,226,240,294,349],"this":[31,165,329,340],"thesis":[32],"has":[33,58],"successfully":[34],"been":[35],"incorporated":[36],"potential":[38],"inhibitors":[39,392],"of":[40,76,100,119,131,134,159,174,204,221,229,268,277,285,291,307,318,335,359,372,379,393],"HIV-1-protease":[42],"as":[43,45,124,187,189],"well":[44,188],"malarial":[47],"plasmepsin":[49,168],"I":[50,169],"and":[51,170,182,215,248,255,298],"II.":[52,171],"The":[53,71,333],"human":[54,193,296,395],"immunodeficiency":[55],"virus":[56,72],"(HIV)":[57],"during":[59],"last":[61],"20":[62],"years":[63],"given":[64],"rise":[65],"to":[66,86,126,224,300,323,352],"a":[67,91,114,209,266,330,362,376,389],"new":[68,148],"fast-spread":[69],"epidemic.":[70],"protease":[73,194],"one":[75],"foremost":[78],"targets":[79],"for":[80,96,150,289,381],"drug":[81,151],"intervention.":[82],"In":[83,197,303],"attempt":[85],"improve":[87],"earlier":[89],"design,":[90],"P1'-anthranilic":[92],"acid":[93,262],"was":[94,223,233,263,273,287,313],"exchanged":[95],"all":[97],"four":[98],"isomers":[99,112,121,358],"2-aminocyclopentanecarboxylic":[101],"acid,":[102],"were":[104,180,250,281],"synthesized":[105],"from":[106,213,315],"racemic":[107],"starting":[108],"materials,":[109],"trans":[111],"via":[113],"novel":[115],"synthetic":[116],"route.":[117],"None":[118],"enhanced":[122],"potency":[123],"compared":[125],"anthranilic":[128],"acid.":[129],"Because":[130],"increasing":[132],"development":[133],"resistance,":[135],"pharmaceutical":[137],"intervention":[138],"with":[139,177,265],"malaria":[140],"becoming":[142],"rapidly":[143],"more":[144],"difficult.":[145],"A":[146,283],"prominent":[147],"target":[149,206,305],"research":[152],"hemoglobin":[155],"degradation":[156],"pathway.":[157],"Two":[158,172],"many":[161,276],"involved":[163],"pathway":[166],"are":[167],"series":[173,200,310],"prepared":[181],"tested":[183,288],"against":[184,190],"these":[185,336],"enzymes":[186],"similar":[192],"cathepsin":[195,385],"D.":[196],"first":[199,354],"central":[202],"nitrogen":[203],"compounds":[207,286,306,337,374],"secondary":[210],"amine,":[211],"derived":[212],"natural":[214],"unnatural":[216],"amino":[217,321],"acids,":[218],"side-chain":[220,341],"bind":[225],"S1'-site":[228],"proteases.":[231],"It":[232,272],"found":[234,274,299],"that":[235,275,339],"para-aryl":[236],"substituted":[237],"phenylalanines":[238],"resulted":[239],"most":[242],"active":[243],"inhibitors.":[244],"While":[245],"P1-":[247],"P2-side-chains":[249],"kept":[251],"constant":[252],"benzyl":[254,363],"isopropyl":[256],"respectively,":[257],"P3":[259],"capping":[260],"carboxylic":[261,270,279],"varied":[264],"set":[267],"diverse":[269],"acids.":[271],"acids":[280,322],"acceptable.":[282],"selection":[284],"inhibition":[290],"parasite":[292],"growth":[293],"infected":[295],"erythrocytes":[297],"active.":[302],"second":[309],"P1'-side-chain":[312],"moved":[314],"\u03b1-carbon":[317],"initial":[320],"adjacent":[325],"nitrogen,":[326],"thus":[327],"rendering":[328],"tertiary":[331],"amine.":[332],"SAR":[334],"suggests":[338],"cannot":[342],"larger":[344],"than":[345],"benzyl,":[346],"sharp":[350],"contrast":[351],"series,":[355],"where":[356],"both":[357],"phenylalanine":[360],"(i.e.":[361],"group":[364],"on":[365],"\u03b1-carbon)":[367],"render":[368],"inactive":[369],"compounds.":[370],"Most":[371],"show":[375],"good":[377,391],"degree":[378],"selectivity":[380],"plasmepsins":[383],"over":[384],"D,":[386],"even":[387],"though":[388],"few":[390],"enzyme":[396],"could":[397],"identified":[399],"also.":[400]},"counts_by_year":[],"updated_date":"2026-09-04T10:56:28.161419","created_date":"2016-06-24T00:00:00"}