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dc.creatorOpsenica, Igor
dc.creatorFilipović, Vuk
dc.creatorNuss, Jon E.
dc.creatorGomba, Laura M.
dc.creatorOpsenica, Dejan
dc.creatorBurnett, James C.
dc.creatorGussio, Rick
dc.creatorŠolaja, Bogdan
dc.creatorBavari, Sina
dc.date.accessioned2019-04-24T12:49:13Z
dc.date.available2019-04-24T12:49:13Z
dc.date.issued2012
dc.identifier.issn0223-5234
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/2676
dc.description.abstractBotulinum neurotoxins (BoNTs), composed of a family of seven serotypes (categorized A-G), are the deadliest of known biological toxins. The activity of the metalloprotease, light chain (LC) component of the toxins is responsible for causing the life-threatening paralysis associated with the disease botulism. Herein we report significantly more potent analogs of novel, lead BoNT serotype A LC inhibitor 2,5-bis(4-amidinophenyl)thiophene (K-i = 10.881 mu M +/- 0.90 mu M). Specifically, synthetic modifications involved simultaneously replacing the lead inhibitor's terminal bis-amidines with secondary amines and the systematic tethering of 4-amino-7-chloroquinoline substituents to provide derivatives with K-i values ranging from 0.302 mu M (+/- 0.03 mu M) to 0.889 mu M (+/- 0.11 mu M).en
dc.publisherElsevier France-Editions Scientifiques Medicales Elsevier, Paris
dc.relationNational Institute of Allergy and Infectious Diseases (USA) [5-U01 AI082051-02]
dc.relationNATOs Public Diplomacy Division
dc.relationNational Cancer Institute
dc.relationNational Institutes of Health (USA) [HHSN261200800001E]
dc.rightsrestrictedAccess
dc.sourceEuropean Journal of Medicinal Chemistry
dc.subjectBioterrorismen
dc.subjectBotulinum neurotoxinen
dc.subjectInhibitionen
dc.titleThe synthesis of 2,5-bis(4-amidinophenyl)thiophene derivatives providing submicromolar-range inhibition of the botulinum neurotoxin serotype A metalloproteaseen
dc.typearticle
dc.rights.licenseARR
dcterms.abstractФилиповић, Вук; Опсеница, Дејан; Солаја, Богдан A.; Гомба, Лаура М.; Опсеница, Игор; Бавари, Сина; Гуссио, Рицк; Бурнетт, Јамес Ц.; Нусс, Јон Е.;
dc.rights.holderElsevier
dc.citation.volume53
dc.citation.spage374
dc.citation.epage379
dc.citation.other53: 374-379
dc.citation.rankM21
dc.description.otherPeer-reviewed version of the article: [http://cer.ihtm.bg.ac.rs/handle/123456789/971]
dc.identifier.pmid22516424
dc.identifier.doi10.1016/j.ejmech.2012.03.043
dc.identifier.scopus2-s2.0-84861589629
dc.identifier.wos000305863100040
dc.type.versionpublishedVersion


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