Design, Synthesis and Biological Activity of Small α-Aminoboron Containing Peptidomimetics

Gozhina, Olga Vladimirovna

dc.contributor.advisor	Lejon, Tore
dc.contributor.author	Gozhina, Olga Vladimirovna
dc.date.accessioned	2013-05-08T08:08:32Z
dc.date.available	2013-05-08T08:08:32Z
dc.date.issued	2013-01-18
dc.description.abstract	Antimicrobial peptides (AMPs) are a special group of small amphipathic peptides (which hold both hydrophilic and hydrophobic regions) composed of different amino acids and produced by all living organisms as a part of innate immunity. With the increasing microbial resistance to traditional antibiotics the need for unconventional therapeutic has become crucial. This thesis deals with the design and synthesis of a library of α-aminoboronic di- and tri- peptides and investigation of their biological activity against different bacteria strains, fungi and kinases in order to discover compounds that can further be developed into drugs. Preliminary results have provided a broad spectrum of data regarding structure-activity relationship of synthesized peptides and several new potential therapeutics have been discovered.	en
dc.description.doctoraltype	ph.d.	en
dc.description.popularabstract	Antimikrobielle peptider (AMP) er en gruppe av små amfifile peptider (dvs. de innholder hydrofile og hydrofobe regioner) som består av forskjellige aminosyrer og som finnes i alle levende organismer som en del av det medfødte immunforsvaret. Flere og flere patogener blir motstandsdyktige mot tradisjonelle antibiotika og utvikling av nye legemiddel trenges for bekjempe disse. I denne avhandlingen beskrives design og syntese av et bibliotek av di- og tri-peptider innholdende en alfa-aminoborsyre eller borester. Effekten av disse er blitt testet mot en rekke forskjellige bakterier, sopp og kinaser for å oppdage forbindelser som kan utvikles til legemiddel. Resultatene fra testingen har gitt data vedrørende forholdet mellom strukturen til peptidene og aktiviteten deres og flere nye forbindelser med god terapeutisk virke er blitt oppdaget.	en
dc.description.sponsorship	NFR (Norges forskningsråd)	en
dc.description	Papers 1, 2, 4 and 5 are not available in Munin: <br/>1. Olga V. Gozhina, Ivar K. Thomassen and Tore Lejon: 'Ultrasound promoted dimerization of benzylic halides' (accepted manuscript in Synthetic Communications). <br/>2. Alexey S. Gorovoy, Olga V. Gozhina, John Sigurd Svendsen, Anna A. Domorad, George V. Tetz, Victor V. Tetz and Tore Lejon: 'Boron containing peptidomimetics – a novel class of selective anti-tubercular drugs', (accepted manuscript in Chemical Biology & Drug Design). <br/>4. Alexey S. Gorovoy, Olga V. Gozhina, John Sigurd Svendsen, George V. Tetz, Anna A. Domorad, Victor V. Tetz and Tore Lejon: 'Synthesis and anti-tubercular activity of β-substituted and α,β-disubstituted β-aminoboronates and boronic acids' (manuscript). <br/>5. Olga V. Gozhina, John Sigurd Svendsen and Tore Lejon: 'Synthesis and antimicrobial activity of α-aminoboronic containing peptidomimetics' (manuscript)	en
dc.identifier.isbn	978-82-8236-084-5
dc.identifier.isbn	978-82-8236-085-2
dc.identifier.uri	https://hdl.handle.net/10037/5145
dc.identifier.urn	URN:NBN:no-uit_munin_4858
dc.language.iso	eng	en
dc.publisher	Universitetet i Tromsø	en
dc.publisher	University of Tromsø	en
dc.rights.accessRights	openAccess
dc.rights.holder	Copyright 2013 The Author(s)
dc.rights.uri	https://creativecommons.org/licenses/by-nc-sa/3.0	en_US
dc.rights	Attribution-NonCommercial-ShareAlike 3.0 Unported (CC BY-NC-SA 3.0)	en_US
dc.subject	VDP::Mathematics and natural science: 400::Chemistry: 440	en
dc.subject	VDP::Matematikk og Naturvitenskap: 400::Kjemi: 440	en
dc.title	Design, Synthesis and Biological Activity of Small α-Aminoboron Containing Peptidomimetics	en
dc.type	Doctoral thesis	en
dc.type	Doktorgradsavhandling	en