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Sinteza zaviralcev encima InhA 1,2,3,4-tetrahidropirolo[1,2-alfa]pirazinskega tipa = Synthesis of 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine type InhA inhibitors : enoviti magistrski študijski program FarmacijaStarc, Andreja, farmacevtkaTuberkuloza je nalezljiva bolezen, ki jo povzroča bakterija Mycobacterium tuberculosis, in ostaja vodilni vzrok smrti predvsem v nerazvitem delu sveta. Zdravilo prve linije kombiniranega zdravljenja ... predstavlja izoniazid, ki moti biosintezo mikolnih kislin, tako da zavira encim InhA. Zaviranje tega encima je povezano s celično smrtjo mikobakterije. Izoniazid je predzdravilo, ki potrebuje oksidativno aktivacijo z mikobakterijsko katalazno peroksidazo KatG. Monorezistentnost proti izoniazidu je najpogostejša odpornost proti zdravilu prvega izbora za terapijo tuberkuloze. Zato so učinkovine, ki neposredno zavirajo InhA in ne potrebujejo aktivacije s KatG, zelo obetavne za spopad z odpornimi sevi M. tuberculosis. Sintetizirati smo želeli štiri nove potencialne neposredne zaviralce encima InhA (spojine 8, 12, 17 in 26). Izhajali smo iz strukture molekule tetrahidropiranskega zaviralca (spojina I), ki smo mu tetrahidropiranski del zamenjali z 1,2,3,4-tetrahidropirolo[1,2-a]pirazinom. Kemijski prostor v aktivnem mestu encima ter njegovo zaviranje smo raziskali z različnimi substituenti na osnovni strukturi našega potencialnega zaviralca. Sintetiziranim spojinam so na Fakulteti za farmacijo Univerze v Ljubljani na izoliranem encimu InhA določili vrednosti IC50. Te so: za spojino 8 70 %M in za spojino 26 20 %M. Spojina 17 je razpadla, preden smo jo uspeli testirati. Tako smo tudi ugotovili, da je nesubstituiran pirol nestabilen, zato bi morali na obroč pripeti elektron-privlačne skupine. Slednji pristop smo preskusili pri spojini 12, kjer smo želeli na pirol uvesti brom, a žal želenega produkta nismo uspeli izolirati. Ne glede na to predvidevamo, da spojina 12 ne bi bila aktivna, pač pa bi imela le povečano kemijsko stabilnost.Type of material - master's thesis ; adult, seriousPublication and manufacture - Ljubljana : [A. Starc], 2020Language - slovenianCOBISS.SI-ID - 4885873
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Faculty of Pharmacy, Ljubljana | Ljubljana | FFALJ |
reading room 1 cop.
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Starc, Andreja, farmacevtka | ![]() |
Pajk, Stane, 1983- | 28861 |
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