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  • Synthesis of benzothiazolepyrrolamide-based DNA-Gyrase B inhibitors = Sintesi di nuovi derivati a nucleo benzotiazolpirrolammidico come inibitori della DNA- Girasi B : Mestrado Integrado em Ciências Farmacêuticas
    Sanna, Erica
    Bacterial resistance to antimicrobial drugs is an increasing health and economic problem, so there is an urgent need to discover new antibiotics with novel target or increase and/or enlarge the ... activity of those currently in use. The bacterial topoisomerases DNA gyrase and topoisomerase IV are validated targets for development of novel antibacterial agents. Fluoroquinolones inhibit the catalytic GyrA and/or ParC(GrlA) subunit and have been commonly used, although these have toxicity liabilities that restrict their use. The ATPase GyrB and ParE(GrlB) subunits have been much less explored and after withdrawal of novobiocin, there are no further marketed inhibitors . ATP-competitive inhibitors of GyrB and/or ParE(GrlB) are of special interest, as this target has been validated, and it is expected that many of the problems associated with fluoroquinolones can be avoided. This work focused on the synthesis of novel ATP-competitive inhibitors of these enzymes, specifically dibromopyrrolamide analogues of 2-aminobenzo[d]thiazole-6-carboxylic acid as DNA gyrase B inhibitors. It was focused on optimizing parts of the molecule to achieve inhibitor interactions with aminoacids in the lipophilic pocket of the ATP-binding site of the enzyme, which can accommodate quite big and chemically diverse substituents. Thus, we try to introduce different substituents attached to the position 4 of the benzothiazole ring in order to tune antimicrobial properties and improve solubility of this type of compounds, which is quite a problem. Problems with insolubility of compound has been quite a problem and biological assays are currently under preparation.
    Vrsta gradiva - magistrsko delo ; neleposlovje za odrasle
    Založništvo in izdelava - Cagliari ; Ljubljana : [E. Sanna], 2019
    Jezik - angleški
    COBISS.SI-ID - 17919235

Nobena knjižnica v sistemu COBISS.SI nima izvoda tega gradiva.
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