Akademska digitalna zbirka SLovenije - logo
VSE knjižnice (vzajemna bibliografsko-kataložna baza podatkov COBIB.SI)
  • Study, synthesis and evaluation of biological activity of new N-phenyl-4,5-dibromopyrrolamides and N-phenyl-3,4-dichloro-5-methylpyrrolamides as ATPase inhibitors of DNA gyrase B
    Lovison, Denise
    Due to an ever increasing number of bacteria resistant to common antibacterial drugs, we have started, during my stay at the University of Ljubljana, a research in the field of the design and ... synthesis of new ATPase inhibitors of DNA gyrase with N-phenyl-4,5-dibromopyrrolamide and N-phenyl-3,4-dichloro-5-methylpyrrolamide general structures. DNA gyrase is a member of type IIA bacterial topoisomerases and is a well-known and clinically validated pharmacological target for antibacterial drugs. The function of DNA gyrase is to catalyse the transient break and reunion of the DNA double strand, a crucial process for negative supercoiling or relaxation of positive supercoils in the DNA molecule during its replication. In the design of our series of compounds, the focus was on the optimisation of biological activities of known N-phenyl-pyrrolamide ATPase inhibitors of DNA gyrase, especially by varying their size, and the position and orientation of key functional groups. During our work, we have synthesised several new potential ATPase inhibitors according to a multi-step synthetic procedure. The identity and purity of the prepared compounds were confirmed by means of various analytical techniques, e.g. TLC, HPLC, MS, and NMR. The enzymatic activity was evaluated against DNA gyrase from E. coli and, for a selected subset of compounds, also the antibacterial activity against different Gram-positive and Gram-negative bacterial strains was determined. Some of the derivatives exhibited interesting antibacterial activity when tested on a panel of bacteria. Moreover, the structure-activity relationship (SAR) was examined and the results were rationalised with molecular docking.
    Vrsta gradiva - magistrsko delo ; neleposlovje za odrasle
    Založništvo in izdelava - Cagliari : [D. Lovison], 2017
    Jezik - angleški
    COBISS.SI-ID - 4649329

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

Vnos na polico