Sökning: "transition-state mimic"

Visar resultat 1 - 5 av 9 avhandlingar innehållade orden transition-state mimic.

1. 1. Design and Synthesis of Novel HIV-1 Protease Inhibitors Comprising a Tertiary Alcohol in the Transition-State Mimic

   Författare :Jenny Ekegren; Anders Hallberg; Daniel Rich; Uppsala universitet; []
   Nyckelord :Chemistry; HIV AIDS; HIV-1 protease inhibitor; transition-state mimic; tertiary alcohol; palladium; cross-coupling; aminocarbonylation; microwave; molybdenum hexacarbonyl; Kemi;

   Sammanfattning : HIV-1 protease inhibitors are important in the most frequently used regimen for the treatment of HIV/AIDS, the highly active antiretroviral therapy (HAART). For patients with access to this treatment, an HIV infection is no longer lethal, but rather a manageable, chronic infection. LÄS MER

3. 2. Phosphonamidates as potential NDM-1 inhibitors

   Författare :Katarzyna Palica; Mate Erdelyi; Lindon Moodie; Uppsala universitet; []
   Nyckelord :NATURVETENSKAP; NATURAL SCIENCES;

   Sammanfattning : WHO’s recent reports indicate that the rapidly growing resistance of bacteria became one of the biggest problems of the XXI century. The most powerful human counter weapon, antibiotics, starts to become ineffective for the treatment of bacterial infections. LÄS MER

4. 3. Development of phosphorus-containing metallo-β-lactamase inhibitors : Synthesis and binding studies by solution NMR and molecular docking

   Författare :Katarzyna Palica; Máté Erdélyi; Christopher J. Schofield; Uppsala universitet; []
   Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; MBL inhibitors; antibiotic resistance; metallo-β-lactamases; NMR spectroscopy; Medicinal Chemistry; Läkemedelskemi;

   Sammanfattning : The rapidly growing bacterial resistance development is turning into one of the main challenges of the 21st century. Our antibiotics are becoming ineffective for the treatment of bacterial infections, and without successful action, simple infections, such as pneumonia or Septicemia, will soon carry a highly probable mortal prognosis. LÄS MER

5. 4. Enzymatic mechanisms in biotin synthesis : vitamin B6 catalysis and phosphoryl transfer

   Författare :Jenny Sandmark; Karolinska Institutet; Karolinska Institutet; []
   Nyckelord :X-ray crystallography; biotin biosynthesis; pyridoxal-5 -phosphate; aminotransferase; aluminium fluoride; S-adenosyl-L-methionine; 7; 8-diaminopelargonic acid synthase; dethiobiotin synthetase; biotin; phosphoryl transfer; amiclenomycin.;

   Sammanfattning : With the large number of pathogenic bacteria that have developed antibiotic resistance it is increasingly important to find new targets for antibiotics. Our interest in the biotin biosynthesis pathway originates from this drug design perspective. All organisms require biotin, but it is only synthesised in bacteria, in plants and in some fungi. LÄS MER

7. 5. Computational Studies and Design of Biomolecular Diels-Alder Catalysis

   Författare :Mats Linder; Tore Brinck; Kendall N. Houk; KTH; []
   Nyckelord :NATURVETENSKAP; NATURAL SCIENCES; Computational chemistry; density functional theory; enzyme design; molecular modeling; organocatalysis; stepwise Diels-Alder; oxyanion hole;

   Sammanfattning : The Diels-Alder reaction is one of the most powerful synthetic tools in organic chemistry, and asymmetric Diels-Alder catalysis allows for rapid construction of chiral carbon scaffolds. For this reason, considerable effort has been invested in developing efficient and stereoselective organo- and biocatalysts. LÄS MER