Sökning: "purine analogues"
Visar resultat 1 - 5 av 8 avhandlingar innehållade orden purine analogues.
1. Targets and strategies for drug development against human African sleeping sickness
Sammanfattning : Trypanosoma brucei is a causative agent of African sleeping sickness. It is an extracellular parasite which circulates in the blood, lymph and eventually invades the central nervous system. LÄS MER
2. Design and Synthesis of Potential Aminoacyl-tRNA Synthetase Inhibitors
Sammanfattning : Aminoacyl-tRNA synthetases (aaRSs) are essential enzymes present in all living organisms, their catalytic activity is involved in the translation of the genetic code into functional proteins and they are potential targets for anti-infective agents. The first step in the biosynthetic pathway catalysed by aaRSs consists of activation of the corresponding amino acid by the reaction with ATP to form an aminoacyl-adenylate (aa-AMP), the key intermediate in the biosynthesis of proteins. LÄS MER
3. Synthesis of Potential Inhibitors Against HIV
Sammanfattning : This thesis describes the syntheses of various potential inhibitors of HIV, e.g. some 3´-hydroxymethyl-substituted carbocyclic nucleoside analogues as reverse transcriptase inhibitors and some symmetry-based peptidomimetics as protease inhibitors. LÄS MER
4. Novel treatment of African trypanosomiasis
Sammanfattning : Human African Trypanosomiasis (HAT) or Sleeping Sickness is fatal if untreated. Current drugs used for the treatment of HAT have difficult treatment regimens and unacceptable toxicity related issues. LÄS MER
5. Pharmacological and molecular investigations on the mechanisms underlying resistance of human leukaemia cells to the antimetabolites methotrexate, 6-mercaptopurine and 6-thioguanine
Sammanfattning : The goal of this thesis has been to elucidate the mechanisms underlying resistance to methotrexate (MTX), 6-mercaptopurine (6-MP) and 6-thioguanine (6-TG), the antimetabolites widely used in treatment of childhood leukemia, as well as to determine the influence of 7-hydroxymethotrexate (7-OHMTX), the major metabolite of MTX, on the therapeutic action of MTX. Resistant sublines of leukemic cell lines were developed by long-term exposure to stepwise increasing concentrations of these different agents. LÄS MER