Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 24 for “"Settore CHIM/08 - Chimica Farmaceutica"”.
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DEVELOPMENT OF SMALL MOLECULES AS INHIBITORS OF FTSZ AND RNPA ACTING AS POTENTIAL ANTIMICROBIAL AGENTS
The antimicrobial resistance (AMR) is nowadays one of the most worrying threats of modern medicine. Recently, AMR has been also called “the silent pandemic” because is as worrying as the COVID-19 outbreak, but without receiving the same public attention. The most important organizations such as …
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DEVELOPMENT OF SUSTAINABLE AND EFFICIENT TAILOR-MADE PROCESSES FOR PHARMA AND FOOD APPLICATIONS
The ecological burdens of chemical processes could not be underestimate anymore and a change of direction is required from the industry as well as from academia. In this scenario, my Doctoral Thesis is focused on the development of tailor-made processes for the production of fine chemicals relevant …
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COMPUTATIONAL DESIGN OF PEPTIDES AND PEPTIDOMIMETICS AS POTENTIAL THERAPEUTIC AGENTS TO SATISFY PRESSING MEDICAL NEEDS
Over the past two decades, peptide drug discovery showed a dramatic increase of interest due to the recent scientific findings and achievements made on the pharmacokinetic profile and peptide delivery. In addition, it is possible to mimic the secondary structure and the pharmacological effects of …
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ALPHA4BETA2 NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS: FROM SUBTYPE SELECTIVE TO STOICHIOMETRIC ISOPHORM SELECTIVE PARTIAL AGONISM.
… goal of Part 1 was the mutational studies of Ser108 residue of the hydrophilic pocket of the β2(-) side of the α4β2 orthosteric binding site with the purpose of studying the importance of the hydroxyl group of serine residue and the steric encumbrance in the pocket. For this reason, binding …
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Thiazolidinone-isatin hybrids as multi-target anticancer agents
During the three years of PhD two main projects have been carried out. The projects were focused on the design, synthesis, and characterization of small molecules with antitumoral activity. Cancer is one of major causes of death in the world and, considering its multi-factorial origin it could be …
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Development of novel reactive oxygen species (ROS)-modulating agents and carbonic anhydrase inhibitors for the treatment of Pancreatic Ductal Adenocarcinoma and other resistant cancers
In the present PhD thesis I propose the study and pharmacobiological optimization of a class of quinazolin-5,8-dione-based (QDs) compounds that showed promising antitumor activity against pancreatic ductal adenocarcinoma (PDAC) as well as other tumor types. In the same context of developing new …
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Design, Chemical Synthesis and Biological Evaluation of Potential New Antiviral Agents
Acquired Immunodeficiency Syndrome (AIDS) is a disease caused by the Human Immunodeficiency Virus (HIV). Since its discovery in 1981, more than 25 million people died due to this disease. To date, an effective HIV-1 vaccine usable in prophylaxis or in the therapy of humans has not yet been …
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Design and synthesis of new potential anticancer agents and high-selective A2B antagonists
The synthesis of antitumor agents covers a large part of current medicinal chemistry efforts. This thesis mainly focuses on the synthesis of different scaffolds as new potential anticancer agents. Two different approaches were applied: a hybrid concept and a rational based drug design. In the first …
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QUANTITATIVE PROTEOMIC APPROACHES TO STUDY DRUG MECHANISM OF ACTION
In recent years an increased number of covalent protein kinase inhibitors has been approved for cancer therapy and many more are undertaking clinical trials. Covalent binding is usually obtained by introducing in these drugs an electrophilic warhead able to bind specific nucleophilic sites in the …
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STUDY OF COVALENT AND NON COVALENT INTERACTIONS OF BIOPOLYMER BY MASS SPECTROMETRY
ESI-MS screening methods directly detect ligand-target non covalent complexes in the gas phase and allow inference of affinity (and specificity) of the ligand-target interaction in solution [1, 2]. The identity of different complexes can be directly assessed as the mass of each molecule works as …
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Secondary Metabolites from Otanthus maritimus, Stachys glutinosa and Withania somnifera: Isolation, Structure Elucidation and Interactions with Cannabinoid and Opioid Systems
In our continuous search for plant secondary metabolites that bind to CB and/or opioid receptors, we selected four extracts that showed interesting affinity versus the above mentioned receptors . In particular: the DCM extract obtained from the aerial parts of Stachys glutinosa (SGE) was able to …
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Structure-based approaches applied to the study of pharmaceutical relevant targets
Computer Aided Drug Design/Discovery methods became complementary to traditional and modern drug discovery approaches. Indeed CADD is useful to improve and speed up the detection and the optimization of bioactive molecules. The present study is focused on the application of structure-based …
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TUMOR-TARGETED RELEASE OF IMMUNOSTIMULATORY AGENTS: SYNTHESIS AND BIOLOGICAL EVALUATION OF IMIDAZOQUINOLINE-BASED PRODRUGS AND ANTIBODY CONJUGATES
Different strategies have been proposed in order to achieve the targeted delivery of anticancer agents at the tumor site. Amongst the different delivery vehicles proposed, antibody drug conjugates (ADCs) have been especially successful in the clinic. Recently, the involvement of the immune system …
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