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Design, synthesis and pharmacological studies of structural analogues modeled on bioactive natural products
(Universita degli studi di Salerno, 2011-03-21)
Microsomal prostaglandin E2 synthase-1 (mPGES-1) is the enzyme responsible for the conversion of the cyclooxygenase (COX)-derived prostaglandins (PG)H2 into PGE2. This enzyme is deeply involved in different pathologies; ...
New techniques of molecular modelling and structural chemistry for the development of bioactive compounds
(Universita degli studi di Salerno, 2013-05-14)
Computational chemistry represents today a valid and fast tool for the research of new compounds with potential biological activity. The analysis of ligand-macromolecule interactions and the evaluation of possible “binding ...
Enzymatic synthesis of macrolactones
(Universita degli studi di Salerno, 2011-02-24)
Macrolactones are a large and structurally diverse class of compounds. Natural products having a
macrolactone structure have been isolated from many natural sources such as plants, insects,
marine organism and bacteria. ...
Synthesis and properties of linear and cyclic peptoids
(Universita degli studi di Salerno, 2012-03-26)
Le strutture e le attività metaboliche di tutte le cellule si basano su una vasta gamma di molecole comprendenti: amminoacidi, carboidrati, lipidi e nucleotidi, insieme alle forme polimeriche di questi composti. Ognuna di ...
Design and structural optimization of new molecules as potential antiinflammatory and/or anticancer agents.
(Universita degli studi di Salerno, 2015-03-10)
L’infiammazione ed il cancro sono due complessi meccanismi patologici in cui risultano coinvolti una serie di differenti mediatori molecolari. La profonda connessione tra cancro ed infiammazione è ben nota e la modulazione ...
Design e sintesi di analoghi delle azumammidi, potenti inibitori degli enzimi HDACs
(Universita degli studi di Salerno, 2011-03-07)
Le azumammidi sono cinque ciclopeptidi di origine marina, isolate nel 2003 da
Fusetani et al dalla spugna Mycale izuensis e brevettate dalla Yamanouchi Pharmaceutical.
L'interesse destato da questi metaboliti secondari ...
Chemical proteomics on ligand protein
(Universita degli studi di Salerno, 2011-03-18)
The emerging field of mass spectrometry-based chemical proteomics provides a powerful instrument in the target discovery of bioactive small-molecules, such as drugs or natural products[1]. The identification of their ...
Stereoselective carbon-carbon and carbon-heteroatom bond formation mediated by bifunctional organocatalysts
(Universita degli studi di Salerno, 2013-01-30)
This PhD work describes the development of different Michael and Michael type processes employing different bifunctional organocatalysts. All the processes studied involved a non-covalent activation of the substrates ...
Design, virtual screening and structural studies of new molecules with potential antitumor and antiinflammatory activity
(Universita degli studi di Salerno, 2012-03-30)
Computational methodologies in combination with experimental techniques as Nuclear Magnetic Resonance (NMR) have become a crucial component in drug discovery process, from hit identification to lead optimization.
The study ...
Total synthesis of terpenoidic unsatured dialdehydes and evaluation of their activity towards TRP receptors
(Universita degli studi di Salerno, 2012-02-02)
The aim of this PhD project has been to develop new synthetic strategies in
enantioselective preparation of natural products.
In particular my attention has been focused on preparation of some natural
metabolite, ...