Diseño, Síntesis y Evaluación Biológica de Derivados Carboxamídicos e Imidamídicos como Inhibidores de Óxido Nítrico Sintasa
Metadatos
Afficher la notice complèteAuteur
Arias Bordajandi, FabioEditorial
Universidad de Granada
Departamento
Universidad de Granada.; Universidad de Granada. Programa de Doctorado en FarmaciaMateria
NOS (oxido nítrico sintasa) Inhibidores Derivados Carboxamídicos Imidamídicos
Date
2021Fecha lectura
2020-12-10Referencia bibliográfica
Arias Bordajandi, Fabio. Diseño, Síntesis y Evaluación Biológica de Derivados Carboxamídicos e Imidamídicos como Inhibidores de Óxido Nítrico Sintasa. Granada: Universidad de Granada, 2021. [http://hdl.handle.net/10481/65333]
Patrocinador
Tesis Univ. Granada.Résumé
The main goal of this doctoral thesis is the design, synthesis and biological
evaluation of new carboxamidic and imidamidic derivatives as inhibitors
for the different NOS isoforms. By this means, we are able to contribute
developing potent and selective compounds to target NO overproduction
in potential drugs for the diseases where is involved.
The specific objectives necessaries for this purpose are:
I. Following the path of previous articles from our research group, design
new compounds blending together the characteristics which
proportionate the highest selectivity and the most potent inhibition in
each NOS isoform.
II. Incorporate amidine and guanidine substructures, proven in
bibliography to be great moieties for NOS inhibition, to our own
molecules.
III. Develop a synthetic strategy that will allow obtaining the final products
with the highest yield possible.
IV. Purification and characterization of any new molecule synthesized by
nuclear magnetic resonance studies (NMR) and high resolution mass
spectrometry (HRMS).
V. Biological activity determination for the neuronal and inducible NOS
isoforms in all the final products, and in the endothelial one on those
with the best inhibition values.
VI. Analyze how the structural modifications influence on the potency and
selectivity of the inhibitors.