A5048648989- Synthesis and biological activity
- Nitric Oxide and Endothelin Effects
- Synthesis and Biological Evaluation
- Electron Spin Resonance Studies
- Synthesis of heterocyclic compounds
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Synthesis and Characterization of Heterocyclic Compounds
- Eicosanoids and Hypertension Pharmacology
- Tryptophan and brain disorders
- Organic Chemistry Cycloaddition Reactions
- Click Chemistry and Applications
- Quinazolinone synthesis and applications
- Neuroendocrine regulation and behavior
- Structural and Chemical Analysis of Organic and Inorganic Compounds
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Synthesis and Catalytic Reactions
- Pharmacological Receptor Mechanisms and Effects
- Adenosine and Purinergic Signaling
- Photodynamic Therapy Research Studies
- Ferrocene Chemistry and Applications
- Sulfur-Based Synthesis Techniques
- Metal complexes synthesis and properties
- Organic Chemistry Synthesis Methods
- Organic and Molecular Conductors Research
Universidad de Granada
2012-2023
Complejo Hospitalario Universitario de Granada
2019
Instituto de Investigación Biosanitaria de Granada
2019
University of Ferrara
2012-2014
In an attempt to find new compounds with neuroprotective activity, we have designed, synthesized and characterized 19 nNOS inhibitors a 4,5-dihydro-1H-pyrazole structure. Compounds 11r [1-cyclopropanecarbonyl-3-(2-amino-5-chlorophenyl)-4,5-dihydro-1H-pyrazole] 11e [1-cyclopropanecarbonyl-3-(2-amino-5-methoxyphenyl)- 4,5-dihydro-1H-pyrazole] show the highest activities inhibition percentages of 70% 62%, respectively. A structure−activity relationship for can be established from structural...
Abstract Herein we describe the synthesis of a new family kynurenamine derivatives with urea or thiourea moiety, together their in vitro biological evaluation as inhibitors both neuronal and inducible nitric oxide synthases (nNOS iNOS, respectively), enzymes responsible for biogenesis NO. These compounds were synthesized from 5‐substituted‐2‐nitrophenyl vinyl ketone scaffold five‐step procedure moderate to high chemical yields. In general, assayed show greater inhibition iNOS than nNOS,...
To find new compounds with potential neuroprotective activity, we have designed, synthesized, and characterized a series of neural nitric oxide synthase (nNOS) inhibitors kynurenamine structure. Among them, N-[3-(2-amino-5-methoxyphenyl)-3-oxopropyl]acetamide is the main melatonin metabolite in brain shows highest activity series, an inhibition percentage 65% at 1 mM concentration. The structure-activity relationship partially reflects that previously reported...
In search of new Nitric Oxide Synthase (NOS) inhibitor agents, two isosteric series derivatives with an imidamide scaffold (one them a hydroxyl group and the other carbonyl one) were synthesized evaluated on inducible (iNOS) neuronal (nNOS) isoforms. These compounds have been designed by combining kynurenamine framework amidine moiety in order to improve selectivity for isoform. general, vitro inhibitory assays exhibited better inhibition values iNOS isoform, being...
<italic>N</italic>,<italic>N</italic>′-Disubstituted thioureas and ureas as nNOS iNOS inhibitors were synthesized. Thiourea <bold>4g</bold> was the best inhibitor without eNOS inhibition.
Nitric oxide is an important inflammation mediator with a recognized role in the development of different cancers. Gliomas are primary tumors central nervous system poor prognosis, and expression inducible nitric synthase correlates degree malignancy, changes vascular reactivity, neo-angiogenesis. Therefore, targeting biosynthesis appears as potential strategy to impair glioma progression. In present work set aryl amido-aryl acetamidine derivatives were synthesized obtain new potent...
Nowadays, the expansion of new technologies in developed countries requires their inclusion higher educational systems, focused on development skills to promote a continuous and independent learning process for students. Internet have reached wide social diffusion, mainly among young people, therefore use digital at university, from smartphone apps online collaboration tools, is becoming more embedded. This article describes exploration using wiki study degree Pharmacy, particularly area...
The synthesis of different compounds with a quinazolinone, quinazolinthione, or quinazolinimine skeleton and their in vitro biological evaluation as inhibitors inducible neuronal nitric oxide synthase (iNOS nNOS) isoforms are described. These derivatives were obtained from substituted 2-aminobenzylamines, using diverse cyclization procedures. Furthermore, the diamines synthesized by two routes: A conventional pathway an efficient one-pot continuous-flow hydrogenator. structures these...
Aim: Identification of new antiproliferative compounds. Methodology: Four series compounds were synthesized by the Mitsunobu reaction. Their activity was studied against several cancer cells and a noncancerous fibroblast cell line. apoptotic analyzed using caspase 3/7 fluorescence assay. Results & conclusion: 9-alkylated-6-halogenated 2,6-dihalogenated purines show remarkable inhibition tumor proliferation, with dichloro derivatives being most potent all series. The promising compound,...
Abstract The 1 H and 13 C NMR resonances of seventeen N ‐alkyl aryl‐ ′‐[3‐hydroxy‐3‐(2‐nitro‐5‐substitutedphenyl)propyl]‐thioureas ureas ( 1–17 ), or ′‐[3‐(2‐amino‐5‐substitutedphenyl)‐3‐hydroxypropyl]‐thioureas 18–34 designed as NOS inhibitors, were assigned completely using the concerted application one‐ two‐dimensional experiments (DEPT, HSQC HMBC). NOESY studies confirm preferred conformation these compounds. Copyright © 2016 John Wiley & Sons, Ltd.
The selective inhibition of inducible nitric oxide synthase (iNOS) has become an interesting goal for the treatment diseases where immune and inflammatory response organism is involved. Septic shock one prominent example this type affections. In paper, design synthesis twelve substituted pyridinyl- imidamide derivatives described, together with their biological evaluation as NOS inhibitors. most potent compound was N-(3-hydroxy-3-(pyridin-3-yl)propyl)acetimidamide 9a (IC50 = 4.6 µM, against...
The 13 C NMR resonances of 19 1‐acyl‐3‐(2‐nitro‐5‐substitutedphenyl)‐4,5‐dihydro‐1 H ‐pyrazoles, and 1‐acyl‐3‐(2‐amino‐5‐substituted)‐4,5‐dihydro‐1 were completely assigned using the concerted application one‐ two‐dimensional experiments (DEPT, gs‐HSQC gs‐HMBC). Copyright © 2012 John Wiley & Sons, Ltd.
Two new families of pyrazoline and thiadiazoline heterocycles have been developed. Their inhibitory activities against two different isoforms nitric oxide synthase (inducible neuronal NOS) are reported. The novel derivatives were synthesized combining the arylthiadiazoline or arylpyrazoline skeleton a carboxamide carbothioamide moiety, used as starting material ethyl 2-nitrobenzoates substituted nitrobenzaldehydes, respectively. structure-activity relationships final molecules discussed in...