A5031776030- Supramolecular Self-Assembly in Materials
- Chemical Synthesis and Analysis
- Phenothiazines and Benzothiazines Synthesis and Activities
- Polydiacetylene-based materials and applications
- Synthesis and biological activity
- Organometallic Compounds Synthesis and Characterization
- Pharmacological Receptor Mechanisms and Effects
- Synthesis and Biological Evaluation
- Computational Drug Discovery Methods
- Synthesis and Characterization of Heterocyclic Compounds
- HIV/AIDS drug development and treatment
- Synthesis of Organic Compounds
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Cancer therapeutics and mechanisms
- Marine Biology and Environmental Chemistry
- Synthesis and Reactivity of Heterocycles
- Metal complexes synthesis and properties
- Synthesis and Reactions of Organic Compounds
- Viral Infections and Immunology Research
- Synthesis of β-Lactam Compounds
- Alzheimer's disease research and treatments
- Carbohydrate Chemistry and Synthesis
- Synthesis and pharmacology of benzodiazepine derivatives
- Prion Diseases and Protein Misfolding
- Chemical Synthesis and Reactions
Center for Research in Molecular Medicine and Chronic Diseases
2020-2024
Universidade de Santiago de Compostela
2020-2024
Sapienza University of Rome
2014-2024
University of Genoa
2003-2016
University of Milan
1998
Multitarget therapeutic leads for Alzheimer's disease were designed on the models of compounds capable maintaining or restoring cell protein homeostasis and inhibiting β-amyloid (Aβ) oligomerization. Thirty-seven thioxanthen-9-one, xanthen-9-one, naphto- anthraquinone derivatives tested direct inhibition Aβ(1-40) aggregation electric eel acetylcholinesterase (eeAChE) horse serum butyrylcholinesterase (hsBChE). These are characterized by basic side chains, mainly quinolizidinylalkyl moieties,...
The toxicity and antitumor activity of the novel organotin compound triethyltin(IV)lupinylsulfide hydrochloride (IST-FS 29), administered by oral route, have been evaluated against three transplantable murine tumor models: P388 lymphocytic leukemia, B16F10 melanoma 3LL Lewis lung carcinoma. Mild reversible signs acute such as behavioral symptoms, weight loss histological alterations were mainly reported at highest single dose 28 mg/kg. Conversely, lower concentrations ranging from 7 to 21...
Abstract Light‐induced molecular piping of cyclic peptide nanotubes to form bent tubular structures is described. The process based on the [4+4] photocycloaddition anthracene moieties, whose structural changes derived from interdigitated flat disposition precursors corresponding cycloadduct induced geometrical modifications in packing that provokes their curvature. For this purpose, we designed a new class formed by β‐ and α‐amino acids. presence former predisposes stack parallel fashion...
We have investigated the patterns of in vitro cytotoxicity, induced by six newly synthesized gold and tin compounds, three human ovarian cancer cell lines (SW 626, IGROV 1 OVCAR-3). Four i.e. gold(I)lupinylsulfide hydrochloride [1] (containing a naked atom), triethylphosphinogold(I)lupinylsulfide [2], triphenyl-phosphinogold(I)lupinylsulfide [3] ,2-bis(diphenylphosphino)ethane bis[gold(I)lupinylsulfide] dihydrochloride [4] (all containing atom coordinated with different phosphines), were...
Chloroquine is commonly used in the treatment and prevention of malaria, but Plasmodium falciparum, main species responsible for malaria-related deaths, has developed resistance against this drug. Twenty-seven novel chloroquine (CQ) analogues characterized by a side chain terminated with bulky basic head group, i.e., octahydro-2H-quinolizine 1,2,3,4,5,6-hexahydro-1,5-methano-8H-pyrido[1,2-a][1,5]diazocin-8-one, were synthesized tested activity D-10 (CQ-susceptible) W-2 (CQ-resistant) strains...
(+)-Laburnamine (1), a rare alkaloid extracted from Laburnum anagyroides seeds (∼4 mg 1 kg), was shown to bind with high affinity (Ki, 293 nM) the α4β2 nicotinic receptor subtype, which is, respectively, 126 and 136 times higher than α3β4 (Ki 37 μM) α7 subtypes 40 μM). When its ability release [(3)H]-dopamine striatal slices tested in functional assay, compound behaved as partial agonist an EC50 of 5.8 μM Emax that 43% nicotine. incubated nicotine same prevented maximal effect being reached.
Abstract A new class of amphipathic cyclic peptides, which assemble in bacteria membranes to form polymeric supramolecular nanotubes giving them antimicrobial properties, is described. The method based on the use two orthogonal clickable transformations incorporate different hydrophobic or hydrophilic moieties a simple, regioselective, and divergent manner. resulting cationic peptides described this article exhibit strong properties with broad therapeutic window. Our studies suggest that...
Natural events, such as earthquakes, floods, etc., can play a significant role in triggering industrial accidents of various intensities (the so-called Na-Tech risk), so that their inclusion comprehensive risk assessment is very important. However, detailed and quantitative approach often unrealistic, because the extremely large number calculations to be carried out scenarios analysed. A preliminary semi-quantitative methodology here presented for characterization safety level different...
In this protocol, we describe how to perform the photo-isomerization of cyclic peptides containing an unsaturated β-amino acid. This process triggers formation or disassembly peptide nanotubes under appropriate light irradiation. Specifically, start by describing solid-phase synthesis component. We also present a technique for performing isomerization studies in solution and extend it microfluidic aqueous droplets. For complete details on use execution please refer Vilela-Picos et al.