A5040812057- Synthesis of Indole Derivatives
- Chemical Synthesis and Analysis
- Circadian rhythm and melatonin
- Catalytic C–H Functionalization Methods
- Receptor Mechanisms and Signaling
- Asymmetric Synthesis and Catalysis
- Synthesis and Catalytic Reactions
- Research on Leishmaniasis Studies
- Enzyme Catalysis and Immobilization
- Carbohydrate Chemistry and Synthesis
- Chemical Synthesis and Reactions
- Synthesis and Biological Evaluation
- Analytical Chemistry and Chromatography
- Probiotics and Fermented Foods
- Click Chemistry and Applications
- Antimicrobial agents and applications
- Surfactants and Colloidal Systems
- Trypanosoma species research and implications
- Fermentation and Sensory Analysis
- Phytochemicals and Antioxidant Activities
- Crystallization and Solubility Studies
- Neuroendocrine regulation and behavior
- Lanthanide and Transition Metal Complexes
- Metal complexes synthesis and properties
- Supramolecular Chemistry and Complexes
University of Urbino
2016-2025
Japan Science and Technology Agency
2007
The University of Tokyo
2007
University of Milan
2006
University of Parma
2006
University of Florence
2005
University of Kansas
2004
University of Bologna
2001-2002
The discovery and development of a new Lewis acid system based on complex formed from niobium(V) methoxide (R)-3,3'-bis(2-hydroxy-3-isopropylbenzyl)-1,1'-binaphthalene-2,2'-diol, novel tetradentate BINOL derivative, is presented. was shown to be extremely effective in promoting the desymmetrative ring opening linear cyclic meso-epoxides using anilines as nucelophiles, delivering corresponding (R,R) anti-amino alcohols good excellent yields (up quantitative) enantioselectivity 96% ee)....
Molecular superposition models guided the design of novel melatonin receptor ligands characterized by a 2-acylaminomethyltetrahydroquinoline scaffold. Starting from structure N-anilinoethylamide ligands, flexible chain was conformationally constrained to reproduce bioactive conformation melatonin. Structure-activity relationships were investigated, focusing on substituent at nitrogen atom, position methoxy group, and replacement amide side urea thiourea groups. The compounds tested for...
Highly regioselective electrophilic substitution of indoles with N-acetylated α,β-dehydroalanine methyl ester, promoted by different transition metal salts was achieved. The orthogonal regioselectivity provides an efficient protocol toward highly functionalized 3-indolyl-α-amino acids. mechanism the reactions explored NMR studies.
A practical and efficient synthesis of 3-substituted hexahydropyrrolo[2,3-b]indole is described. The addition/cyclization indoles with alpha,beta-dehydroamino esters in the presence a Lewis acid provides adducts good yields stereoselectivities. This approach has been applied to concise esermethole employing an appropriately substituted indole N-acyl dehydroamino ester.
Abstract A copper‐based catalytic technique for the regioselective hydroboration and hydrosilylation of dehydroalanine derivatives has been developed. This method introduces synthetically versatile boron silicon groups, while simultaneously performing a anti‐Markovnikov hydrofunctionalization dehydroalanines dehydropeptides synthesis amino acids peptides bearing unnatural side‐chains. The products obtained were expediently converted into valuable nonproteinogenic acid building blocks...
Carbonylation reactions carried out at room temperature and atmospheric pressure of carbon monoxide are highly attractive extremely rare the same time. Here, oxidative alkoxycarbonylation styrenes to industrially relevant cinnamates has been developed under such a mild conditions (rt, 1 atm CO) in presence palladium(II) complex bearing bis(aryl)acenaphthenequinonediimine ligand, benzoquinone p-toluenesulfonic acid. Remarkably, variously substituted styrene derivatives have efficiently...
A ditopic palladacycle with SCS pincer coordination, L(PdCl)2 (1), was isolated and structurally characterized represents the first example of a transition metal complex polythioamide-based macrocycle. Preliminary studies 1 in catalytic coupling 4-iodotoluene styrene indicated it to be robust presence oxygen high temperatures, turnover numbers relatively short times.
A Pd(II)-catalyzed intramolecular oxidative C–H/C–H cross-coupling has been developed for the direct construction of valuable polycyclic heteroarene scaffolds. From a retrosynthetic point view, strategic formation C–C bond via C(sp2)–H/C(sp2)–H dehydrogenative coupling across C3,N-linked biheterocyclic precursors may be useful in de novo syntheses indole-derived natural products and pharmaceuticals. The reaction exhibited good functional group/heterocycle tolerance, proposed mechanism...
Indole-3-carbinol (I3C), an autolysis product of glucosinolates present in cruciferous vegetables, and its dimeric derivative (3,3'-DIM) have been indicated as promising agents preventing the development progression breast cancer. We recently shown that I3C cyclic tetrameric CTet formulated γ-cyclodextrin (γ-CD) efficiently inhibited cellular proliferation cancer cell lines. This study aims to analyze mechanisms involved vitro inhibition evaluate vivo antitumor activity a xenograft...
Abstract A Brønsted acid catalyzed bisindolization reaction with suitable α‐amido acetals that tolerates a wide range of indoles is reported. The method allows rapid access to the biologically relevant bisindolyl ethanamine scaffold in good excellent yields upon mild amide basic hydrolysis. In preliminary pharmacological studies, some these compounds display cytotoxic activity U937 cancer cells. marine natural alkaloid 2,2‐di(6′‐bromo‐3′‐indolyl)‐ethylamine was most active compound and could...
Permeability enhancers are receiving increased attention arising from their ability to increase transepithelial permeability and thus, bioavailability of orally or pulmonary administered biopharmaceutics. Here we present the synthesis in vitro assaying a series lactose-based non-ionic surfactants, highlighting relationship between structure biological effect. Using tensiometric measurements critical micelle concentrations (CMCs) surfactants were determined demonstrate that increasing...
A small library of sugar-based (i.e., glucose, mannose and lactose) monoesters containing hydrophobic aliphatic or aromatic tails were synthesized tested. The antimicrobial activity the compounds against a target panel Gram-positive, Gram-negative fungi was assessed. Based on this preliminary screening, antibiofilm most promising molecules evaluated at different development times selected food-borne pathogens (E. coli, L. monocytogenes, S. aureus, enteritidis). during biofilm formation...
The antimicrobial activity of the marine bisindole alkaloid 2,2-bis(6-bromo-3-indolyl) ethylamine (1) and related synthetic analogues (compounds 2⁻8) against target microorganisms was investigated by Minimum Inhibitory Concentration (MIC) determination. Compound 1 showed greatest with lowest MIC (8 mg/L) Escherichia coli, Staphylococcus aureus, Klebsiella pneumoniae, while derivatives exhibited higher MICs values (from 16 to 128 mg/L). Compounds 1, 3, 4, 8, most active ones, were then tested...
The rapid and expedient assembly of three new classes biheterocycles biological interest, viz. indole–imidazoles 4 , indole–pyrroles 6 indole–triazoles 8 was accomplished using different combinations tryptamines, 1,2‐diaza‐1,3‐dienes, aldehydes, and/or alkynes as readily available building blocks. Twenty‐six derivatives were thus prepared in excellent yields (up to 100 %). products screened for in‐vitro studies. Some these revealed promising anticancer activity against MCF7 Caco‐2 human...
Marine organisms such as corals, sponges and tunicates produce active molecules which could represent a valid starting point for new drug development processes. Among the various structural classes, attention has been focused on 2,2-bis(6-bromo-3-indolyl) ethylamine, marine alkaloid showed good anticancer activity against several tumor cell lines. Here, first time, mechanisms of action ethylamine have evaluated in U937 model. Morpho-functional molecular analyses, highlighting its preferred...
N-Acyl amino acids are biodegradable anionic amphiphilic molecules made up of linear fatty as hydrophobic tails and polar heads, which promising for their applicability in different technological fields. In the light widening use, a deeper understanding interactions with biological membranes is required, especially to further assess toxicological profile. We investigated interaction between N-decanoyl acid surfactants phospholipid bilayers simple vitro models comparison sodium dodecyl...
Leishmaniasis is a neglected tropical disease which presents significant global health challenges due to the lack of effective vaccines and limitations existing chemotherapeutics in view their toxicity, resistance, high costs. In this study, we realized library novel bisindole derivatives as potential anti‐leishmanial agents through rapid Suzuki‐Miyaura coupling reaction, utilizing NH2‐unprotected bromobisindoles ethanamines boronic acids. Optimization reaction conditions allowed for...
Abstract The design of compounds selective for the MT 1 melatonin receptor is still a challenging task owing to limited knowledge structural features conferring selectivity subtype, and only few have been reported so far. N ‐(Anilinoalkyl)amides are versatile class ligands that include nonselective /MT 2 agonists ‐selective antagonists. We synthesized new series ‐(anilinoalkyl)amides bearing 3‐arylalkyloxy or 3‐alkyloxy substituents at aniline ring, looking potent ligands. To evaluate effect...