A5088371344- Malaria Research and Control
- Computational Drug Discovery Methods
- Synthesis and biological activity
- HIV/AIDS drug development and treatment
- Nanoparticle-Based Drug Delivery
- Pomegranate: compositions and health benefits
- Synthesis and Catalytic Reactions
- Organic Chemistry Cycloaddition Reactions
- Chemical Synthesis and Analysis
- Cancer therapeutics and mechanisms
- Analytical Chemistry and Chromatography
- Phytochemistry and Bioactivity Studies
- Bioactive Natural Diterpenoids Research
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Nanoplatforms for cancer theranostics
- Inflammatory mediators and NSAID effects
- Plant-based Medicinal Research
- Chemical Synthesis and Reactions
- Synthesis and Biological Evaluation
- Research on Leishmaniasis Studies
- Gold and Silver Nanoparticles Synthesis and Applications
- Drug Transport and Resistance Mechanisms
- Bioactive Compounds and Antitumor Agents
- Botanical Research and Chemistry
- Advanced Synthetic Organic Chemistry
University of Milan
2012-2023
Mylan (Switzerland)
2015
Ospedale San Pietro Fatebenefratelli
2007
University of Florida
2006
GTx (United States)
2006
University of Wisconsin–Madison
1993-1994
University of Wisconsin System
1994
Sapienza University of Rome
1991-1993
The sun-dried rind of the immature fruit pomegranate (Punica granatum) is presently used as a herbal formulation (OMARIA, Orissa Malaria Research Indigenous Attempt) in Orissa, India, for therapy and prophylaxis malaria. pathogenesis cerebral malaria, complication infection by Plasmodium falciparum, an inflammatory cytokine-driven disease associated to up-regulation activity metalloproteinase-9 increase TNF production. vitro anti-plasmodial Punica granatum (Pg) was recently described. aim...
Malaria is an infectious disease caused by Plasmodium parasites. It results in annual death-toll of ~ 600,000. Resistance to all medications currently use exists, and novel antimalarial drugs are urgently needed. Plasmepsin V (PmV) essential protease a highly promising target, which still lacks molecular characterization drug-like inhibitors. PmV, cleaving the PExEl motif, key enzyme for PExEl-secretion, indispensable parasitic process virulence infection. Here, we describe accessibility PmV...
Gold nanocages (AuNCs) have been shown to be a useful tool for harnessing imaging and hyperthermia therapy of cancer, thanks their unique optical properties, low toxicity, facile surface functionalization. Herein, we use AuNCs selective targeting prostate cancer cells (PC3) via specific interaction between neuropeptide Y (NPY) receptor three different NPY analogs conjugated AuNCs. Localized plasmon resonance band the nanoconjugates was set around 800 nm, which is appropriate in vivo...
The aim of this study was to develop new antiplasmodial compounds acting through distinct mechanisms during both the liver and blood stages parasite life cycle. Compounds were designed on basis "double-drug" approach: primaquine, which has been linked statine-based inhibitors plasmepsins (PLMs), plasmodial aspartic proteases involved in degradation hemeoglobin. tested vitro for anti-PLM I/PLM II activities against chloroquine-sensitive (D10) chloroquine-resistant (W2) strains P. falciparum....
Our previous studies showed that (-)-epigallocatechin-3-gallate (EGCG) inhibits signal transducer activator of transcription 1 (STAT1) activation. Since EGCG may be a promising lead compound for new anti-STAT1 drug design, 15 synthetic catechins, characterized by the (-)-gallocatechin-3-gallate stereochemistry, were studied in human mammary MDA-MB-231 cell line to identify minimal structural features preserve activity. We demonstrate presence three hydroxyl groups B ring and one group D is...
Au naturel! (+)-Usnic acid (green) is a weak antimalarial agent, however, in conjugation with known scaffolds and drugs, such as dihydroartemisinin (blue), potent activity against the blood-stage parasite can be seen both vitro vivo. The compound shown exhibits an IC(50) value of 1.4 nM Plasmodium falciparum proved nearly efficacious artesunate mouse model infection.
Natural products are a prolific source for the identification of new biologically active compounds. In present work, we studied in vitro and vivo antimalarial efficacy ADME-Tox profile molecular hybrid (AM1) between 4-aminoquinoline quinolizidine moiety derived from lupinine (Lupinus luteus). The aim was to find compound endowed with target product profile-1 (TCP-1: molecules that clear asexual blood-stage parasitaemia), proposed by Medicine Malaria Venture accomplish goal malaria...
Abstract New therapeutics are urgently needed to fight tuberculosis and mycobacteria‐related diseases that a major health hazard especially in poor countries. Natural products have been the source of important antitubercular drugs past still need receive attention as potent reservoir chemical structures. Fifteen known two new (+)‐usnic acid (a benzofurandione formerly isolated from lichens) enamines hydrazones here described tested against sensitive multidrug‐resistant strains mycobacteria....
The 4-aminoquinoline drugs, such as chloroquine (CQ), amodiaquine or piperaquine, are still commonly used for malaria treatment, either alone (CQ) in combination with artemisinin derivatives. We previously described the excellent vitro activity of a novel pyrrolizidinylmethyl derivative 4-amino-7-chloroquinoline, named MG3, against P. falciparum drug-resistant parasites. Here, we report optimized and safer synthesis now suitable scale-up, its additional vivo characterization. MG3 is active...
Combining chemicals. Malaria is one of the most widespread parasitic infections in world, however, unavailability a vaccine and spread intensification drug resistance over past 15–20 years have led to dramatic decline efficacy affordable antimalarial drugs. Herein, development “double-drugs” tackle inhibition P. falciparum growth discussed. Supporting information for this article available on WWW under http://www.wiley-vch.de/contents/jc_2452/2008/z700166_s.pdf or from author. Please note:...
Here we report synthetic methodology affording in the most efficient way rapid preparation of new dithiolethiones (DTTs) and methanethiosulfonates (MTSs).These were evaluated as STAT3 inhibitors since these electrophilic systems could react with thiol groups STAT3-SH2 domain.The results showed that MTSs strongly interacted SH2 domain, whereas corresponding DTTs possessed lower affinity, independently from nature linked heterocyclic scaffold.