Ciprofloxacin (CPX) is one of the most employed antibiotics in clinics to date. However, the rise of drug-resistant bacteria is dramatically impairing its efficacy, especially against life-threatening pathogens, such as
This essay picks up a few threads in the ongoing debate on national identity in Italy. Immigration and the intertwining of cultures locally have stretched the contours of the nation state to a breaking point. As a result, the social self has become a sharply contested terrain between those who want to install a symbolic electronic fence around an imagined fatherland and those who want a more inclusive nation at home in a global world. After discussing the views of Amin Maalouf (2000), Alessandro Dal Lago (2009), Abdelmalek Sayad (1999) and Patrick Manning (2005) on national identity and migration in the first half, the essay goes on in the second half to examine the powerful contribution to the debate by leading Italian Romani intellectual, Santino Spinelli (2012), and Romanologist Lorenzo Monasta (2008). The depth of the current identity crisis in Italy makes this country an ideal laboratory to probe new approaches on the subject.
The antimicrobial properties of one of the most important secondary metabolites, Eugenol (EU), inspired us to design and synthesize three different series of derivatives enhancing its parent compound’s anti-Helicobacter pylori activity. Thus, we prepared semisynthetic derivatives through (A) diazo aryl functionalization, (B) derivatization of the hydroxy group of EU, and (C) elongation of the allyl radical by incorporating a chalcogen atom. The antibacterial evaluation was performed on the reference NCTC 11637 strain and on three drug-resistant clinical isolates and the minimal inhibitory and bactericidal concentrations (MICs and MBCs) highlight the role of chalcogens in enhancing the antimicrobial activity (less than 4 µg/mL for some compounds) of the EU scaffold (32–64 µg/mL).
Introduction Vibrio cholerae bacteria cause an infection characterized by acute diarrheal illness in the intestine. Cholera is sustained by people swallowing contaminated food or water. Even though symptoms can be mild, if untreated disease becomes severe and life-threatening, especially in low-income countries.
Exploring the chemical diversity and molecular mechanisms of natural products continues to be an important research area for identifying novel promising therapeutic approaches for fighting cancer. This is a complex disease and poses important challenges, which require not only targeted interventions to improve chemotherapy efficacy and tolerability, but also adjuvant strategies to counteract chemoresistance development and relapses.
Responsiveness of liposomes to external stimuli, such as light, should allow a precise spatial and temporal control of release of therapeutic agents or ion transmembrane transport. Here, some aryl-azo derivatives of thymol are synthesized and embedded into liposomes from 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine to obtain light-sensitive membranes whose photo-responsiveness, release behaviour, and permeability towards Cl
ABSTRACTABSTRACTIntroduction Human African Trypanosomiasis is a neglected disease caused by infection from parasites belonging to the Trypanosoma brucei species. Only six drugs are currently available and employed depending on the stage of the infection: pentamidine, suramin, melarsoprol, eflornithine, nifurtimox, and fexinidazole. Joint research projects were launched in an attempt to find new therapeutic options for this severe and often lethal disease.Areas covered After a brief description of the recent literature on the parasite and the disease, we searched for patents dealing with the proposal of new antitrypanosomiasis agents and, following the PRISMA guidelines, we filtered the results to those published from 2018 onwards returning suitable entries, which represent the contemporary landscape of compounds/strategies against Trypanosoma brucei. In addition, some relevant publications from the overall scientific literature were also discussed.Expert opinion This review comprehensively covers and analyzes the most recent advances not only in the discovery of new inhibitors and their structure–activity relationships but also in the assessment of innovative biological targets opening new scenarios in the MedChem field. Finally, also new vaccines and formulations recently patented were described. However, natural and synthetic compounds were analyzed in terms of inhibitory activity and selective toxicity against human cells.KEYWORDS: Trypanosoma bruceicysteine proteaseinhibitorsdihydrofolate reductasepterine reductase 1oxaborole analoguesfusaricidin Ahuman African trypanosomiasis Article highlights The current status of the anti-trypanosomal therapy was updated.New therapeutic targets in Trypanosoma brucei-related diseases emerged in the last 5 years.Newly synthesized molecules and naturally occurring bacterial metabolites were licensed as anti-T. brucei agents.Peptidomimetic drugs, aliphatic macrocycles, oxaborole analogues, and heterocycles are the most studied scaffolds in this field.Compounds were herein described in terms of inhibitory activity against the parasite's infection and selective toxicity against human cells.Declaration of interestThe authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.Reviewer disclosuresPeer reviewers on this manuscript have no relevant financial or other relationships to disclose.Authors contributionsF Melfi and E Haloci searched for the literature. C Campestre, A Ammazzalorso, and R Grande filtered the search results. All the authors analyzed the data. F Melfi, S Carradori, and I D'Agostino wrote the manuscript. All the authors read and approved the final version of the manuscript.Additional informationFundingThis paper was not funded.
