1,721,120 research outputs found
The 1-(2,3-dichlorophenyl)-piperazine-to-aripiprazole ratio at steady state in rats and schizophrenic patients
No full textUnlocking the potential of biostimulants in sustainable agriculture: Effect of wood distillate on the nutritional profiling of apples
Full text linkIn this work, we report the investigation of the effect of exposure of apple trees to the bioeffector wood distillate (WD), a plant biostimulant used for improving the nutritional profiling of crop plants. We measured the effect by evaluating the biochemical and nutritional profile of both pulps and skin of fruits. WD (0.2 %, v/v) was applied once a week by foliar application, from May 2023 until September 2023. The results indicate that the WD-treated apples have a significant increase in several analyzed parameters (i.e., phenols, flavonoids, tannins, total antioxidant power, sugars, pectin, free amino acids, and mineral element content), especially in the pulp. These data were also confirmed by NMR and LC-ESI-MS techniques. This study pointed out that WD could be a handy tool for the cultivation of fruit trees
Metalloenzyme Inhibitors against Zoonotic Infections: Focus on Leishmania and Schistosoma
No full textThe term “zoonosis” denotes diseases transmissible among vertebrate animals and humans. These diseases constitute a significant public health challenge, comprising 61% of human pathogens and causing an estimated 2.7 million deaths annually. Zoonoses not only affect human health but also impact animal welfare and economic stability, particularly in low- and middle-income nations. Leishmaniasis and schistosomiasis are two important neglected tropical diseases with a high prevalence in tropical and subtropical areas, imposing significant burdens on affected regions. Schistosomiasis, particularly rampant in sub-Saharan Africa, lacks alternative treatments to praziquantel, prompting concerns regarding parasite resistance. Similarly, leishmaniasis poses challenges with unsatisfactory treatments, urging the development of novel therapeutic strategies. Effective prevention demands a One Health approach, integrating diverse disciplines to enhance diagnostics and develop safer drugs. Metalloenzymes, involved in parasite biology and critical in different biological pathways, emerged in the last few years as useful drug targets for the treatment of human diseases. Herein we have reviewed recent reports on the discovery of inhibitors of metalloenzymes associated with zoonotic diseases like histone deacetylases (HDACs), carbonic anhydrase (CA), arginase, and heme-dependent enzyme
Old but gold: tracking the new guise of Histone Deacetylase 6 (HDAC6) enzyme as a biomarker and therapeutic target in rare diseases
No full textEpigenetic regulation orchestrates many cellular processes and greatly influences key disease mechanisms. Histone deacetylase (HDAC) enzymes play a crucial role either as biomarkers or therapeutic targets owing to their involvement in specific pathophysiological pathways. Beyond their well-characterized role as histone modifiers, HDACs also interact with several nonhistone substrates and their increased expression has been highlighted in specific diseases. The HDAC6 isoform, due to its unique cytoplasmic localization, modulates the acetylation status of tubulin, HSP90, TGF-β, and peroxiredoxins. HDAC6 also exerts noncatalytic activities through its interaction with ubiquitin. Both catalytic and noncatalytic functions of HDACs are being actively studied in the field of specific rare disorders beyond the well-established role in carcinogenesis. This Perspective outlines the application of HDAC(6) inhibitors in rare diseases, such as Rett syndrome, inherited retinal disorders, idiopathic pulmonary fibrosis, and Charcot-Marie-Tooth disease, highlighting their therapeutic potential as innovative and targeted disease-modifying agents
The green chemistry of chalcones: Valuable sources of privileged core structures for drug discovery
Full text linkThe sustainable use of resources is essential in all production areas, including pharmaceuticals. However, the aspect of sustainability needs to be taken into consideration not only in the production phase, but during the whole medicinal chemistry drug discovery trajectory. The continuous progress in the fields of green chemistry and the use of artificial intelligence are contributing to the speed and effectiveness of a more sustainable drug discovery pipeline. In this light, here we review the most recent sustainable and green synthetic approaches used for the preparation and derivatization of chalcones, an important class of privileged structures and building blocks used for the preparation of new biologically active compounds with a broad spectrum of potential therapeutic applications. The literature here reported has been retrieved from the SciFinder database using the term “chalcone” as a keyword and filtering the results applying the concept: “green chemistry”, and from the Reaxys database using the keywords “chalcone” and “green”. For both databases the time-frame was 2017–2022. References were manually selected based on relevance
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