The "Click-tail approach" for the design and synthesis of novel carbonic anhydrase inhibitors

The Carbonic Anhydrases (CAs) are a family of zinc enzymes deputed to the interconversion of carbonic dioxide to hydrogen carbonate. Herein, we report on a sustainable modular strategy, also called "clicktail approach", used to obtain two series of 4-(4-substituted-lH-l,2,3-triazol-lyl) benzenesulfonamides. Design and synthesis strategies, x-ray derived CA-ligand binding mode and enzyme-based inhibition results will be presented

Searching for novel carbonic anhydrase inhibitors: from virtual screening to the lab bench

Carbonic Anhydrases (CAs) are zinc metalloenzymes that catalyze the reversible hydration of carbon dioxide to bicarbonate both in prokaryotes and eukaryotes. In this context, Computer Aided Drug Design strategies have emerged as powerful tools in the modern drug discovery paradigm. In particular, using ligand- and pharmacophore-based virtual screening approaches, we identified novel chemical entities with original chemotypes, that showed an interesting and selective inhibitory activity in nanomolar/low micromolar range toward CA I and CAII, isoforms. Herein, we present the hit-to-lead optimization process for these prototypes

Perinatal Depression and Anxiety Symptoms, Parental Bonding and Dyadic Sensitivity in Mother–Baby Interactions at Three Months Post-Partum

The quality of the early parent-infant relationship is crucial for the child's optimal development, and parental sensitivity plays a key role in early interactions. The purpose of the study was to evaluate the influence of maternal perinatal depression and anxiety symptoms on dyadic sensitivity at three months post-partum, also considering a large set of maternal and infant variables. At the third trimester of pregnancy (T1) and at three months postpartum (T2), 43 primiparous women filled in a set of questionnaires evaluating symptoms of depression (CES-D) or anxiety (STAI), the woman's parental bonding experiences (PBI), alexithymia (TAS-20), maternal attachment to the baby (PAI, MPAS) and the perceived social support (MSPSS). At T2 mothers also completed a questionnaire on infant temperament and took part in the CARE-Index videotaped procedure. Dyadic sensitivity was predicted by higher maternal trait anxiety scores in pregnancy. In addition, the mother's experience of being cared for by her father in childhood was predictive of her infant's lower compulsivity, while paternal overprotection predicted higher unresponsiveness. The results highlight the influence of perinatal maternal psychological well-being and maternal childhood experiences on the quality of the dyadic relationship. The results may be useful to foster mother-child adjustment during the perinatal period

Gender and country differences in academic motivation, coping strategies, and academic burnout in a sample of Italian and Russian first-year university students

Background: The first year of university represents a challenging period that requires students to make significant investments in adaptive resources to face the new academic environment. The present study intends to contribute to the controversial discussion of gender differences in academic motivation, coping strategies, and academic burnout. This cross-sectional study examined above-mentioned constructs among first-year university students in a cross-cultural context. Methods: The sample consisted of 637 Italian and 496 Russian first-year university students (n = 1133), 40.3% of whom were females. The participants’ ages ranged from 17 to 23 years, with a mean age of 18.75 years (SD = 1.07). To assess academic motivation, coping strategies, and academic burnout, participants responded to the Academic Motivation Scale (AMS), the Coping Inventory for Stressful Situations (CISS), and the Maslach Burnout Inventory–Student Survey (MBI–SS) application. Results: The findings reveal gender and country differences in academic motivation, emotion and avoidance oriented coping strategies, and emotional exhaustion and expands previous studies in this educational area. Conclusion: Given the technical nature of the research topic, the target audience for our study is academic career guidance practitioners, who can apply the findings to the design of effective programmes aimed at improving positive academic goals and reducing the tendency to switch academic courses or abandon the university among first-year students

Antibiotic susceptibility profiles of ropy slime-producing Leuconostoc mesenteroides isolated from cooked meat products

The transfer of antibiotic resistance via the food chain is a global concern. Nevertheless, more attention is required to non-pathogenic strains, such as spoilage bacteria, which could transmit genes to pathogens. Although Lactic Acid Bacteria are microorganisms generally recognized as safe, Leuconostoc mesenteroides may reach and maintain high concentration levels on the surface of cooked products and ready-to-eat products throughout the entire shelf life. It is therefore important to consider the possibility for this species to carry antibiotic- resistance genes. The present research deals with the antibiotic susceptibility profile of strains of L. mesenteroides, isolated from vacuum packaged cooked meat products. In this study, the antimicrobial susceptibility of L.mesenteroides, previously isolated from cooked ham, was investigated through disk diffusion assay according to CLSI standards. Isolated strains from ready-to-eat food show high levels of resistance to ampicillin and methicillin and, according to a settled panel of 21 antibiotics, the antibiotic resistance was demonstrated for the 50% of the tested molecules

Inhibition of ?±-class cytosolic human carbonic anhydrases I II IX and XII and ?²-class fungal enzymes by carboxylic acids and their derivatives: New isoform-I selective nanomolar inhibitors

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Effects of UV irradiation in a continuous turbulent flow UV reactor on microbiological and sensory characteristics of cow's milk.

The dairy industry under current pasteurization conditions (15 s at 72°C) and sanitary standards achieves a safe product with excellent quality. In an ever-competitive market there is still a need to improve product quality and extend shelf life of dairy products to increase competitiveness and open up new markets. In an attempt to test the effect of UV irradiation on microbiota of fluid milk, a continuous flow UV system at 254 nm was used to treat 3.5 and 2% fat milk at two UV doses (880 and 1,760 J liter(-1)). Milk was obtained from three processors, and two lots from each processor were assessed. To assess the impact on the most descriptive native microbiota in pasteurized milk after UV illumination, the product was held at two storage temperatures (4 and 7°C) and tested weekly for 5 weeks for aerobic plate counts (psychrotrophic and mesophilic bacteria), laboratory pasteurization counts, aerobic sporeformers, coliform organisms, and titratable acidity. Microbial counts for all tested microorganisms were lower in UV-treated milk when compared with control throughout storage at 4 and 7°C in both 3.5 and 2% fat milk. Sensory analysis indicated that there is a sensory defect associated with UV treatment at the wavelength used

Relationship between prehistoric settlements and landscape evolution in the central western coast of Sardinia (Gulf of Oristano)

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In vitro bactericidal activities of various extracts of saffron (Crocus sativus L.) stigmas from Torbat-e Heydarieh, Gonabad and Khorasan, Iran

Saffron is one of the most expensive spices in the world (20,000 €/kg) and this is due not only to the high demand for its various uses such as cooking, production of staining medicines, cosmetics etc., but also for the high costs of cultivation and production. Several studies have demonstrated that differences in saffron quality are mainly due to the methodology followed in the processing of stigmas, and environmental conditions independent of the origin. Some authors found phenotypic variations within cultivated saffron, but very limited genetic diversity. The reason for the very limited genetic diversity in cultivated saffron is explained by its asexual mode of reproduction (propagation). The aim of this study was to assess the antimicrobial activity of stigma saffron, which were tested against different bacteria strains. The results obtained from the antimicrobial activity study indicate that stigmas of C. sativus have some antimicrobial effect