Chemistry and properties of fluorescent pyrazole derivatives: an approach to bioimaging applications.

Fluorescent bioimaging is a crucial technique for studies in real cell samples, providing vital information about the metabolism of ions or molecules of biological and pharmaceutical significance. This technique typically uses probes based on organic small-molecule fluorophores, with N-heteroaromatic scaffolds playing an essential role due to their exceptional electronic properties and biocompatibility. Among these, pyrazole derivatives stand out as particularly promising due to their high synthetic versatility and structural diversity.

Impact of mental disorders on low adherence to antiretroviral therapy in people living with HIV in Spain.

The relationship between mental disorders other than depression or anxiety, and low adherence to both antiretroviral treatment (ART) and linkage to HIV care are unclear. The aim of our study was to compare the prevalence of mental disorders in people living with HIV (PLHIV) in Spain who present low versus high adherence to ART. We performed a cross-sectional study comparing two groups of PLHIV: 20 PLHIV with low adherence and 80 PLHIV with high adherence to ART.

Valproic acid could help in the fight against COVID-19: A case-control study.

Objective: There is early evidence about Valproic acid (VPA) antiviral effect. Our aim was to investigate the incidence and severity of SARS-CoV-2 infection in VPA users as compared with the general population.

Material And Methods: A case-control study nested within a cohort, carried out between March 1 and December 17, 2020.

Patient Participant Perspectives on Implementation of Long-Acting Cabotegravir and Rilpivirine: Results From the Cabotegravir and Rilpivirine Implementation Study in European Locations (CARISEL) Study.

Introduction: CARISEL is an implementation-effectiveness "hybrid" study examining the perspectives of people living with HIV-1 (patient study participants [PSPs]) on cabotegravir (CAB) plus rilpivirine (RPV) long-acting (LA) dosed every 2 months (Q2M) across 5 European countries.

Methods: PSPs completed questionnaires on acceptability (Acceptability of Intervention Measure), appropriateness (Intervention Appropriateness Measure), and feasibility (Feasibility of Intervention Measure) at their first (Month [M] 1), third (M4), and seventh (M12) injection visits. Semistructured qualitative interviews were also conducted.

Dolutegravir/Lamivudine Efficacy and Safety Outcomes in People With HIV-1 With or Without Historical Resistance Results at Screening: 48-Week Pooled Analysis.

Background: Drug resistance testing aids in appropriate antiretroviral therapy selection to improve treatment success but may not be readily available. We evaluated the impact of switching to dolutegravir/lamivudine (DTG/3TC) using pooled data from the TANGO and SALSA trials in adults who were virologically suppressed with or without historical resistance results at screening.

Methods: Adults who were virologically suppressed (HIV-1 RNA <50 copies/mL for >6 months) with no prior virologic failure were randomized to switch to DTG/3TC (TANGO, n = 369; SALSA, n = 246) or continue their current antiretroviral regimen (CAR; TANGO, n = 372; SALSA, n = 247).

Microwave-assisted synthesis and functionalization of 2-arylimidazo[1,2-]pyrimidin-5(8)-ones.

Despite the limited applications and scarcity of commercial examples of imidazo[1,2-]pyrimidines, their exceptional properties hold great potential, representing a significant challenge in discovering more critical applications. Herein, we present a microwave-assisted approach for preparing 2-arylimidazo[1,2-]pyrimidin-5(8)-ones and their alkylation and bromination products using easily accessible and inexpensive reagents, thus offering a promising avenue for further search. Notably, the photophysical properties of an -alkyl derivative were investigated, and the results highlight the high potential of these compounds as modular fluorophores.

CsCO-Promoted Alkylation of 3-Cyano-2(1H)-Pyridones: Anticancer Evaluation and Molecular Docking.

Herein, a CsCO-promoted N-alkylation of 3-cyano-2(1H)-pyridones containing alkyl groups with diverse alkyl halides to synthesize N-alkyl-2-pyridones over O-alkylpyridines is reported. The use of alkyl dihalides resulted in complex mixtures of N- and O-alkylated products. The primary factor influencing regioselectivity in these reactions is the electronic effects of substituents on the 2(1H)-pyridone ring, as evidenced by the preferential formation of O-alkylpyridines upon the introduction of aryl groups.

Health-Related Quality of Life in People with Advanced HIV Disease, from 1996 to 2021: Systematic Review and Meta-analysis.

The purpose of the study was to assess the effects of advanced HIV disease (AHD) on health-related quality of life (HRQoL) in PLHIV, the changes in HRQoL outcomes over the last 25 years, and the differences between countries according to level of economic development. We conducted a systematic review and meta-analysis. The search was conducted in PubMed and Web of Science using the terms: "health-related quality of life", "HQRoL", "HIV", "AIDS", "advanced HIV disease" and "low CD4 cells".

A Deep Learning Approach for Fear Recognition on the Edge Based on Two-Dimensional Feature Maps.

Applying affective computing techniques to recognize fear and combining them with portable signal monitors makes it possible to create real-time detection systems that could act as bodyguards when users are in danger. With this aim, this paper presents a fear recognition method based on physiological signals obtained from wearable devices. The procedure involves creating two-dimensional feature maps from the raw signals, using data augmentation and feature selection algorithms, followed by deep learning-based classification models, taking inspiration from those used in image processing.

A Randomized Trial of Dolutegravir Plus Darunavir/Cobicistat as a Switch Strategy in HIV-1-Infected Patients With Resistance to at Least 2 Antiretroviral Classes.

Background: Suppressed patients with drug-resistant HIV-1 require effective and simple antiretroviral therapy to maintain treatment adherence and viral suppression.

Methods: This randomized, open-label, noninferiority, multicenter pilot study involved HIV-infected adults who met the following criteria: confirmed HIV-1 RNA <50 copies/mL for ≥6 months preceding the study randomization, treatment with at least 3 antiretroviral drugs, and a history of drug resistance mutations against at least 2 antiretroviral classes but remaining fully susceptible to darunavir (DRV) and integrase inhibitors. Participants were randomized 1:1 to switch to dolutegravir (DTG; 50 mg once per day) plus DRV boosted with cobicistat (DRV/c; 800/150 mg once per day; 2D group) or continue with their baseline regimen (standard-of-care [SOC] group).

Evaluation of the validity of the HPV viral load compared to conventional techniques for the detection of high-grade anal intraepithelial lesions in men with HIV who have sex with men.

Background: The incidence of high-grade anal intraepithelial lesions (HSILs) has increased in recent years among men who have sex with men with human immunodeficiency virus (HIV). This work evaluated the validity of the human papilloma virus viral load (HPV-VL) versus cytological and qualitative HPV results to detect HSILs.

Methods: From May 2017 to January 2020, 93 men who have sex with men and HIV were included in an anal cancer screening program from the Infectious Diseases Unit at a tertiary-care hospital in Alicante (Spain).

Effectiveness and safety of integrase strand transfer inhibitors in Spain: a prospective real-world study.

Introduction: Second-generation integrase strand transfer inhibitors (INSTIs) are preferred treatment options worldwide, and dolutegravir (DTG) is the treatment of choice in resource-limited settings. Nevertheless, in some resource-limited settings, these drugs are not always available. An analysis of the experience with the use of INSTIs in unselected adults living with HIV may be of help to make therapeutic decisions when second-generation INSTIs are not available.

Antineutrophil Cytoplasmic Antibody (ANCA)-Associated Aortitis Presenting With Acute Dissection: Case Report and Comprehensive Literature Review.

Description Vasculitides are a group of diseases that produces vasculitis, which is characterized by inflammatory infiltrates within blood vessel walls and results in intimal injury as well as progressive mural destruction. Infiltrates are characterized per the Chapel Hill classification, into large, medium, and small-vessel vasculitides. ANCA-associated vasculitis (AAV) is a disease that has been described as involving small-sized vessels.

Synthesis of structural analogues of Reversan by ester aminolysis: an access to pyrazolo[1,5-]pyrimidines from chalcones.

Reversan, a multidrug resistance-associated protein (MRP1) inhibitor described more than a decade ago, is a commercial drug (CAS: 313397-13-6) that has a high price and is six to eight times more potent than known drug transporter inhibitors. However, to date, a complete route for synthesizing pyrazolo[1,5-]pyrimidine-based Reversan is yet to be published. Herein, the silica gel-mediated synthesis of Reversan and a novel family of its structural analogues (amides) the microwave-assisted amidation reaction of 3-carboethoxy-5,7-diphenylpyrazolo[1,5-]pyrimidine (ester) with primary amines is reported.

Integrated analysis of industrial limitations and image quality: an end-to-end design approach.

There is a trend in optical system design toward explicitly considering real-world industrial demands in the metrics to be optimized, from which emerges a cost-performance trade-off. Another relevant recent tendency is the so-called end-to-end design, where the design metric is an expected quality index of the final image, after digital restoration. We propose an integrated approach for analyzing the cost-performance trade-off in end-to-end designs.

Beyond hyperglycemia: glycaemic variability as a prognostic factor after acute ischemic stroke.

Introduction: Glycaemic variability (GV) refers to variations in blood glucose levels, and may affect stroke outcomes. This study aims to assess the effect of GV on acute ischaemic stroke progression.

Methods: We performed an exploratory analysis of the multicentre, prospective, observational GLIAS-II study.

Robust numerical solution to the Levi-Civita wavefront coupling problem via level set computation of the point characteristic function.

The Levi-Civita wavefront coupling problem consists of, given two prescribed wavefronts, obtaining a refractive or reflective surface coupling them. We propose a robust numerical method to solve Levi-Civita's problem, whose rationale is to consider that Levi-Civita's solutions are level surfaces of the point characteristic function established between points of incoming and outgoing wavefronts. The method obtains both surface data points and their normals, enabling a more robust surface reconstruction.

Photophysical and anion sensing properties of a triphenylamine-dioxaborinine trimeric compound.

Herein, we report the synthesis and photophysical characterization of the novel tris(4-(2,2-difluoro-6-methyl-2-1λ,3,2λ-dioxaborinin-4-yl)phenyl)amine trimeric probe (A2) the reaction between triphenylamine (1), acetic anhydride, and BF·OEt implying the twelve new bond formation in a one-pot manner. This highly fluorescent compound in solution ( up to 0.91 at 572 nm) and solid state ( = 0.

Knowledge and Perceived Emotions Regarding an Anal Cancer Preventive Program in People Diagnosed With HIV: A Qualitative Study.

Background: To the best of our knowledge, no studies have yet examined the emotional repercussions of the care processes among people infected with the human immunodeficiency virus who participate in preventive anal cancer screening programs.

Objective: This study aimed to explore the knowledge, emotions, sexuality, barriers, and facilitators perceived by this patient group during the process of anal cancer screening and diagnosis.

Methods: Detailed, semistructured, qualitative interviews were completed with 17 men and 3 women to explore their knowledge, experiences, and emotions regarding the screening process.

BF-Mediated Acetylation of Pyrazolo[1,5-]pyrimidines and Other π-Excedent (-Hetero)arenes.

An operably simple microwave-assisted BF-mediated acetylation reaction of pyrazolo[1,5-]pyrimidines and a plausible mechanism based on density functional theory (DFT) theoretical calculations for this transformation are reported. Remarkably, and to the best of our knowledge, this is the first example of the direct acetylation for the functional pyrazolo[1,5-]pyrimidine (PP) core. The synthesis of this essential building block is reported in high yields using mild reaction conditions, inexpensive reagents, and even substrates with electron-deficient or highly hindered groups.