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At a time of global health crisis, fear, anxiety, and stress levels increase. The effects of protracted social isolation, and media related misinformation's about the coronavirus disease 2019 (COVID-19) resulting in increased fear/stress related to the insufficiently known illness. The aim was to assess the influence of the COVID-19 health crisis on patients with chronic inflammatory demyelinating polyradiculoneuropathy (CIDP). A cross-sectional study on 29 adult CIDP patients was performed. The Medical Research Council scale was used to evaluate muscle strength. The degree of functional disability was measured using the Inflammatory Neuropathy Cause and Treatment disability scale. The overall quality of life (QoL) was self-estimated on a 0-100 numeric rating scale. We also used a specifically designed 22-question-survey about COVID-19. Regarding the COVID-19 pandemic, 62% of CIDP patients were concerned. The daily activities of 55% of patients were negatively influenced by the pandemic. During the COVID-19 outbreak, 21% of patients reported their CIDP got worse. In 39% of CIDP patients, the influence of the pandemic on CIDP therapy was reported (reducing the dose or time interval or even discontinuation). The mean value of the self-estimated QoL was 64±19. Independent predictors of worse QoL were age of patients (beta=-0.35, p<0.05) and fear of the COVID-19 (beta=-0.34, p<0.05). The COVID-19 pandemic has a significant impact on CIDP patients. Besides the direct influence of the virus and fear of the virus, restrictive measures can indirectly harm the patients with CIDP. The COVID-19 pandemic has a significant impact on CIDP patients. Besides the direct influence of the virus and fear of the virus, restrictive measures can indirectly harm the patients with CIDP.Four new chromene derivatives, pestalotiochromenoic acids A - D (1, 2, 4, and 5), and two new chromone derivatives, pestalotiochromones A and B (6 and 7), were obtained from the marine alga-derived fungus Pestalotiopsis neglecta SCSIO41403, as well as a reported derivate named piperochromenoic acid (3) with its configuration determined for the first time. Their structures were determined by detailed nuclear magnetic resonance (NMR) and mass spectroscopic analyses, while the absolute configurations were established by theoretical NMR and electronic circular dichroism (ECD) calculation, including Mo2(OAc)4-induced ECD experiments. Those chromene and chromone derivatives displayed weak cytotoxicity, but showed obvious liver X receptors (LXRs) modulatory activities, by in vitro tests on the expression of LXRα, LXRβ and theirtarget gene ABCA1, as well as in silico docking analysis. Moreover, the high binding affinities between pestalotiochromone A (6) and LXRα, revealed by surface plasmon resonance (SPR) with the dissociation equilibrium constant (KD) value of 6.2 μM, demonstrated 6 could act as a new potential LXR agonist.Organic anion-transporting polypeptide 2B1 (OATP2B1) is a multispecific membrane transporter mediating the cellular uptake of various exo- and endobiotics, including drugs and steroid hormones. Increased uptake of steroid hormones by OATP2B1 may increase tumor proliferation. Therefore, understanding OATP2B1's substrate/inhibitor recognition and inhibition of its function, e.g., in hormone-dependent tumors, would be highly desirable. To identify the crucial structural features that correlate with OATP2B1 inhibition, here we designed modifications at four positions of the estrane skeleton. 13α- or 13β-estrone phosphonates modified at ring A or ring D were synthesized. Hirao and Cu(I)-catalyzed azide-alkyne click reactions served in the syntheses as key steps. 13β-Derivatives displayed outstanding OATP2B1 inhibitory action with IC50 values in the nanomolar range (41-87 nM). A BODIPY-13α-estrone conjugate was additionally synthesized, modified at C-3-O of the steroid, containing a four-carbon linker between the triazole moiety and the BODIPY core. The fluorescent conjugate displayed efficient, submicromolar OATP2B1 inhibitory potency. The newly identified inhibitors and the structure-activity relationships specified here promote our understanding about drug recognition of OATP2B1.Alkaloids and phenols are potent inhibitors family for many enzymes used in many therapies. We aim to evaluate in vitro and in silico, the inhibition effect of Hispidin, Harmaline, and Harmine as pure molecules to bovine milk xanthine oxidase (BXO), Molecular docking and SAR study with GOLD was done to explain the mechanism of action related to its inhibition, ADMET parameters were checked to confirm their pharmacokinetics (PK) using preADMET 2.0 server, we classified our inhibitors by applying five drug-likeness rules, the best-ranked inhibitors were chosen based on the approved ADMET properties, drug-likeness qualifications, and the best PLPchem score generated by GOLD. The in vitro results show important inhibition activity to BXO comparing to the control with an IC50 of 39.72 ± 3.60 µM, 51.00 ± 1.0 µM, and 48.52 ± 1.76 µM for Hispidin, Harmaline, and Harmine respectively. The in silico results show that Hispidin was the best inhibitor model with approved ADMET properties and qualification in all drug-likeness rules; Harmaline was saved second-best model to BXO with suitable ADMET properties and qualified in most drug-likeness rules. Eventually, Harmine was ranked third potent inhibitor model with acceptable ADMET properties, drug-likeness rules, and PLPchem score. The tested inhibitors could be significant in drug discovery, especially in treating gout disease; therefore, drug development, including clinical trials, should be done with promising results.Thirty novel 2,5-disubstituted-1,3,4-oxadiazole derivatives bearing urea moiety were designed and synthesized. https://www.selleckchem.com/products/ly333531.html IR, 1H-NMR, 13C-NMR and mass spectroscopic methods and elemental analysis were used to confirm the structures of the compounds. Their monoamine oxidase inhibitory activity was determined against the MAO-A and MAO-B isoforms. None of the compounds showed the potent MAO-A inhibitory activity, while the MAO-B inhibition was significantly found in the range of 62 to 98%. Among them, the compounds H8, H9 and H12 bearing chloro substituent at the fourth position of phenylurea were found to show potent monoamine oxidase B inhibitory activity with IC50 values 0.039-0.066 µM. To define and evaluate the interaction mechanism between compound H8 and monoamine oxidase B, molecular docking studies have been made.
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