Design and synthesis of cis-2,6-disubstituted N-arylsulfonyl morpholines as novel γ-secretase inhibitors for the potential treatment of Alzheimer's disease (AD) is reported. Several different small alkyl groups are installed on the left-hand side to lower the CYP3A4 liability while maintaining excellent in vitro potency.
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http://dx.doi.org/10.1016/j.bmcl.2010.09.028 | DOI Listing |
Eat Weight Disord
January 2025
Obesity Research Center, Research Institute for Endocrine Sciences, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Objective: This systematic review explores the intricate relationship between body composition, with a specific focus on skeletal muscle mass, and vascular health indices, including measures of arterial stiffness-pulse wave velocity (PWV) and cardio-ankle vascular index (CAVI)-as well as arterial structure, specifically carotid artery intima-media thickness (cIMT).
Methods: An extensive literature search, encompassing PubMed, Scopus, EMBASE, Web of Science, and Google Scholar, was conducted until January 2024. Inclusion criteria involved original observational studies, with cross-sectional or longitudinal designs, reporting body composition parameters and vascular health measures.
BMC Cancer
January 2025
Department of Community & Family Medicine, All India Institute of Medical Sciences, 151001, Bathinda, Punjab, India.
Introduction: Existing evidence suggests a lower uptake of cervical cancer screening among Indian women. Coverage is lower in rural than urban women, but such disparities are less explored. So, the present study was conducted to explore the self-reported coverage of cervical cancer screening in urban and rural areas stratified by socio-demographic characteristics, determine the spatial patterns and identify any regional variations, ascertain the factors contributing to urban-rural disparities and those influencing the likelihood of screening among women aged 30-49 years factors residing in urban, rural, and overall Indian settings.
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January 2025
BBF, Biodiversité et Biotechnologie Fongiques, INRAE, Aix-Marseille Univ, Marseille, France.
Pectin is a complex plant heteropolysaccharide whose structure and function differ depending on its source. In animal feed, breaking down pectin is essential, as its presence increases feed viscosity and reduces nutrient absorption. Soybean meal, a protein-rich poultry feed ingredient, contains significant amounts of pectin, the structure of which remains unclear.
View Article and Find Full Text PDFNat Commun
January 2025
Department of Pharmacy, The First Affiliated Hospital of USTC, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, China.
The difluoromethyl group is a crucial fluorinated moiety with distinctive biological properties, and the synthesis of chiral CF₂H-containing analogs has been recognized as a powerful strategy in drug design. To date, the most established method for accessing enantioenriched difluoromethyl compounds involves the enantioselective functionalization of nucleophilic and electrophilic CF₂H synthons. However, this approach is limited by lower reactivity and reduced enantioselectivity.
View Article and Find Full Text PDFNat Commun
January 2025
Center for Synaptic Neuroscience, Istituto Italiano di Tecnologia, Genova, Italy.
The lack of effective therapies for visual restoration in Retinitis pigmentosa and macular degeneration has led to the development of new strategies, such as optogenetics and retinal prostheses. However, visual restoration is poor due to the massive light-evoked activation of retinal neurons, regardless of the segregation of visual information in ON and OFF channels, which is essential for contrast sensitivity and spatial resolution. Here, we show that Ziapin2, a membrane photoswitch that modulates neuronal capacitance and excitability in a light-dependent manner, is capable of reinstating, in mouse and rat genetic models of photoreceptor degeneration, brisk and sluggish ON, OFF, and ON-OFF responses in retinal ganglion cells evoked by full-field stimuli, with reactivation of their excitatory and inhibitory conductances.
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