This study involved the synthesis of several new derivatives of progesterone, 11a-hydroxyprogesterone, 11a-t-butyldimethylsilanyloxyprogesterone, and andrenosterone. The new derivatives were prepared by condensation of the 4-en-3-one moiety of the four steroids with 2-hydroxy-1-naphthaldehyde to afford a series of 4-(R)-hydroxy-(2-hydroxynaphtalen-1-yl) adducts. These adducts were further modified by cyclization reactions of the dihydroxynaphthalenyl moieties with succinic acid, and the resulting cyclic succinates were then condensed with ethylenediamine to form imine derivatives at all available carbonyl groups. These compounds were then derivatized by N-acylation of the 11- and 17-imine nitrogens with chloroacetyl chloride and the resulting chloroacetamides were then condensed with 2-hydroxy-1-napthaldehyde in Darzens-type reactions forming the corresponding epoxy acetamides in the side chains. In addition, the chemical structure of steroid derivatives was confirmed by NMR spectroscopic data.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.steroids.2016.04.012 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Quantification of ivermectin in veterinary products consumed off-label as a treatment for COVID-19.
Pharmazie
December 2024
Centre of Excellence for Pharmaceutical Sciences (Pharmacen™), North-West University, Potchefstroom, Republic of South Africa.
The COVID-19 pandemic caused global pandemonium, and due to an unprecedented global response, the popularity and use of (veterinary) ivermectin, amongst many other conceivable 'treatments', experienced a meteoric rise. Ivermectin is a macrocyclic lactone compound belonging to the avermectin drug class and is a registered medicine in many countries, although the most common use is as veterinary medicine. In this study, a fast HPLC method was developed and validated for the quantification of ivermectin in veterinary products that were used off-label by a substantial number of people during COVID-19.
View Article and Find Full Text PDFCorrelations between postmortem quantitative MRI parameters and demyelination, axonal loss and gliosis in multiple sclerosis: A systematic review and meta-analysis.
Brain Imaging Behav
January 2025
Macquarie Medical School, Macquarie University, Sydney, NSW, Australia.
Magnetic resonance imaging (MRI) is frequently used to monitor disease progression in multiple sclerosis (MS). This study aims to systematically evaluate the correlation between MRI measures and histopathological changes, including demyelination, axonal loss, and gliosis, in the central nervous system of MS patients. We systematically reviewed post-mortem histological studies evaluating myelin density, axonal loss, and gliosis using quantitative imaging in MS.
View Article and Find Full Text PDFSystematic Review of Hybrid Vision Transformer Architectures for Radiological Image Analysis.
J Imaging Inform Med
January 2025
School of Computing, Informatics, and Decision Systems Engineering, Arizona State University, Tempe, AZ, USA.
Vision transformer (ViT)and convolutional neural networks (CNNs) each possess distinct strengths in medical imaging: ViT excels in capturing long-range dependencies through self-attention, while CNNs are adept at extracting local features via spatial convolution filters. While ViT may struggle with capturing detailed local spatial information, critical for tasks like anomaly detection in medical imaging, shallow CNNs often fail to effectively abstract global context. This study aims to explore and evaluate hybrid architectures that integrate ViT and CNN to leverage their complementary strengths for enhanced performance in medical vision tasks, such as segmentation, classification, reconstruction, and prediction.
View Article and Find Full Text PDFAutomated Integration of AI Results into Radiology Reports Using Common Data Elements.
J Imaging Inform Med
January 2025
Department of Radiology, University of Pennsylvania Perelman School of Medicine, 3400 Spruce St., Philadelphia, PA, 19104, USA.
Integration of artificial intelligence (AI) into radiology practice can create opportunities to improve diagnostic accuracy, workflow efficiency, and patient outcomes. Integration demands the ability to seamlessly incorporate AI-derived measurements into radiology reports. Common data elements (CDEs) define standardized, interoperable units of information.
View Article and Find Full Text PDFAdipose-derived stem cells regulate mitochondrial dynamics to alleviate the aging of HFF-1 cells.
In Vitro Cell Dev Biol Anim
January 2025
Department of Outpatient Service, The Affiliated Nanhua Hospital, Hengyang Medical School, University of South China, Hengyang, 421002, Hunan, China.
The objective of this study is to explore how adipose-derived stem cells (ASCs) regulate mitochondrial structure and function and the impact of this regulation on slowing cellular senescence. HFF-1 cells were induced by HO to establish a cellular senescence model, and ASCs or Mdivi-1 (mitochondrial fission inhibitor) was added. MTT examined the cell proliferation; flow cytometry detected mitochondrial membrane potential as well as apoptosis and cell cycle; kit measured ATP production; ELISA analyzed the levels of interleukin-6 (IL-6), interleukin 1 beta (IL-1β), tumor necrosis factor alpha-like (TNF-α), glutathione (GSH), malondialdehyde (MDA), and superoxide dismutase (SOD); Western blotting and qRT-PCR detected the expression of protein and mRNA levels; and β-galactosidase staining observed the degree of cellular senescence.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!