Small-molecule heterocycles bearing orthogonal functionality have the potential to deliver diverse structural motifs that aid the drug-discovery effort. This work highlights how a readily assembled N-hydroxyethyl pyrazole trifluoroborate offers rapid access to architecturally distinct 5-6-6- and 5-7-6-fused tricyclic compounds. This chemistry is not only amenable to single compound synthesis, but also to high-throughput experimentation. It gives easy access to diverse compound arrays with various physicochemical and ADME profiles by fully automated library synthesis. The combination of the high-throughput experimentation with rapid testing of the compounds in an integrated physicochemical and ADME profiling workflow allows accelerated design of novel lead compounds in drug-discovery projects.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1002/cmdc.202000187 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Optimization design and application of library face recognition access control system based on improved PCA.
PLoS One
January 2025
College of Artificial Intelligence Technology, Changchun Institute of Technology, Changchun, China.
The application of face recognition technology in Library Access Control System (LACS) has an important impact on improving the security and management efficiency of the library. However, the traditional face recognition methods have some limitations in the face of complex environmental conditions such as illumination and posture change. To solve this problem, an improved method combining the Aggregating Spatial Embeddings for Face Recognition (ASEF) algorithm and Principal Component Analysis (PCA) is proposed.
View Article and Find Full Text PDFOptimizing Ultrasound Probe Disinfection for Healthcare-Associated Infection Control: A Comparative Analysis of Disinfectant Efficacy.
Microorganisms
November 2024
School of Pharmacy, Polo Medicina Sperimentale e Sanità Pubblica "Stefania Scuri", Via Madonna delle Carceri 9, 62032 Camerino, Italy.
Ultrasound is a key diagnostic tool in modern medicine due to its ability to provide real-time, high-resolution images of the internal structures of the human body. Despite its undeniable advantages, there are challenges related to the contamination of ultrasound probes, with the risk of healthcare-associated infections. The aim of this review was to identify the most effective disinfectants for disinfecting ultrasound probes to prevent the transmission of pathogens between patients.
View Article and Find Full Text PDFThe influence of electronic health record design on usability and medication safety: systematic review.
BMC Health Serv Res
January 2025
School of Pharmacy and Biomolecular Sciences (PBS), Royal College of Surgeons in Ireland (RCSI), 1st Floor Ardilaun House Block B, 111 St Stephen's Green, Dublin 2, Ireland.
Background: The advantages of electronic health records (EHRs) are well-documented regarding the process of care, enhanced data accessibility and cost savings. However, EHR design can also contribute to usability challenges, with poorly designed EHRs being implicated in user errors including patient overdoses. Our study seeks to evaluate how EHR design influences both usability and medication safety.
View Article and Find Full Text PDFTiRobot-assisted versus freehand femoral neck system placement in the treatment of femoral neck fractures: a systematic review and meta-analysis.
J Robot Surg
January 2025
The Third Ward of Orthopaedic Department, General Hospital of Ningxia Medical University, 804 Shengli South Street, Hui Autonomous Region, Yinchuan, Ningxia, 750004, People's Republic of China.
The purpose of this study is to assess the safety and effectiveness of TiRobot-assisted treatment for femoral neck fractures, in comparison to traditional freehand treatment methods. Throughout the research process, we conducted an extensive literature search across numerous databases, including PubMed, EMBASE, Cochrane Library, Web of Science, China National Knowledge Infrastructure (CNKI), CQVIP, and Wanfang. Based on the literature screening criteria, we selected six studies, encompassing 358 cases of femoral neck fracture patients, for this meta-analysis.
View Article and Find Full Text PDF3D CT to 2D X-ray image registration for improved visualization of tibial vessels in endovascular procedures.
Int J Comput Assist Radiol Surg
January 2025
Department of Medical Biophysics, University of Toronto, Toronto, Canada.
Article Synopsis
- The study aims to improve visualization of arteries during endovascular procedures for peripheral artery disease by using an image registration technique that fuses X-ray and CT angiography images.
- The method involved aligning digital images based on the positions of the bones and achieved successful registration in most cases, with accurate alignment of less than 1 mm in distance.
- The results indicate that this technique is clinically viable for guiding interventions, as it allows for early detection of potential complications like guidewire perforations while maintaining a reasonable processing time.
Want 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!