A series of 5-alkylaminolquinolines was designed and synthesized as potential novel CRF(1) receptor antagonists. The structure-activity relationships (SARs) of the substituents on each position (R(2), R(3), R(5) and R(5')) were investigated.
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http://dx.doi.org/10.1016/j.bmcl.2012.05.066 | DOI Listing |
Cell Rep
January 2025
State Key Laboratory of Natural Medicines, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, Jiangsu, China. Electronic address:
Sterols target sterol-sensing domain (SSD) proteins to lower cholesterol and circulating and hepatic triglyceride levels, but the mechanism remains unclear. In this study, we identify acyl-coenzyme A (CoA) synthetase long-chain family member 1 (ACSL1) as a direct target of ergosterol (ES). The C-terminal domain of ACSL1 undergoes conformational changes from closed to open, and ES may target the drug-binding pocket in the acetyl-CoA synthetase-like domain 1 (ASLD1) of ACSL1 to stabilize the closed conformation and maintain its activity.
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January 2025
Department of Mathematical Sciences, Faculty of Science, Somali National University, Mogadishu Campus, Mogadishu, Somalia.
In recent years, machine learning has gained substantial attention for its ability to predict complex chemical and biological properties, including those of pharmaceutical compounds. This study proposes a machine learning-based quantitative structure-property relationship (QSPR) model for predicting the physicochemical properties of anti-arrhythmia drugs using topological descriptors. Anti-arrhythmic drug development is challenging due to the complex relationship between chemical structure and drug efficacy.
View Article and Find Full Text PDFInt Dent J
January 2025
Department of Microbiology, University of Dhaka, Dhaka, Dhaka, Bangladesh.
Hydroxyapatite nanoparticles (HANPs) are becoming increasingly crucial in dental implant applications as they are highly compatible with biological systems, actively support biological processes, and closely resemble bone minerals. This review covers the latest progress in how HANPs are made, studied, and used in dentistry. It looks at critical methods for creating HANPs, such as sol-gel, microwave hydrothermal synthesis, and biomimetic approaches, and how they affect the particles' size, structure, and activity.
View Article and Find Full Text PDFInt J Biol Macromol
January 2025
Department of Materials Engineering, Materials and Energy Research Center, Dezful Branch, Islamic Azad University, Dezfool, Iran.
Polymer-based nanocomposite coatings that are enhanced with nanoparticles have gained recognition as effective materials for antibacterial purposes, providing improved durability and biocidal effectiveness. This research introduces an innovative chitosan-based polymer nanocomposite, enhanced with titanium oxide nanopowders and carbon quantum dots. The material was synthesized via the sol-gel process and applied to 316L stainless steel through dip-coating.
View Article and Find Full Text PDFInt J Biol Macromol
January 2025
Xiamen Meijiamei New Material Technology Co., Ltd., Xiamen 361110, PR China. Electronic address:
Natural polymer based food packaging has attracted more and more attention, but the lack of active functions of natural polymer hinders its application in the field of active packaging. In this study, chlorogenic acid carbon dots (CGA-CDs) was synthesized mildly using natural plant polyphenol CGA as carbon source, and CGA functionalized layered clays (LDHs@CGA) was introduced as reinforcing agent. Alg active films were fabricated by solution casting method using natural polysaccharide-alginate (Alg), CGA-CDs and LDHs@CGA.
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