The ongoing quest to discover effective treatments for diseases remains a significant challenge for the scientific community. Multicomponent reactions (MCRs) have emerged as powerful tools in accelerating drug discovery, enabling the rapid generation of chemical libraries with high diversity in a time-efficient and environmentally sustainable manner. In this review, we focus on central nervous system (CNS) disorders, particularly Alzheimer's disease, Parkinson's disease, schizophrenia, depression, and epilepsy, where MCRs have contributed to the development of promising ligands in recent years.
View Article and Find Full Text PDFJ Med Chem
July 2024
Cannabinoid receptor subtype 2 (CB2R) is emerging as a pivotal biomarker to identify the first steps of inflammation-based diseases such as cancer and neurodegeneration. There is an urgent need to find specific probes that may result in green and safe alternatives to the commonly used radiative technologies, to deepen the knowledge of the CB2R pathways impacting the onset of the above-mentioned pathologies. Therefore, based on one of the CB2R pharmacophores, we developed a class of fluorescent -adamantyl-1-alkyl-4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives spanning from the green to the near-infrared (NIR) regions of the light spectrum.
View Article and Find Full Text PDFBackground: Limited serial neuroimaging studies use magnetic resonance imaging (MRI) to define the evolution of hypoxic-ischemic insults to the brain of term infants and encompass both the primary injury and its secondary impact on cerebral development. The optimal timing of MRI to fully evaluate the impact of hypoxic-ischemic encephalopathy on brain development and associated neurodevelopmental sequelae remains unknown.
Methods: Goals: (a) review literature related to serial neuroimaging in term infants with HIE; (b) describe pilot data in two infants with HIE treated with therapeutic hypothermia who had a brain injury at day 3-5 and underwent four additional MRIs over the next 12 weeks of life and developmental evaluation at 24 months of age.