Open Access. Powered by Scholars. Published by Universities.®
Physical Sciences and Mathematics Commons™
Open Access. Powered by Scholars. Published by Universities.®
Articles 1 - 2 of 2
Full-Text Articles in Physical Sciences and Mathematics
Enabling Technologies For Medicinal Chemistry And Synthesis: I. Cannabinoids; Ii. Illudalic Acid; Iii. Microwave Chemistry, Harvey Fulo
Graduate Theses, Dissertations, and Problem Reports
Innovations in synthetic organic chemistry such as methodology improvements, new chemical transformations and technology development significantly impact medicinal chemistry and continue to drive the drug discovery process. Here, new cyclization strategies to the pharmaceutically underexplored 3,3-dimethylcyclopentane-fused aromatic rings are described. One approach highlighted oxidative cycloisomerization, intermolecular [2+2+2] cyclotrimerization and 5-exo-dig cyclization providing indanoylindole cannabinoids that possess high affinity for human CB2 receptors at nanomolar concentration and good selectivity index. Another featured a [4+2]-type benzannulation reaction which enabled the 5-step synthesis of illudalic acid — compared to the current available sequences (≥16 steps) — and its equipotent and LAR-selective analogs. …
Biocompatible And Multifunctional Trityl Spin Probes For Electron Paramagnetic Resonance Spectroscopy, Teresa D. Gluth
Biocompatible And Multifunctional Trityl Spin Probes For Electron Paramagnetic Resonance Spectroscopy, Teresa D. Gluth
Graduate Theses, Dissertations, and Problem Reports
The primary objective of my thesis was to develop and utilize a biocompatible multifunctional trityl spin probe for concurrent measurement of pO2, pHe, and [Pi] in vivo by electron paramagnetic resonance (EPR) spectroscopy (Chapter 2). My first goal was to synthesize the proposed probe we are terming HOPE71. Secondly, HOPE71 was characterized by X-band and L-band EPR spectroscopy. Next, the biocompatibility of HOPE71 was assessed through an albumin binding test, cytotoxicity assays, and in vivo intravenous tolerance. Then, the use of HOPE71 to measure the target parameters was demonstrated in a breast cancer …