New imidazoline/α2-adrenoceptors affecting compounds—4(5)-(2-aminoethyl)imidazoline (dihydrohistamine) derivatives. Synthesis and receptor affinity studies

Identification of Small Molecule Inhibitors of Amyloid β-Induced Neuronal Apoptosis Acting through the Imidazoline I2 Receptor

“…Characterization of the affinity profile of compounds 9 , 10 , and 17 across a set of 19 AD-relevant targets revealed that their mechanisms of action are unique as compared to those established for current AD drugs and other multitarget strategies proposed recently. − Essentially, apart from the low micromolar affinity identified for I 2 ( 9 , 10 , and 17 ), I 1 ( 9 ), and σ-1 ( 17 ) receptors, no significant affinity (<20% at 10 μM) is obtained for any of the other 16 AD-relevant targets screened, including classical AD targets such as MAO-B, AChE, and NMDAR, the latter two linked to FDA-approved AD drugs such as donepezil, galantamine, and rivastigmine, on one side, and Memantine, on the other side . Thus, molecules 9 , 10 , and 17 exemplify that it is possible to achieve neuroprotective levels similar to or better than Memantine (Figure ), through a NMDAR-independent mechanism of action that involves interacting with the I 2 receptor (Figure ).…”

Improvements in Efficiency and Selectivity for C–F Bond Halogen-Exchange Reactions by Using Boron Reagents

“…This thermodynamic driving force in boron-mediated C-F functionalization results in halex being applicable to perfluorinated centers, such as the trifluoromethyl group, which Brønsted acids, and a myriad of other strong conditions, do not modify. 21,50 This is notable, as it opens the possibility of the trifluoromethyl group to be used as an alterable site, and perhaps even a functional group handle. Unlike the trifluoromethyl group, tribromomethyl (CBr3) and trichloromethyl (CCl3) centers are moderately reactive, with known transformations to generate heterocycles, alkynes, alkenes, esters, cyano groups, and others.…”