Multitarget Approach for the Treatment of Alzheimer’s Disease: Inhibition of Phosphodiesterase 9 (PDE9) and Histone Deacetylases (HDACs) Covering Diverse Selectivity Profiles was written by Rabal, Obdulia;Sanchez-Arias, Juan A.;Cuadrado-Tejedor, Mar;de Miguel, Irene;Perez-Gonzalez, Marta;Garcia-Barroso, Carolina;Ugarte, Ana;Estella-Hermoso de Mendoza, Ander;Saez, Elena;Espelosin, Maria;Ursua, Susana;Tan, Haizhong;Wu, Wei;Xu, Musheng;Pineda-Lucena, Antonio;Garcia-Osta, Ana;Oyarzabal, Julen. And the article was included in ACS Chemical Neuroscience in 2019.Computed Properties of C9H8BrFO2 This article mentions the following:
Here, we present a series of dual-target phosphodiesterase 9 (PDE9) and histone deacetylase (HDAC) inhibitors devised as pharmacol. tool compounds for assessing the implications of these two targets in Alzheimer’s disease (AD). These novel inhibitors were designed taking into account the key pharmacophoric features of known selective PDE9 inhibitors as well as privileged chem. structures, bearing zinc binding groups (hydroxamic acids and ortho-amino anilides) that hit HDAC targets. These substituents were selected according to rational criteria and previous knowledge from our group to explore diverse HDAC selectivity profiles (pan-HDAC, HDAC6 selective, and class I selective) that were confirmed in biochem. screens. Their functional response in inducing acetylation of histone and tubulin and phosphorylation of cAMP response element binding (CREB) was measured as a requisite for further progression into complete in vitro absorption, distribution, metabolism and excretion (ADME) and in vivo brain penetration profiling. Compound 31b, a selective HDAC6 inhibitor with acceptable brain permeability, was chosen for assessing in vivo efficacy of these first-in-class inhibitors, as well as studying their mode of action (MoA). In the experiment, the researchers used many compounds, for example, Ethyl 4-bromo-3-fluorobenzoate (cas: 1130165-74-0Computed Properties of C9H8BrFO2).
Ethyl 4-bromo-3-fluorobenzoate (cas: 1130165-74-0) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. alpha-Bromoesters are employed in the Reformatsky reaction for the synthesis of beta-hydroxyesters. Bromine-containing agents predominate because not only are they more efficient than similar chlorine-containing species, but also the high atomic weight of bromine ensures that it is present in a high mass fraction within most organobromine compounds.Computed Properties of C9H8BrFO2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary