Kinetic characterization of novel HIV-1 entry inhibitors: discovery of a relationship between off-rate and potency was written by Meuser, Megan E.;Murphy, Michael B.;Rashad, Adel A.;Cocklin, Simon. And the article was included in Molecules in 2018.Name: 1-Boc-Azetidine-3-yl-methanol This article mentions the following:
The entry of HIV-1 into permissible cells remains an extremely attractive and underexploited therapeutic intervention point. We have previously demonstrated the ability to extend the chemotypes available for optimization in the entry inhibitor class using computational means. Here, we continue this effort, designing and testing three novel compounds with the ability to inhibit HIV-1 entry. We demonstrate that alteration of the core moiety of these entry inhibitors directly influences the potency of the compounds, despite common proximal and distal groups. Moreover, by establishing for the first time a surface plasmon resonance (SPR)-based interaction assay with soluble recombinant SOSIP Env trimers, we demonstrate that the off-rate (kd) parameter shows the strongest correlation with potency in an antiviral assay. Finally, we establish an underappreciated relationship between the potency of a ligand and its degree of electrostatic complementarity (EC) with its target, the Env complex. These findings not only broaden the chem. space in this inhibitor class, but also establish a rapid and simple assay to evaluate future HIV-1 entry inhibitors. In the experiment, the researchers used many compounds, for example, 1-Boc-Azetidine-3-yl-methanol (cas: 142253-56-3Name: 1-Boc-Azetidine-3-yl-methanol).
1-Boc-Azetidine-3-yl-methanol (cas: 142253-56-3) belongs to alcohols. Similar to water, an alcohol can be pictured as having an sp3 hybridized tetrahedral oxygen atom with nonbonding pairs of electrons occupying two of the four sp3 hybrid orbitals. Converting an alcohol to an alkene requires removal of the hydroxyl group and a hydrogen atom on the neighbouring carbon atom. Dehydrations are most commonly carried out by warming the alcohol in the presence of a strong dehydrating acid, such as concentrated sulfuric acid.Name: 1-Boc-Azetidine-3-yl-methanol
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts