Tuning Side Arm Electronics in Unsymmetrical Cyclotriazadisulfonamide (CADA) Endoplasmic Reticulum (ER) Translocation Inhibitors to Improve their Human Cluster of Differentiation 4 (CD4) Receptor Down-Modulating Potencies was written by Chawla, Reena;Van Puyenbroeck, Victor;Pflug, Nicholas C.;Sama, Alekhya;Ali, Rameez;Schols, Dominique;Vermeire, Kurt;Bell, Thomas W.. And the article was included in Journal of Medicinal Chemistry in 2016.Reference of 63624-28-2 This article mentions the following:
Cyclotriazadisulfonamide prevents HIV entry into cells by down-modulating surface CD4 receptor expression through binding to the CD4 signal peptide. According to a two-site binding model, 28 new unsym. analogs bearing a benzyl tail group and nine bearing a cyclohexylmethyl tail have been designed and synthesized. The most potent new CD4 down-modulator (40 (CK147); IC50 63 nM) has a 4-dimethylaminobenzenesulfonyl side arm. One of the two side arms was varied with substituents in different positions. This gave a range of CD4 down-modulation potencies that correlated well with anti-HIV-1 activities. The side arms of 21 of the new benzyl-tailed analogs were modeled by means of quantum mech. calculations For CADA analogs with arenesulfonamide side arms, the pIC50 values for CD4 down-modulation correlated with the component of the elec. dipole moment in the aromatic ring, suggesting that an attractive electronic interaction is a major factor determining the stability of the complex between the mol. and its target. In the experiment, the researchers used many compounds, for example, 2,4-Dimethoxybenzene-1-sulfonyl chloride (cas: 63624-28-2Reference of 63624-28-2).
2,4-Dimethoxybenzene-1-sulfonyl chloride (cas: 63624-28-2) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. Organochlorine compounds are lipophylic, meaning they are more soluble in fat than in water. This gives them a high tenancy to accumulate in the food chain (biomagnification).Reference of 63624-28-2
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics