β-Sulfonamido Functionalized Aspartate Analogues as Excitatory Amino Acid Transporter Inhibitors: Distinct Subtype Selectivity Profiles Arising from Subtle Structural Differences was written by Hansen, Jacob C.;Bjoern-Yoshimoto, Walden E.;Bisballe, Niels;Nielsen, Birgitte;Jensen, Anders A.;Bunch, Lennart. And the article was included in Journal of Medicinal Chemistry in 2016.SDS of cas: 777-44-6 This article mentions the following:
In this study inspired by previous work on 3-substituted Asp analogs, the authors designed and synthesized a total of 32 beta-sulfonamide Asp analogs and characterized their pharmacol. properties at the excitatory amino acid transporter subtypes EAAT1, EAAT2 and EAAT3. In addition to several potent EAAT inhibitors displaying IC50 values ∼1 μM at all three subtypes, this elaborate structure-activity-relationship also identified analogs characterized by distinct preference or selectivity for one transporter subtype. Introduction of two fluorine atoms on the Ph ring yielded the analog that displayed an IC50 of 0.8 μM at EAAT1 with a 14- and 9-fold preference over EAAT2 and EAAT3, resp. Conversely, the m-CF3-Ph analog was a potent selective EAAT2-inhibitor (IC50= 2.8 μM) exhibiting 30- and 50-fold selectivity over EAAT1 and EAAT3, resp. In conclusion, even small structural differences in these beta-sulfonamide Asp analogs provide analogs with diverse EAAT subtype selectivity profiles. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6SDS of cas: 777-44-6).
3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations.While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available. Alkyl chlorides readily undergo attack by nucleophiles.SDS of cas: 777-44-6
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics