Tideglusib and Its Analogues As Inhibitors of Staphylococcus aureus SrtA was written by Yang, Teng;Zhang, Tao;Guan, Xiang-Na;Dong, Ze;Lan, Lefu;Yang, Song;Yang, Cai-Guang. And the article was included in Journal of Medicinal Chemistry in 2020.SDS of cas: 2253-73-8 The following contents are mentioned in the article:
Sortase A (SrtA) anchors surface proteins to the cell wall envelope, and it has attracted increasing interesting as a potential antivirulence target. Several small-mol. inhibitors for SrtA have been developed, but target validation remains largely underexplored. Herein, we report a new class of SrtA inhibitors that supports antivirulence therapy through small-mol. targeting of SrtA. Tideglusib (TD), a drug candidate for myotonic dystrophy, was outstanding in high-throughput screening. A concise synthetic route quickly provided TD analogs, and the structure-activity relationships for SrtA inhibition have been established from those analogs. Several compounds largely retained the in vitro potency and exhibited a better solubility than TD. Addnl., TD attenuated virulence-related phenotypes in vitro and protected mice against lethal S. aureus USA300 bacteremia. Our study indicates that TD and its analogs could be new candidates as SrtA inhibitors with potential in the development of new antivirulence agents. This study involved multiple reactions and reactants, such as Isopropylisothiocyanate (cas: 2253-73-8SDS of cas: 2253-73-8).
Isopropylisothiocyanate (cas: 2253-73-8) belongs to esters. Esters typically have a pleasant smell; those of low molecular weight are commonly used as fragrances and are found in essential oils and pheromones. Esterification is the general name for a chemical reaction in which two reactants (typically an alcohol and an acid) form an ester as the reaction product. Esters are common in organic chemistry and biological materials.SDS of cas: 2253-73-8
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics