Zhang, Rui published the artcileDesign, synthesis, and biological evaluation of tetrahydroisoquinolines derivatives as novel, selective PDE4 inhibitors for antipsoriasis treatment, Safety of 2-Bromoethyl Methyl Sulfone, the publication is European Journal of Medicinal Chemistry (2021), 113004, database is CAplus and MEDLINE.
In this study, a series of novel tetrahydroisoquinoline I [R1 = CHO, CH2CH2SO2Me, CH2CO2Me, etc.; configuration = S, Rac, R], II [R2 = Bn, Et; R3 = CO2Me, CHO, etc.; configuration = S, Rac] and III [R4 = Et, Me; R5 = 5-phenyl-1H-indolyl, 5-methoxy-1H-indolyl, etc.; configuration = S, Rac] were developed based on the crystal structure of PDE4D in complex with I [R1 = CHO, configuration = S]. Anti-inflammatory effects of these compounds were evaluated and III [R4 = Me, R5 = 7-chloro-1H-indolyl, configuration = S] with high safety, permeability and selectivity, exhibited significant inhibitory potency against the enzymic activity of PDE4D and the TNF-α release from the LPS-stimulated RAW 264.7 and hPBMCs. Moreover, an in-vivo study demonstrated that a topical administration of III [R4 = Me, R5 = 7-chloro-1H-indolyl, configuration = S] achieved more significant efficacy than calcipotriol to improve the features of psoriasis-like skin inflammation. Overall, this study provided a basis for further development of tetrahydroisoquinoline-based PDE4 inhibitors against psoriasis.
European Journal of Medicinal Chemistry published new progress about 16523-02-7. 16523-02-7 belongs to bromides-buliding-blocks, auxiliary class Bromide,Sulfone,Aliphatic hydrocarbon chain, name is 2-Bromoethyl Methyl Sulfone, and the molecular formula is C8H16N2O, Safety of 2-Bromoethyl Methyl Sulfone.
Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary