SDS of cas: 16629-19-9In 2021 ,《Synthesis, biological evaluation and molecular docking study of some new rohitukine analogs as protein tyrosine phosphatase 1B inhibitors》 was published in Bioorganic Chemistry. The article was written by Balaramnavar, V. M.; Srivastava, R.; Varshney, S.; Kumar, S.; Rawat, A. K.; Chandasana, H.; Chhonker, Y. S.; Bhatta, R. S.; Srivastava, A. K.; Gaikwad, A. N.; Lakshmi, V.; Saxena, A. K.. The article contains the following contents:
Rohitukine (RH) I [R = H] was derivatized to different aryl sulfonated derivatives I [R = 4-MeC6H4SO2, 2-O2NC6H4SO2, 2-thienylsulfonyl, etc.] by treating with the corresponding aryl sulfonyl chlorides. These derivatives were tested in-vitro on protein tyrosine phosphatase 1B (PTP1B) inhibition. Among these the active compounds I [R = 4-O2NC6H4SO2, 3-O2NC6H4SO2, 2,4,6-tri-MeC6H2SO2, 1-naphthylsulfonyl] significantly inhibited the PTP1B by 51.3%, 65.6%, 71.9%, and 55.9% resp. at 10μg/mL, the results were also supported by in-silico docking experiments The most potent compound I [R = 2,4,6-tri-MeC6H2SO2] was analyzed for antidiabetic and antidyslipidemic activity in vivo. It showed a marked reduction in blood glucose level (random and fasting) and serum insulin level in db/db mice. It improved glucose intolerance as ascertained by the oral glucose tolerance test (OGTT). These NCEs (New Chem. Entities) also lowered cholesterol and triglyceride profiles while improved high-d. lipoprotein cholesterol in db/db mice. The compound I [R = 2,4,6-tri-MeC6H2SO2] was further evaluated for antiadipogenic activity on MDI (Methylisobutylxanthine, dexamethasone, and insulin)-induced adipogenesis, where it significantly inhibited MDI-induced adipogenesis in 3 T3-L1 preadipocytes, at 10μM and 20μM concentration These results were compared with the parent compound I [R = H] which inhibited 35% and 45% lipid accumulation while the RH analog compound I [R = 2,4,6-tri-MeC6H2SO2] inhibited the lipid accumulation by 41% and 51% at 10 and 20μM concentration, resp. These results well corroborated with in-silico studies. The experimental process involved the reaction of Thiophene-2-sulfonyl chloride(cas: 16629-19-9SDS of cas: 16629-19-9)
Thiophene-2-sulfonyl chloride(cas: 16629-19-9) is a member of sulfonyl chlorides. Sulfonyl chlorides are reactive sulfonic acid derivatives similar in properties and reactivity to acid chlorides of carboxylates. The sulfonic acid group, however, is a highly hindered molecule, containing a tetrahedral configuration of substituents. SDS of cas: 16629-19-9
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics