Recommanded Product: 3141-27-3In 2022 ,《Synthesis, molecular docking, and biological evaluation of 5-alkyl(aryl)-2-isobutylthiazole derivatives as α-amylase, α-glucosidase, and protein kinase inhibitors》 was published in Applied Organometallic Chemistry. The article was written by Khan, Siraj; Bugday, Nesrin; Rehman, Asim Ur; Haq, Ihsan Ul; Yasar, Sedat; Ozdemir, Ismail. The article contains the following contents:
A series of 18 biol. active C5-arylated-2-isobutylthiazoles (aryl = Ph, 4-MeCOC6H4, 4-methyl-1-naphthyl, 5-formyl-2-furyl, etc.) was synthesized from 2-isobutylthiazole and the corresponding aryl bromides via C-H bond activation using Pd-NHC complexes [Pd(μ-Cl)Cl(NHC)]2 [NHC = 1,3-bis(2,6-dimethylphenyl)imidazolylidene] and [LCl2Pd-NHC] (L = PPh3, pyridine, 3-formylpyridine). All Pd-NHC complexes were prepared and characterized by 1H NMR, 13C NMR and FTIR spectroscopy, quadrupole-time of flight-liquid chromatog./mass spectroscopy (Q-TOF-LC/MS), gas chromatog.-mass spectrometry (GCMS), and m.p. techniques. The physicochem. properties, pharmacokinetics and drug-likeness of the thiazole products were calculated by SwissADME. PkCSM database was used to calculated the toxicity profile. Almost all the compounds showed no to low toxicity. All the products were addnl. assessed in vitro for their antidiabetic potential using α-amylase and α-glucosidase inhibitory activities. Except for 7 compounds, the prepared thiazoles showed good α-glucosidase inhibitory potential (IC50 7.17 ± 0.201 to 74.08 ± 0.244μg/mL) when compared with acarbose standard (IC50 16.59 ± 0.135μg/mL). All compounds had moderate to good inhibitory potential against the α-amylase enzyme, with IC50 values ranging from 12.00 ± 0.289 to 76.15 ± 0.477μg/mL. The protein kinase inhibition potential was determined for the first time, and 7 compounds showed activity with the zone of inhibition in the range of 9 ± 1.3 to 19 ± 1.5 mm. The ligands and active site binding interactions of α-glucosidase, α-amylase, and protein kinase enzymes were also studied using mol. modeling. In the experiment, the researchers used many compounds, for example, 2,5-Dibromothiophene(cas: 3141-27-3Recommanded Product: 3141-27-3)
2,5-Dibromothiophene(cas: 3141-27-3) , is mainly used as pharmaceutical intermediate and synthesis intermediate. 2,5-Dibromothiophene polymerizes by debromination with magnesium catalyzed by nickel compounds to form poly(2,5- thienylene) .Recommanded Product: 3141-27-3
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary