On February 28, 2022, Daud, Saima; Abid, Obaid-ur-Rahman; Sardar, Asma; Shah, Basit Ali; Rafiq, Muhammad; Wadood, Abdul; Ghufran, Mehreen; Rehman, Wajid; Zain-ul-Wahab; Iftikhar, Fatima; Sultana, Rifhat; Daud, Habiba; Niaz, Basit published an article.Related Products of 2010-06-2 The title of the article was Design, synthesis, in vitro evaluation, and docking studies on ibuprofen derived 1,3,4-oxadiazole derivatives as dual α-glucosidase and urease inhibitors. And the article contained the following:
Present study aimed at the discovery of new non-sugar α-glucosidase inhibitors included synthesis of a series of 1,3,4-oxadiazole based Schiff base derivatives of ibuprofen. Initially oxadiazoles from ibuprofen were synthesized by treating ibuprofen hydrazide with carbon disulfide. Oxadiazoles upon treatment with different substituted phenacyl bromides gave acylated 1,3,4-oxadizole derivatives I [R1 = 2-MeC6H4, 3-MeC6H4, 4-MeC6H4, 4-PhC6H4, 2-O2NC6H4] which further react with amines to gave 1,3,4-oxadiazole based Schiff base derivatives of ibuprofen II [R1 = 2-MeC6H4, 3-MeC6H4, 4-MeC6H4, 4-PhC6H4, 2-O2NC6H4; R2 = Ph, 2-MeC6H4, 2-(4-Ph)thiazolyl]. Synthesized ibuprofen derivatives were characterized by 1H NMR, 13C NMR and HRMS (EI). These derivatives were evaluated in vitro for their α-glucosidase and urease inhibitory activity. In case of α-glucosidase enzyme, all the synthesized derivatives showed potent inhibition in comparison to standard acarbose and the most potent amongst these was the compoundsII [R1 = 4-PhC6H4, R2 = 2-(4-Ph)thiazolyl; R1 = 3-H3CC6H4, R2 = Ph] having IC50 value 16.01 ± 1.27μM and 39.06 ± 0.27μM, resp. In case of urease enzyme, the synthesized derivatives showed varying degree of inhibitory potential, however, potent inhibition was shown by I [R1 = 2-O2NC6H4] (IC50 = 9.36 ± 1.02μM), I [R1 = 4-MeC6H4] (IC50 = 17.65 ± 1.03μM), II [R1 = 4-PhC6H4, R2 = 2-(4-Ph)thiazolyl] (IC50 = 18.29 ± 1.26μM), I [R1 = 2-MeC6H4] (IC50 = 19.52 ± 1.25μM) and II [R1 = 4-PhC6H4, R2 = 2-H3CC6H4] (IC50 = 19.63 ± 1.08μM). The mol. docking was performed in order to check binding interactions between the synthesized derivatives and the enzymes. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Related Products of 2010-06-2
The Article related to oxadiazole schiff base preparation alpha glucosidase inhibitor urease docking, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Related Products of 2010-06-2
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica