340722-36-3Relevant academic research and scientific papers
Biological effects of bis-hydrazone compounds bearing isovanillin moiety on the aldose reductase
Akocak, Suleyman,Beydemir, ?ükrü,Durgun, Mustafa,Esra Duran, Hatice,I??k, Mesut,Lolak, Nebih,Türke?, Cüneyt,Yapar, G?nül
, (2021/11/16)
Aldose reductase (ALR2), one of the metabolically important enzymes, catalyzes the formation of sorbitol from glucose in the polyol pathway. ALR2 inhibition is required to prevent diabetic complications. In the present study, the novel bis-hydrazone compounds bearing isovanillin moiety (GY1-12) were synthesized, and various chromatographic methods were applied to purify the ALR2 enzyme. Afterward, the inhibitory effect of the synthesized compounds on the ALR2 was screened in vitro. All the novel bis-hydrazones demonstrated activity in nanomolar levels as AR inhibitors with IC50 and KI values in the range of 12.55–35.04 nM, and 13.38–88.21 nM, respectively. Compounds GY-11, GY-7, and GY-5 against ALR2 were identified as the highly potent inhibitors, respectively, and were superior to the standard drug, epalrestat. Moreover, a comprehensive ligand-receptor interactions prediction was performed using ADME-Tox, Glide XP, and MM-GBSA modules of Schr?dinger Small-Molecule Drug Discovery Suite to elucidate the novel bis-hydrazone derivatives, potential binding modes versus the ALR2. As a result, these compounds with ALR2 inhibitory effects may be potential alternative agents that can be used to treat or prevent diabetic complications.
Synthesis, antibacterial, antielastase, antiurease and antioxidant activities of new methoxy substitued bis-1,2,4-triazole derivatives
Sokmen, Bahar Bilgin,Gumrukcuoglu, Nurhan,Ugras, Serpil,Ugras, Halil Ibrahim,Yanardag, Refiye
, p. 72 - 77 (2013/04/23)
The methoxy substitued two novel bis triazole-schiff bases (6 a-b) were synthesized with 4-amino-3,5-diethyl-4H-1,2,4-triazole and various bis-aldehydes. Their amine derivatives prepared by reduced with NaBH4 (5 a-b). The obtained products 6 a-b and 7 a-b were identified by FT-IR, H-NMR, 13C-NMR. The bis triazole-schiff bases and amine derivatives were tested for antimicrobial activity using the agar diffusion technique against 11 bacteria. The synthesized compounds (6 a-b and 7 a-b) were screened for their antielastase, antiurease and antioxidant activities. The resuts showed that the synthesized compounds (6 a-b and 7 a-b) had effective antielastase and antiurease activities.
Synthesis of macrocycles derived from vanillin and isovanillin
Kumar,Mashraqui
, p. 5 - 10 (2007/10/03)
Readily available vanillin 1 and isovanillin 2 have been exploited for the first time to synthesise thia and aza-bridged macrocycles. Utilising a common approach, 1 and 2 are first converted into the corresponding key intermediates, dicholoro compounds 5
