5922-21-4Relevant academic research and scientific papers
A simple and efficient synthesis of novel inhibitors of alpha-glucosidase based on benzimidazole skeleton and molecular docking studies
?zil, Musa,Emirik, Mustafa,Etlik, Semiha Y?lmaz,ülker, Serdar,Kahveci, Bahittin
, p. 226 - 235 (2016)
A novel series of benzimidazole derivatives were prepared starting from o-phenylenediamine and 4-nitro-o-phenylenediamine with iminoester hydrochlorides. Acidic proton in benzimidazole was exchanged with ethyl bromoacetate, then ethyl ester group was transformed into hydrazide group. Cyclization using CS2/KOH leads to the corresponding 1,3,4-oxadiazole derivative, which was treated with phenyl isothiocyanate resulted in carbothioamide group, respectively. As the target compounds, triazole derivative was obtained under basic condition and thiadiazole derivative was obtained under acidic condition from cyclization of carbothioamide group. Most reactions were conducted using both the microwave and conventional methods to compare yields and reaction times. All compounds obtained in this study were investigated for α-glucosidase inhibitor activity. Compounds 6a, 8a, 4b, 5b, 6b and 7b were potent inhibitors with IC50 values ranging from 10.49 to 158.2?μM. This has described a new class of α-glucosidase inhibitors. Molecular docking studies were done for all compounds to identify important binding modes responsible for inhibition activity of α-glucosidase.
Rapid synthesis and lipase inhibition activity of some new benzimidazole and perimidine derivatives
Mente?e,Y?lmaz,Karaali,ülker,Kahveci
, p. 336 - 342 (2014/06/09)
This study presents a synthesis of new series of some benzimidazole, bisbenzimidazole and perimidine derivatives via microwave technique, which, leads to the good product yields and short reaction times. The structure of newly synthesized compounds was confirmed by 1H NMR and 13C NMR spectra. These compounds were screened for their lipase inhibition activity. Then, all compounds were evaluated with regard to pancreatic lipase activity, and some of the 2-substituted perimidines, bisperimidine and bisbenzimidazole derivatives showed lipase inhibition at various concentrations.
Microwave-assisted synthesis of some 2-substituted quinazolin-4(3H)-one derivatives from iminoester hydrochlorides
Mentese, Emre,Kahveci, Bahittin
, p. 147 - 150 (2015/01/16)
Herein, a method that involves a reaction of iminoester hydrochloride with methyl anthranilate via microwave assisted synthesis is reported. This efficient procedure provides pure products within few minutes. This method can be used as a general technique for synthesizing quinazoline derivatives.
