Efficient synthesis of 2-[(3,4-dichlorophenyl)methyl]-1h-benzimidazole derivatives, and their ?-glucosidase inhibitory and antioxidant activities

In this work, some new 2-[(3,4-dichlorophenyl)methyl]-1H-benzimidazole derivatives containing different five-membered heterocycles like 1,3,4-oxadiazole, 1,3,4-triazole, and 1,3,4-thiadiazole moieties were designed and efficiently synthesized starting from 2-[(3,4-dichlorophenyl) methyl]-1H-benzimidazole. The products were screened for their in vitro antioxidant and ?-glucosidase inhibitory activities. Among the synthesized compounds, some of them showed efficient ?-glucosidase inhibition with IC50 values ranging between 16.05 ± 0.94 and 77.02 ± 1.12 µg/mL when they were compared with the standard ?-glucosidase inhibitor acarbose having IC50 value 12.04 ± 0.68 µg/mL. The antioxidant activity of all products was screened by using various in vitro antioxidant assays, including CUPric Reducing Antioxidant Capacity (CUPRAC) and Ferric Reducing Antioxidant Power (FRAP) assays. Also, the radical scavenging activities of the products were assayed by using the ABTS method. © 2020 Bentham Science Publishers.Recep Tayyip Erdogan Üniversitesi: 2014.102.02.02This work was supported by Recep Tayyip Erdogan University Scientific Research Project Unit (RTEUBAP) under the project number of 2014.102.02.02. The authors thank all theoclalguees inethrpoject unit foretirhuspports

Synthesis and In Vitro Urease Inhibition of Some Novel Benzimidazole-based Hydrazones

WOS: 000479700000001A novel series of N '-(substituted benzylidene)-2-(5,6-dichloro-2-methyl-1H-benzimidazol-1-yl)acetohydrazides and N '-(1-(substituted phenyl)ethylidene)-2-(5,6-dichloro-2-methyl-1H-benzimidazol-1-yl)acetohydrazides were synthesized and then studied for their urease inhibitory activities using thiourea as a standard drug. All newly synthesized compounds were found to exhibit potent inhibitory properties against urease enzyme in the range of IC50 = 0.0155 +/- 0.0039-0.0602 +/- 0.0071 mu M, when compared with the thiourea as standard (IC50 = 0.5115 +/- 0.0233 mu M). All target molecules were characterized by H-1-NMR, C-13-NMR, IR, and electrospray ionization mass spectrometry