Abstract

Dhaval M. Patel^1*, Nirmal K. Patel², Sunil M. Khristi², Arvnabh Mishra¹

DOI : http://dx.doi.org/10.13005/ojc/380331

New derivatives of benzimidazole were synthesized which were containing 1- and 2-substituted 5- nitro benzimidazole derivatives. The presence of specific functional group was confirmed by IR spectroscopic analysis. The determination of structure for the synthesized compounds was confirmed by 1-H proton magnetic resonance. Anthelmintic activity of the derivatives was investigated and compared with standard FDA approved anthelmintic drug albendazole. The obtained results show that out of the investigated compositions 100mg/ml were found much active compound in paralyzing and death of the earth worm that shows the time of paralysis 20 minute and the time of death stage is 24 minutes. In silico ADMET and pharmacokinetic parameters of compounds (DP-1 to DP-3) were also evaluated for drug likeliness. Calculations related to protein binding, blood–brain barrier (BBB), MDCK cell permeability, Caco-2 cell permeability and human oral absorption in the gastrointestinal tract showed that these values for the derivatives (DP-1-DP-3) fell within the standard ranges generally observed for drugs.

Anthelmintic activity; Anti-oxidant activity; Benzimidazole; Earth worm Paralysis; In-silico ADMET Study; Nitration; Spectroscopy

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