SYNTHESIS, CHARACTERIZATION AND EVALUATION OF ANTIMICROBIAL ACTIVITIES AND CYTOTOXICITY OF SOME NEW 1,2,4-TRIAZOLE DERIVATIVES CONTAINING 2-SUBSTITUTED BENZIMIDAZOLE
Date
2023-08-17
Authors
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Publisher
Amrit Campus
Abstract
The development of a potent new drug with high biological activity is a challenge in drug
design and is of strategic importance. Due to the increasing resistance of pathogens on the
existing drugs there is always a need for the development of a potent drug with high
biological activity. The pharmacological effects are seen in compounds with the presence
of different moieties of pharmaceutical importance such as triazole, Schiff’s base,
benzimidazole as described in the chemical literature. By applying different synthetic
reactions in a convergent pattern, two new compounds have been prepared with three
pharmacophores viz. triazole, benzimidazole and Schiff base incorporated in a single
compound. The structure of the prepared compounds was confirmed by different
spectroscopic techniques like, FT-IR, UV-VIS,
1H-NMR, and 13C-NMR. The progress of
the reaction was monitored by TLC and determination of melting point. All compounds
exhibited moderate antibacterial activity against Staphylococcus aureus (ATCC 6538P) and
Staphylococcus epidermidis (ATCC 1228). Antioxidant activity was carried out by DPPH
radical scavenging test and among the tested five compounds, the IC50 value of 4-amino-2-
(2-hydroxyphenyl)-1H-1,2,4-triazole-5-thione was found to be 32.364 μgmL-1 which is
closer to the ascorbic acid sample that was found to be 28.546 μgmL-1. All tested compounds were toxic against brine shrimp where 5-((1H-benzo[d]imidazol-2-yl)thio)-4-((4-
chlorobenzylidene) amino)-4H-1,2,4-triazol-3-yl) (2-hydroxyphenyl) methanone was
comparatively more toxic (LC50= 26.827 μgmL-1)
Description
Keywords
Triazole, Schiff’s base, Benzimidazole, Biological activity.