Design, Optimization, Synthesis and AntiTB Screening of Benzimidazole Derivatives

(E-pub Ahead of Print)

Author(s): Theivendren Panneerselvam, Govindaraj Saravanan*, Veerachamy Alagarsamy, Selvaraj Kunjiappan, Pavadai Parasuraman.

Journal Name: Anti-Infective Agents

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Abstract:

Introduction: A biologically active benzimidazole synthesis was carried out at laboratory scale in order to reduce environmental pollution as well as to identify effective synthetic route.

Methods: In this connection optimization was performed by Central Composite Rotatable Design (CCRD) to develop experimental data through Response Surface Methodology (RSM). The optimization of title analogue was performed by RSM which led us to the identification of high quality of synthetic yield. The effects of four independent parameters [1-5 mol of oxobutanoic acid (X1), 1-5 mol of thionyl chloride (X2), 1-5 mol of imidazol-2-yl-4-oxobutanoyl chloride (X3), and 1-5 mol of 4-nitro aniline (X4)] were taken into optimize the synthetic yields of title scaffold.

Results and Conclusion: A result on randomly generated benchmark and real values such as percentage yield, λmax and retention time (RT) of title compound are found to be highly significant. The present model connected into maximizing percentage yield of title scaffold with developed optimal set. The high significant benzimidazole was screened for their MTB activity against MTB H37Ra strain by MABA screening.

Keywords: CCRD, RSM, Benzimidazole, % of yield, ?max, RT

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(E-pub Ahead of Print)
DOI: 10.2174/2211352517666190301144054