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ISSN (Print): 2211-3525
ISSN (Online): 2211-3533

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Research Article

Design, Optimization, Synthesis and AntiTB Screening of Benzimidazole Derivatives

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

Volume 18, Issue 1, 2020

Page: [24 - 42] Pages: 19

DOI: 10.2174/2211352517666190301144054

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 of 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 is connected to maximize the percentage yield of title scaffold with the developed optimal set. The highly significant benzimidazole was screened for its MTB activity against MTB H37Ra strain by MABA screening.

Keywords: CCRD, RSM, Benzimidazole, % yield, λmax, RT, oxobutonic acid.

Graphical Abstract

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