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Synthesis, Characterization and Biological Evaluation of Benzimidazole Derivatives as Potential Anxiolytics


Affiliations
1 Vijaya College of Pharmacy, Hyderabad - 501511, India
2 Department of Botany, Osmania University, Hyderabad, India
     

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Considerable attention has been focused on the synthesis of benzimidazoles due to their broad spectrum of biological activities such as antimicrobial, anti diabetic, anti cancer, anti hypertensive, anti anxiolytic and inflammatory activities etc. As a part of our research work, a series of benzimidazole derivatives were synthesized in good to high yields by reaction of o-phenylenediamine and different aromatic aldehydes in the presence of ammonium chloride (NH4Cl), as an efficient catalyst at room temperature. This environmentally safe and practical method offers several advantages, such as high yields, use of an available catalyst, mild reaction conditions and easy work-up process. All synthesized compounds were characterized by detailed spectral analysis by using LC-MS, IR, and NMR spectroscopy. The synthesized benzimidazoles were screened for chronic anti anxiety activity in albino rats by using light and dark box model with standard Buspirone. Behavioral parameters were recorded during the test session of 5 minutes. All benzimidazole derivatives have shown significant anti anxiety activity compared to the standard. However, benzimidazole analog (3e) exhibited highest anxiolytic action.

Keywords

Aromatic Aldehydes, Ammonium Chloride, O-Phenylenediamine, Room Temperature, Light and Dark Box Apparatus, Buspirone.
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  • Synthesis, Characterization and Biological Evaluation of Benzimidazole Derivatives as Potential Anxiolytics

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Authors

Sudheer K. Dokuparthi
Vijaya College of Pharmacy, Hyderabad - 501511, India
J. Baloji Naik
Vijaya College of Pharmacy, Hyderabad - 501511, India
K. Sunil Kumar
Vijaya College of Pharmacy, Hyderabad - 501511, India
A. Saidulu
Department of Botany, Osmania University, Hyderabad, India

Abstract


Considerable attention has been focused on the synthesis of benzimidazoles due to their broad spectrum of biological activities such as antimicrobial, anti diabetic, anti cancer, anti hypertensive, anti anxiolytic and inflammatory activities etc. As a part of our research work, a series of benzimidazole derivatives were synthesized in good to high yields by reaction of o-phenylenediamine and different aromatic aldehydes in the presence of ammonium chloride (NH4Cl), as an efficient catalyst at room temperature. This environmentally safe and practical method offers several advantages, such as high yields, use of an available catalyst, mild reaction conditions and easy work-up process. All synthesized compounds were characterized by detailed spectral analysis by using LC-MS, IR, and NMR spectroscopy. The synthesized benzimidazoles were screened for chronic anti anxiety activity in albino rats by using light and dark box model with standard Buspirone. Behavioral parameters were recorded during the test session of 5 minutes. All benzimidazole derivatives have shown significant anti anxiety activity compared to the standard. However, benzimidazole analog (3e) exhibited highest anxiolytic action.

Keywords


Aromatic Aldehydes, Ammonium Chloride, O-Phenylenediamine, Room Temperature, Light and Dark Box Apparatus, Buspirone.

References