Synthesis, Characterisation and Evaluation of Benzimidazoles Containing Biphenylcarbonylpiperazine at C-2 Position for Antipsychotic Activity

Indian Journal of Pharmaceutical Education and Research

  • Rani S. Kankate1Department of Pharmaceutical Chemistry, MET’s Institute of Pharmacy, Bhujbal Knowledge City, Nashik, Maharashtra, INDIA.
  • Zenish J. Jain1Department of Pharmaceutical Chemistry, MET’s Institute of Pharmacy, Bhujbal Knowledge City, Nashik, Maharashtra, INDIA.
  • Shantanu S. Ghodke1Department of Pharmaceutical Chemistry, MET’s Institute of Pharmacy, Bhujbal Knowledge City, Nashik, Maharashtra, INDIA.
  • Paraag S. Gide2Department of Pharmaceutics, HSNCB's Dr. L. H. Hiranandani College of Pharmacy, CHM Campus, Ulhasnagar, Maharashtra, INDIA.
  • Kaustubh S. Patil1Department of Pharmaceutical Chemistry, MET’s Institute of Pharmacy, Bhujbal Knowledge City, Nashik, Maharashtra, INDIA.
  • Smita P. Kakad1Department of Pharmaceutical Chemistry, MET’s Institute of Pharmacy, Bhujbal Knowledge City, Nashik, Maharashtra, INDIA.
  • Sunita N. Surse1Department of Pharmaceutical Chemistry, MET’s Institute of Pharmacy, Bhujbal Knowledge City, Nashik, Maharashtra, INDIA.

Volume 59 Issue 3s Pages s1090-s1100

DOI: 10.5530/ijper.20256783

Abstract

Aim/Background: The development of antipsychotic medications with a better clinical profile and fewer neurological side effects is still necessary. Since it is widely known that a dopamine D2 opposing component is required for antipsychotic efficaciousness, the majority of modern pharmacological treatments under investigation are based on the development of medications that partially or entirely interfere with dopamine D2-like receptors. Compounds that selectively block a subtype of dopamine D2-like receptors or those that bind to particular serotonin receptor subtypes in addition to dopamine D2 receptors may be able to produce an atypical antipsychotic profile. Materials and Methods: In present research work, 14 derivatives of 2-[N4-(4'-phenylbenzoyl)piperazin-1-yl-alkyl]-1H-alkyl/aryl/5-alkyl/chloro/5,6-dichloro-benzo(d) imidazoles were synthesized successfully and confirmed with the spectral characterization by IR, 1H-NMR, 13C-NMR and Mass. Results: All 14 synthesized derivatives were evaluated for antipsychotic potential. Catalepsy model was used because it is also a type of negative symptom of schizophrenia. Thus, all the compounds successfully reversed to varying extent, the haloperidol induced cataleptic effect in female mice. Conclusion: It was found from the activity profile of the 14 compounds that the synthesized compounds effectively decreased the catalepsy caused by Haloperidol. With respect to this, compounds BPB02, BPB03, BPB05, BPB08, BPB09, BPB12 were found to be more effective.

Keywords

  • Antipsychotic
  • Benzimidazole
  • Biphenyl
  • Piperazine
  • Schizophrenia
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