Journal :   Asian Journal of Research in Chemistry

Volume No. :   5

Issue No. :  7

Year :  2012

Pages :   918-921

ISSN Print :  0974-4169

ISSN Online :  0974-4150


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Synthesis and Biological Evaluation for Antihistaminic activity of N1-Alkyl–2(N4- Alkyl/Aryl piperazinyl methyl) Benzimidazole derivatives



Address:   Gadhave R.V.1 ,Vijaya Vichare2 and Joshi S.V.2
1MAEER’s Maharashtra Institute of Pharmacy, Paud Road, Kothrud, Pune-411038
2PES’s Modern College of Pharmacy (For Ladies), Borhadewadi, Dehu-Alandi Road, Moshi , Pune-412105
*Corresponding Author
DOI No:

ABSTRACT:
Benzimidazole derivatives are known for their wide spread pharmacological activities and benzimidazole derived antihistaminics are more widely used group of therapeutic agents in allergic diseases because of their low toxicities. As a part of ongoing effort finding novel Antihistaminics, several N1, 2-substituted benzimidazole derivatives were synthesized and screened for their antihistaminic potential. O-fluoro nitrobenzene condensed with alkyl amines and these condensation products were hydrogenated to get N1-alkyl-o-phenylene diamines. Condensation of substituted o-phenylene diamines with chloro acetic acid gives cyclised intermediates and these intermediates when condensed with N1-alkyl/aryl piperazines gives variously substituted piperazinyl benzimidazole derivatives. The synthesized N1-Alkyl–2(N4- Alkyl/Aryl piperazinyl methyl) Benzimidazole derivatives were screened for antihistaminic activity using Chlorpheniramine maleate (CPM) as reference standard. Interestingly, few synthesized compounds exhibited slight to moderate antihistaminic activity. Based on results obtained we can conclude that these molecules hold potential for further modification as selective Antihistaminics for H1 receptor.
KEYWORDS:
Benzimidazole, Piperazine, Antihistaminic activity, Chlorpheniramine maleate, Goat tracheal chain.
Cite:
Gadhave R.V. ,Vijaya Vichare, Joshi S.V.. Synthesis and Biological Evaluation for Antihistaminic activity of N1-Alkyl–2(N4- Alkyl/Aryl piperazinyl methyl) Benzimidazole derivatives. Asian J. Research Chem. 5(7): July, 2012; Page 918-921.
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