Journal of Pharmaceutical
Technology, Research and
Management
Vol. 1
May 2013
pp. 69–79
©2013 by Chitkara
University. All Rights
Reserved.
Synthesis and Pharmacological Evaluation of
Some Novel Imidazole Derivatives for
Their Potential Anti-Hypertensive
Activity
Anju Goyal
Chitkara College of Pharmacy, Chitkara University,
Punjab, INDIA
Email: anju.goyal@chitkara.edu.in
Jitender Singh
Lord Shiva College of Pharmacy, Sirsa,
Haryana, INDIA
Dharam Pal Pathak
Delhi Institute of Pharamceutical Sciences And Research,
New Delhi, INDIA
Abstract
Benzimidazole, which is a heterocyclic nucleus, plays an important role in various
medicines. A number of therapeutic agents such as H1 antihistaminic agent clemizole,
a potent opioid analgesic etonitazene, nonnucleoside antiviral compound enviroxime,
for promotion of excretion of uric acid irtemazole, non sedating antihistaminic agent
astemizole, anti ulcer drugs omeprazole and pentoprazole, antihelmintic thiabendazole,
antinematodal nocodazole etc. are based on benzimidazole heterocyclic nucleus. The
synthesis of various benzimidazole derivatives by the reaction of ortho phenylene
diamine I with various organic acids to yield 2-substituted benzimidazole derivatives
II which on further treatment with nitric acid and sulphuric acid yielded 5-nitro-2-
substituted benzimdazoles III. Coupling of this compound with halogenated beta
picoline V yielded the title compounds. The structures of synthesized compounds
were elucidated mainly by spectral evidence. All the compounds were screened for
their anti-hypertensive activity. The compounds exhibited moderate to significant
activities.
Key Words: Synthesis, benzimidazoles, anti-inflammatory activity, anti-convulasant
activity
1 INTRODUCTION
C
ardiovascular diseases are a cause of significant number of mortalities
among deaths reported due to various diseases. One of the most
common ailments of cardiovascular system is hypertension. A patient
as per guidelines is said to be hypertensive when blood pressure measures of
140/90mmHg (systolic/diastolic pressure). Hypertension also involves slow