Biologically Active Benzimidazole Derivatives

2015 ◽  
Vol 12 (2) ◽  
pp. 178-195 ◽  
Author(s):  
Subramaniyan Arulmurugan ◽  
Helen P. Kavitha ◽  
Samiyappan Sathishkumar ◽  
Rajaram Arulmozhi
2020 ◽  
Vol 18 (1) ◽  
pp. 24-42
Author(s):  
Theivendren Panneerselvam ◽  
Selvaraj Kunjiappan ◽  
Veerachamy Alagarsamy ◽  
Govindaraj Saravanan ◽  
Pavadai Parasuraman

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 on 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 connected into maximizing percentage yield of title scaffold with developed optimal set. The high significant benzimidazole was screened for their MTB activity against MTB H37Ra strain by MABA screening.


2019 ◽  
Vol 58 (5) ◽  
pp. 75-80
Author(s):  
Anastasia A. Yadrova ◽  
◽  
Roman V. Shafigulin ◽  
Andzhela V. Bulanova ◽  
◽  
...  

The effect of water-acetonitrile and water-methanol eluents composition on newly synthesized benzimidazole derivatives sorption by supercrosslinked polystyrene (SCP) using high performance liquid chromatography was studied. It is shown that the nature of the organic modifier affects on the considered biologically active compounds sorption. The angular coefficients of the Snyder-Sochevinsky equation, characterizing the number of organic modifier molecules, displaced by one molecule of sorbate, for benzimidazole derivatives, are calculated. The angular coefficients was calculated from the dependence, characterized by a high coefficient of determination. The article demonstrated that the Snyder-Sochevinsky model could be used for describing of all studied compounds sorption in the system “SCP – water-methanol eluent” and for describing of volume sorbates with hydrophobic substituting groups sorption in the system “SCP – water-acetonitrile solution”. The value of the slope of the Snyder-Sochevinsky equation of benzimidazoles sorption from water-methanol solutions is higher than that from water-acetonitrile solution; this fact indicates a lower elution power of the water-methanol eluent in compare to water-acetonitrile eluent. The Snyder-Sochevinsky model is not fulfilled in the concentration range from 75% to 85% of acetonitrile for small volume benzimidazole molecules containing hydrophilic amino and hydroxymethylene groups in the «SCP – water-acetonitrile eluent» system. The composition of the mobile phase influence of benzimidazoles sorption was studied. It is demonstraited the relationships between volume fraction of the organic modifier increase and decreases of benzimidazoles sorption.


2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Shobhit Srivastava ◽  
S. N. Pandeya ◽  
Meena K. Yadav ◽  
B. K. Singh

A series of novel 2-phenylhydrazinomethyl and 2-(2-hydroxyphenyl)-benzimidazole derivatives substituted at the N1-position of benzimidazole nucleus were synthesized as well as screened for analgesic activity. Some of these compounds showed promising analgesic activity when compared with the standard drug diclofenac sodium. The incorporation of a phenylhydrazinomethyl nucleus at 2-position of benzimidazole compound gave a biologically active pharmacophore.


2021 ◽  
Author(s):  
Sahil Kohli ◽  
Garima Rathee ◽  
Sunita Hooda ◽  
Ramesh Chandra

This work is generally focused on synthesis of an efficient, reusable and novel heterogeneous Al2O3/CuI/PANI nanocatalyst which have been well synthesized by a simple self-assembly approach where aniline is oxidized...


2021 ◽  
Vol 21 (1) ◽  
pp. 273-284
Author(s):  
NASEEM AHMAD ◽  
MOHAMMAD IRFAN AZAD ◽  
ABDUL RAHMAN KHAN ◽  
IQBAL AZAD

Heterocyclic derivatives are unavoidable in many fields of natural disciplines. These derivatives play numerous significant roles in research, medication, and nature. Nitrogenous heterocyclic derivatives extremely are the main target of concern in synthetic chemistry to ensue active natural products with pharmaceuticals and agrochemicals interest. Benzimidazole skeleton is another example of some active heterocyclic moiety that significantly contributes in the numerous bioactive of essential compounds. Benzimidazole skeleton is studied as a prominent moiety of biologically active compounds with various activities including antimicrobial, antiprotozoal, anticancer, antiviral, acetylcholinesterase, antihistaminic, anti-inflammatory, antimalarial, analgesic, anti-HIV and antitubercular. Therefore, in this review we summarize the various antiviral activities of several benzimidazole derivatives and outline the correlation among the structures of different benzimidazoles scaffold with their therapeutic significance.


2020 ◽  
Vol 13 (3) ◽  
pp. 159-171
Author(s):  
K. Pakeeraiah ◽  
Sujit Kumar Mohanty ◽  
K. Eswar ◽  
K. Raju

Azo compounds are a very unique class of chemical compounds, drawing considerations in scientific research. Azo compounds are studied as class of organic colorants which have at least a conjugated chromophore azo (-N=N-) group in fusion with one or more aromatic or heterocyclic ring system. Benzimidazole derivatives are privileged intermediates for the development of molecules of pharmaceutical or biological interest. Benzimidazole derivatives have gathered wide applications in diverse therapeutic areas such as antiulcer, anticancer agents, and anthelmintic species to name just a few. Although many azo derivatives of benzimidazole nucleus has been reported in literature but only few of them have been evaluated for their biological potencies. This review focuses primarily on those derivatives which are evaluated as anticancer, antibacterial, antifungal, antitubercular, and other medicinal agents. This review may be helpful for the investigators on the basis of substitution pattern on the nucleus with an objective to assist medicinal chemists for developing an SAR on azo benzimidazoles or similar compounds.


Author(s):  
Ashish Patel ◽  
Drashti Shah ◽  
Naiya Patel ◽  
Khushbu Patel ◽  
Nidhi Soni ◽  
...  

Abstract: The benzimidazole and its derivatives are privileged heterocyclic motif and important building block for the development of the biologically active compound. However, several research reports are produced in a short period of time due to the rapid production of new drugs having a benzimidazole nucleus. In order to understand the current status of the benzimidazole nucleus in medicinal chemistry science, it is therefore important to combine the latest knowledge with earlier information. Hence, synthetic organic chemists concentrated on inventing an effective green methodology for synthesizing benzimidazole derivatives. In addition to this, non-degradable chemical compounds cause the ecosystem to become fragile, damage or irritation as contaminants and pose a danger to the environment. However, conventional methods of synthesis need longer heating time, complicated and tedious apparatus set up which result in high cost and pollution in contrast to greener methods which are inexpensive. In the present review, therefore, we have attempted to shed light on various synthetic strategies leading to the synthesis of different benzimidazole derivatives through the direct condensation reaction between o-phenylenediamine and aromatic aldehydes using green chemistry approaches such as mechanochemistry, ultrasound irradiation, microwave irradiation, environmentally benign solvents/catalysts, reactant immobilized on a solid support and blue light irradiation.


2014 ◽  
Vol 11 (999) ◽  
pp. 1-1
Author(s):  
Arulmurugan S ◽  
Kavitha HP ◽  
Sathishkumar S ◽  
Arulmozhi R

Sign in / Sign up

Export Citation Format

Share Document