scholarly journals POTENT BIOLOGICAL AGENT BENZIMIDAZOLE–A REVIEW

Author(s):  
Pullagura M. Krishna Prasad ◽  
Avdhut Kanvinde S. ◽  
Raja S.

<p>Benzimidazole nucleus is one of the most important heterocycles exhibiting remarkable pharmacological activities. Numerous method for the synthesis of benzimidazole and also their diverse reactions offer enormous scope in the field of medicinal chemistry. Various reported biological activities (analgesic, anti-inflammatory, anthelmintic, anticancer, anthelmintic, antioxidant, antitubercular, and antiviral activity) of bezimidazole are collected and summarized here. Large numbers of drugs are available to treat various diseases, but they are associated with some drawbacks like resistance, toxicities and other adverse effects. To combat with these problems there is need to discover and synthesize newer chemical entities with better efficacy and novel mechanism of action. The benzimidazole ring is an important pharmacophore in modern drug discovery. The synthesis of novel benzimidazole derivatives remains a main focus of medicinal research. There is still scope for more research work to be done in this field to find a novel agent. The versatility of new generation benzimidazole would represent a fruitful pharmacophore for further development of better medicinal agents. Therefore this substrate has a tremendous scope for the discovery of new, better, safe and more potent biological agents.</p>

2020 ◽  
Vol 16 (8) ◽  
pp. 1147-1156
Author(s):  
Ruchi Singh ◽  
Syed M. Hasan ◽  
Amit Verma ◽  
Sanjay K. Panda

Background: A plant is a reservoir of potentially useful active chemical entities which act as drugs as well as intermediates for the discovery of newer molecules and provide newer leads for modern drug synthesis. The demand for new compounds in the field of medicine and biotechnology is centuries old and with a rise in chronic diseases and resistance to existing drugs in the field of anti-infective agents, the chemicals obtained from plant sources have been an area of attraction. The whole plant has possessed multiple pharmacological activities. This is scientifically established by in-vivo and in-vitro studies. Methods: Various electronic databases such as PubMed, Science Direct, Scopus and Google were searched to collect the data of the present review. All the collected information is categorized into different sections as per the aim of the paper. Results: Fifty-six research and review papers have been studied and were included in this review article. After a detailed study, we provide a significant description of various phytochemicals present in Nyctanthes arbor-tristis Linn., which is responsible for various pharmacological activities. Twenty of studied articles gives a general introduction and ethnobotanical information about the plant, two papers contained microscopic detail of leaf and fruit. Twenty papers contained information about the phytoconstituents present in different parts of Nyctanthes arbor-tristis plant and fourteen articles reported pharmacological activities like antioxidant, anti-inflammatory, antiarthritic, antimicrobial and immunobiotic activity. Conclusion: This review explores the published research work comprising the ethnobotanical description of the subjected plant, distribution, phytochemical profile, and arthritis-related pharmacological activities.


2020 ◽  
Vol 8 ◽  
Author(s):  
Xueyi Wang ◽  
Shangying Ma ◽  
Feifan Lai ◽  
Yiqi Wang ◽  
Chenghua Lou

Eupatorium lindleyanum DC. (EL) has a long history of traditional use in China to cure coughs, chronic bronchitis, lobar pneumonia, and hypertension. Because of this extensive use of EL in traditional medicine, this present review gives a systematic overview of the conventional applications, phytochemistry, and pharmacological effects of the herb. Literature was systematically searched using the scientific databases ScienceDirect, SciFinder, CNKI, Wiley, Baidu Scholar, SpringerLink, PubMed, Web of Science, and other professional websites. Information was also gathered from books on traditional Chinese herbal medicine, the Chinese Pharmacopoeia and Chinese Materia Medica. To date, many preparations of EL have been widely used clinically to treat various diseases of the respiratory system. More than 100 compounds have been isolated from the herb, including triterpenes, sesquiterpenes, sesquiterpene lactones, flavonoids, acyclic diterpenoids, sterols, and so on. Among them, terpenoids are considered to be the most important bioactive substances in EL. The pharmacological functions of EL, including anti-asthmatic, anti-tussive, anti-inflammatory, anti-hyperlipidemic, anti-hypertensive, anti-virus, and anti-tumor activities, have been widely investigated. However, most of the studies are preclinical research. Further studies are required to examine the underlying mechanisms of action. Traditionally, EL is used for treating many diseases, especially respiratory diseases. Unfortunately, up to now, modern studies have not yet well elucidated the conventional usage of EL. Most importantly, its biological activities and the corresponding constituents are still unclear. Moreover, studies on the pharmacokinetics and toxicity of EL are few, so data on the clinical safety of EL are lacking. Taken together, research work on EL is quite preliminary. More in-depth studies of phytochemistry, pharmacological activities, pharmacokinetics, and toxicity of the herb are needed. This review aims to provide valuable information on EL to guide future investigations and applications.


2020 ◽  
Vol 17 (8) ◽  
pp. 661-670
Author(s):  
Mohamed Ahmed Elian Sophy ◽  
Mohamed Ahmed Mahmoud Abdel Reheim

Aim and Objective: According to the literature survey, pyrazole is a unique template that is associated with several biological activities. This article highlighted the research work of many researchers reported in the literature for synthesis and different pharmacological activities of the pyrazole nucleus. In the present work, pyrazol- 3-one 1 was reacted with cyanoacetic acid hydrazide and elemental sulfur to afford the corresponding thieno[3,2-c]pyrazol-6-carbohydrazide 3 derivatives. The latter compound reacted with some electrophilic reagents such as DMF-DMA, triethylorthoformate, arylidenemalononitriles and chalcones under neat conditions to give substituted oxadiazole and pyrazole, respectively. The treatment of compound 3 with active methylene reagents such as acetylacetone, diethylmalonate, ethyl acetoacetate and ethyl cyanoacetate under suitable conditions afforded pyrazole derivatives 10, 11, 13, and 15, respectively. Novel pyrazolothienopyrimidine 27 and 30 were prepared from precursor 26 with carbon disulfide and triethylorthoformate, respectively. The chemical structures of the newly synthesized compounds were established by elemental and spectral analyses including IR, and 1HNMR in addition to 13C-NMR and mass spectra. Materials and Methods: A novel substituted pyrazole, pyrimidine and pyrazolothienopyrimidine were obtained via Gewald synthesis of thiophene and fused thiophene and Mannich reactions of 5-amino-3-phenyl-1Hthieno[ 3,2-c]pyrazole-6-carbohydrazide. Results and Discussion: A series of some newly azoles and azines were prepared via reaction of thieno[3,2- c]pyrazol-6-carbohydrazide derivative 3 as starting material with some electrophilic and nucleophilic reagents. The structures of target compounds were established by elemental analyses and spectral data. Conclusion: Pyrazole is a unique template that is associated with several biological activities. This article highlighted the research work of many researchers reported in the literature for synthesis and different pharmacological activities of the pyrazole nucleus. In the current investigation, we have developed new and efficient methods for the synthesis of thieno[3,2-c]pyrazol-6-carbohydrazide derivatives. In addition, we have explored the preparative potential of these substances as intermediates for the synthesis of substituted pyrazoles and fused pyrazoles 10-30, respectively.


2021 ◽  
Vol 3 (3) ◽  
pp. 3-6
Author(s):  
Bhushan D Varpe ◽  
Gajanan Gavande ◽  
Amol Lavate ◽  
Vaibhav Dhakane ◽  
Dnyaneshwar Jagtap ◽  
...  

Quinoline and derivatives of Benzimidazole are widely studied for their different activities. One of the essential classes of anti-malarial and anti-bacterial treatment is the quinoline derivatives. Quinoline and Benzimidazole are flexible lead molecules used to model the future molecules of drugs. The present review outlines the potential pharmacological activities of quinoline and Benzimidazole derivatives.


2018 ◽  
Vol 9 (3) ◽  
pp. 136-143
Author(s):  
Rahul Kumar Gupta ◽  
Meena Deogade

Martynia annua Linn (Martyniaceae) is an important herbaceous annual medicinal herb found as a wild plant throughout India. In spite of the fact that the majority of its parts are utilized as a part of folklore and it is known as kakanasika in Ayurved, fruits, seeds, roots and Leaves are the most vital parts which are utilized therapeutically. The present article gives an account of updated complete information on its phytochemical and pharmacological properties. The review shows that large numbers of phytochemical constituents have been isolated from the Martynia annua Linn plant which possesses actions like Antioxidant, Anthelmintic, Analgesic and Antipyretic, Antibacterial, Anti-convulsant,  Antinociceptive  and, Antifertility, Central Nervous System (CNS) depressant, Wound Healing, Antidiabetic, Gastroprotective, Antifungal, Cytotoxic  Activity and various other important medicinal properties. In folk medicine, Decoction of whole plant is used in pneumonia and cold fever. Leaves are eaten in times of scarcity and also given in epilepsy and its juice is gargled for sore throat. The fruits are used for the treatment of asthma; the seeds are also applied locally for itching and eczema. The Roots are boiled with milk and taken as a tonic and roots made into a poultice and applied in snake bite. For the last few decades or so, extensive research work has been done to prove its biological activities and pharmacology of its extracts. The aim of this review article was to summarize the information associated to Pharmacognostical, ethnobotanical, traditional, Phytochemical and pharmacological activity of the Martynia annua Linn plant.  


2019 ◽  
Vol 16 (2) ◽  
pp. 111-126 ◽  
Author(s):  
Mayura Kale ◽  
Vijayalaxmi Chavan

The development of benzoxazole containing drugs and research compounds has been discussed in the present review along with its varied pharmacological activities such as antimicrobial, antiinflammatory, anticancer, antiviral, antiasthmatic, antitubercular, anticonvulsant, lipid modulating, anticoagulants, antidiabetic and anthelmintic activities. The present review is a compilation of the biological activities determined in the research work conducted on benzoxazole-based compounds fused and linked with various other heterocycles.


2021 ◽  
Author(s):  
David Cate ◽  
Helen Hsieh ◽  
Veronika Glukhova ◽  
Joshua D Bishop ◽  
H Gleda Hermansky ◽  
...  

<p></p><p>The global COVID-19 pandemic has created an urgent demand for large numbers of inexpensive, accurate, rapid, point-of-care diagnostic tests. Analyte-based assays are suitably inexpensive and can be rapidly mass-produced, but for sufficiently accurate performance they require highly optimized antibodies and assay conditions. We used an automated liquid handling system, customized to handle arrays of lateral flow immunoassay (LFA) tests in a high-throughput screen, to identify anti-nucleocapsid antibodies that will perform optimally in an LFA. We tested 1021 anti-nucleocapsid antibody pairs as LFA capture and detection reagents with the goal of highlighting pairs that have the greatest affinity for unique epitopes of the nucleocapsid protein of SARS-CoV-2 within the LFA format. In contrast to traditional antibody screening methods (e.g., ELISA, bio-layer interferometry), the method described here integrates real-time reaction kinetics with transport in, and immobilization directly onto, nitrocellulose. We have identified several candidate antibody pairs that are suitable for further development of an LFA for SARS-CoV-2.</p><p></p>


2020 ◽  
Vol 27 (35) ◽  
pp. 5970-6014 ◽  
Author(s):  
Md. Jawaid Akhtar ◽  
Mohammad Shahar Yar ◽  
Vinod Kumar Sharma ◽  
Ahsan Ahmed Khan ◽  
Zulphikar Ali ◽  
...  

This review presents the detailed account of factors leading to cancer and design strategy for the synthesis of benzimidazole derivatives as anticancer agents. The recent survey for cancer treatment in Cancer facts and figures 2017 American Chemical Society has shown progressive development in fighting cancer. Researchers all over the world in both developed and developing countries are in a continuous effort to tackle this serious concern. Benzimidazole and its derivatives showed a broad range of biological activities due to their resemblance with naturally occurring nitrogenous base i.e. purine. The review discussed benzimidazole derivatives showing anticancer properties through a different mechanism viz. intercalation, alkylating agents, topoisomerases, DHFR enzymes, and tubulin inhibitors. Benzimidazole derivatives act through a different mechanism and the substituents reported from the earlier and recent research articles are prerequisites for the synthesis of targeted based benzimidazole derivatives as anticancer agents. The review focuses on an easy comparison of the substituent essential for potency and selectivity through SAR presented in figures. This will further provide a better outlook or fulfills the challenges faced in the development of novel benzimidazole derivatives as anticancer.


2020 ◽  
Vol 24 (4) ◽  
pp. 439-464 ◽  
Author(s):  
Rizk E. Khidre ◽  
Tahah A. Ameen ◽  
Mounir A. I. Salem

This review summarizes the synthesis, reactions, and biological activities of tetrazolo[1,5-a]quinoline derivatives. These derivatives were synthesized by several methods such as i) from the reaction of 2-chloroquinoline with sodium azide ii) from diazotization 2-hydrazinylquinoline derivatives, and iii) from intramolecular cyclocondensation of 2-azidoarylidenes. Also, the chemical reactions and pharmacological activities of some tetrazoloquinolines such as tetrazolo[1,5-a]quinoline-4-carbaldehyde, 5-chlorotetrazolo[ 1,5-a]quinoline, 4-(chloromethyl)tetrazolo[1,5-a]quinoline, tetrazolo[1,5- a]quinoline-4-carboxylic acid, and 5-azidotetrazolo[1,5-a]quinoline were discussed.


2019 ◽  
Vol 19 (8) ◽  
pp. 624-646 ◽  
Author(s):  
Yogita Bansal ◽  
Manjinder Kaur ◽  
Gulshan Bansal

Structural resemblance of benzimidazole nucleus with purine nucleus in nucleotides makes benzimidazole derivatives attractive ligands to interact with biopolymers of a living system. The most prominent benzimidazole compound in nature is N-ribosyldimethylbenzimidazole, which serves as an axial ligand for cobalt in vitamin B12. This structural similarity prompted medicinal chemists across the globe to synthesize a variety of benzimidazole derivatives and to screen those for various biological activities, such as anticancer, hormone antagonist, antiviral, anti-HIV, anthelmintic, antiprotozoal, antimicrobial, antihypertensive, anti-inflammatory, analgesic, anxiolytic, antiallergic, coagulant, anticoagulant, antioxidant and antidiabetic activities. Hence, benzimidazole nucleus is considered as a privileged structure in drug discovery, and it is exploited by many research groups to develop numerous compounds that are purported to be antimicrobial. Despite a large volume of research in this area, no novel benzimidazole derived compound has emerged as clinically effective antimicrobial drug. In the present review, we have compiled various reports on benzimidazole derived antimicrobials, classified as monosubstituted, disubstituted, trisubstituted and tetrasubstituted benzimidazoles, bisbenzimidazoles, fused-benzimidazoles, and benzimidazole derivative-metal complexes. The purpose is to collate these research reports, and to generate a generalised outlay of benzimidazole derived molecules that can assist the medicinal chemists in selecting appropriate combination of substituents around the nucleus for designing potent antimicrobials.


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