Benzimidazole: A Milestone in the Field of Medicinal Chemistry

2020 ◽  
Vol 20 (7) ◽  
pp. 532-565 ◽  
Author(s):  
Mahesh S. Vasava ◽  
Manoj N. Bhoi ◽  
Sanjay K. Rathwa ◽  
Divya J. Jethava ◽  
Prachi T. Acharya ◽  
...  
Keyword(s):  
Medicinal Chemistry ◽  
Benzimidazole Derivatives ◽  
Drug Candidate ◽  
Pharmacological Activities ◽  
Drug Candidates ◽  
The Future ◽  
Anti Inflammatory ◽  
Anti Fungal ◽  
Derivatives Of ◽  
Anti Hiv

In the last 2-3 decades, the broad research in the application of benzimidazole derivatives made it important for mankind. Many scientists have worked on benzimidazole derivatives and they found that this compound has a diverse role in the field of medicinal chemistry. Few benzimidazole derivatives are currently in the market as a drug candidate against various diseases. Moreover, the benzimidazole derivatives exhibit pharmacological activities such as anti-tuberculosis, anti-malarial, antihistamine, antimicrobial, antiviral, antidiabetic, anticancer, anti-fungal, anti-inflammatory, analgesic, anti-HIV, etc. In this review, we have summarized various derivatives of benzimidazole which have been prepared by many researchers to understand the chemistry as well as diverse pharmacological activities. These findings may lead the scientists who are working in the field of medicinal chemistry to the development of benzimidazole based drug candidates in the future.

Quinoline containing benzimidazole and their biological activities

2021 ◽  
Vol 3 (3) ◽  
pp. 3-6
Author(s):  
Bhushan D Varpe ◽  
Gajanan Gavande ◽  
Amol Lavate ◽  
Vaibhav Dhakane ◽  
Dnyaneshwar Jagtap ◽  
...  
Keyword(s):  
Biological Activities ◽  
Present Review ◽  
Benzimidazole Derivatives ◽  
Quinoline Derivatives ◽  
Pharmacological Activities ◽  
The Future ◽  
Bacterial Treatment ◽  
Derivatives Of

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.

Chemistry and Pharmacology of Acetanilide Derivatives: A Mini Review

2018 ◽  
Vol 16 (1) ◽  
pp. 6-15
Author(s):  
Rajib K. Singh ◽  
Arvind Kumar ◽  
Arun K. Mishra
Keyword(s):  
Present Article ◽  
Aromatic Compound ◽  
Medical Practice ◽  
Phenyl Ring ◽  
Pharmacological Activities ◽  
Anti Cancer ◽  
The Future ◽  
Anti Inflammatory ◽  
Derivatives Of

Acetanilide or N-phenylacetamide is an aromatic compound having phenyl ring attached to an acetamido group (–NHCOCH3). In 1886, acetanilide was introduced as an analgesic and antipyretic drug into medical practice by A. Cahn and P. Hepp. Since then, many acetanilide derivatives have been found to have antimicrobial, analgesic, anti-inflammatory, antipyretic, antioxidant, anticonvulsant, anti- cancer, antihyperglycaemic and antimalarial activities. Acetanilide also plays an important role in the synthesis of a number of chemicals as intermediates and precursors. The chief objective of the present article is to highlight the chemistry and pharmacological aspects of various derivatives of acetanilide and their pharmacological activities to assist the future discovery of more efficacious derivatives with less toxicity.

A Comprehensive Review on the Therapeutic Versatility of Imidazo [2,1-b]thiazoles

2020 ◽  
Vol 27 (40) ◽  
pp. 6864-6887 ◽  
Author(s):  
Mohd Adil Shareef ◽  
Irfan Khan ◽  
Bathini Nagendra Babu ◽  
Ahmed Kamal
Keyword(s):  
Literature Review ◽  
Medicinal Chemistry ◽  
Therapeutic Agents ◽  
Present Review ◽  
Thiazole Derivatives ◽  
Pharmacological Activities ◽  
Comprehensive Review ◽  
Derivatives Of

Background:: Imidazo[2,1-b]thiazole, a well-known fused five-membered hetrocycle is one of the most promising and versatile moieties in the area of medicinal chemistry. Derivatives of imidazo[2,1-b]thiazole have been investigated for the development of new derivatives that exhibit diverse pharmacological activities. This fused heterocycle is also a part of a number of therapeutic agents. Objective:: To review the extensive pharmacological activities of imidazo[2,1-b]thiazole derivatives and the new molecules developed between 2000-2018 and their usefulness. Method:: Thorough literature review of all relevant papers and patents was conducted. Conclusion:: The present review, covering a number of aspects, is expected to provide useful insights in the design of imidazo[2,1-b]thiazole-based compounds and would inspire the medicinal chemists for a comprehensive and target-oriented information to achieve a major breakthrough in the development of clinically viable candidates.

Pharmacologic activities of 5, 6-Diaryl/heteroaryl-3-substituted-1, 2, 4-triazines as a privileged scaffold in drug development

2021 ◽  
Vol 21 ◽  
Author(s):  
Zahra Zakeri Khatir ◽  
Hamid Irannejad
Keyword(s):  
Biological Data ◽  
Pharmacological Activities ◽  
Drug Candidates ◽  
Structure Activity ◽  
Wide Range ◽  
Privileged Structure ◽  
Triazine Derivatives ◽  
Privileged Scaffold ◽  
Substituted 1 ◽  
Anti Hiv

: 1, 2, 4-Triazine derivatives have received much attention due to their multifunctional nature, especially in diverse pharmacological properties as well as a key fragment in many drug candidates. Introduction of a vicinal 5, 6-diaryl/heteroaryl moiety on the 1, 2, 4-triazine ring has attracted plentiful attention in the field of medicinal chemistry. 5, 6-Diaryl/heteroaryl-3-substituted-1, 2, 4-triazine is as a prominent scaffold in many drug candidates which has shown a wide range of pharmacological activities such as anti-diabetic, antifungal, anti-inflammatory, anticancer, anti-HIV, neuroprotective, anticonvulsant, anti- Alzheimer, anti-Parkinson and antioxidant. In this review, we have discussed synthesis, various pharmacological activities of 5, 6-diaryl/heteroaryl-3-substituted-1, 2, 4-triazines, their structure-activity relationship (SAR), pharmacophoric elements and their mechanism of action reported in the published articles during 2000-2019. Evaluation of compounds by PAINS filtering tool was accomplished and showed that this versatile structure could be considered as a privileged structure. Compilation of the biological data confirmed that the position 3 of the 1,2,4-triazine is a key location to determine the affinity and selectivity of the 5,6-diaryl/heteroaryl-3-substituted-1, 2, 4-triazines towards different biologic targets. Specific geometrical and thermodynamic characters of this motif have prompted it as a frequent hitter.

scholarly journals Synthesis and Biological Activities of Some Pyrimidine Derivatives: A Review

2020 ◽  
Vol 36 (6) ◽  
pp. 1001-1015
Author(s):  
Nadia Ali Ahmed Elkanzi
Keyword(s):  
Nitrogen Atom ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Heterocyclic Ring ◽  
Ring System ◽  
Pyrimidine Derivatives ◽  
Pharmacological Activities ◽  
Cardiovascular Agents ◽  
Anti Hiv ◽  
Biological And Pharmacological Activities

Nitrogen containing synthetically and biologically important heterocyclic ring system namely pyrimidine possess both biological and pharmacological activities, and defend as aromatic six heterocyclic with 1and 3 nitrogen atom in ring. Preparation of pyrimidine via different methods offer its importance in fields of medicinal chemistry and Chemistry. Pyrimidines and their derivatives act as anti-inflammatory, anti-malaria, anti-tumor, cardiovascular agents, anti-neoplastic, anti-tubercular, anti- HIV, diuretic ,anti-viral, anti-microbial, ,analgesic .This review give light up on biological and pharmacological activities of pyrimidine nucleus.

In silico designing of some Benzimidazole derivatives for Anti-fungal activity

2021 ◽  
pp. 4983-4986
Author(s):  
Amrita Muralikrishnan ◽  
Radhika R Nair ◽  
Jifitha Banu ◽  
Leena K Pappachen
Keyword(s):  
Fungal Infections ◽  
Living Organism ◽  
Whole Body ◽  
Benzimidazole Derivatives ◽  
Bioinformatics Tool ◽  
Pharmacological Activities ◽  
Discovery Studio ◽  
Drug Designing ◽  
Target Molecules ◽  
Anti Fungal

Fungus is a kind of living organism and yeast mould and mushrooms are types of fungi. The fungal infections are caused by the fungus. A fungus that invades the tissue can cause a disease that confined to the skin, spread into tissue, bone and organs or affect the whole body. Benzimidazole is a class of heterocyclic aromatic organic compound which posses pharmacological activities including antifungal, antitumor, antiparasitic, analgesic etc. Insilico methods can be used to identify target molecules using bioinformatics tool. The aim of our study was to conduct the insilico drug designing of some benzimidazole derivatives having antifungal activities. In our study the insilico drug design was performed using Biovia discovery studio.

scholarly journals PYRIMIDINES AS POTENT CYTOTOXIC AND ANTI-INFLAMMATORY AGENTS

2017 ◽  
Vol 10 (6) ◽  
pp. 237 ◽  
Author(s):  
Ishwar Bhat K ◽  
Abhishek Kumar
Keyword(s):  
Acetic Acid ◽  
Cytotoxic Activity ◽  
Glacial Acetic Acid ◽  
Antimalarial Activity ◽  
Biological Activities ◽  
Cytotoxic Agents ◽  
Pyrimidine Derivatives ◽  
Pharmacological Activities ◽  
Anti Inflammatory ◽  
Derivatives Of

Objective: Many derivatives of pyrimidine are known for the broad-spectrum biological activities such as antimicrobial, antitumor, antibacterial, antitubercular, anti-inflammatory, and cytotoxic activity. Chalcones with an enone group show potent pharmacological activities such as antiinflammatory, antibacterial, antifungal, and antimalarial activity. A series of pyrimidines from chalcones have been synthesized and screened for anti-inflammatory and cytotoxic activity studies.Methods: Chalcones [1-(4-nitrophenyl)-3-substituted-phenylprop-2-en-1-one] were synthesized from various substituted aldehydes with 4-nitroacetophenone and cyclized with urea and glacial acetic acid to give pyrimidine derivatives [4-(4-nitrophenyl)-6-substituted-phenylpyrimidin-2-ol].Results: Anti-inflammatory and cytotoxic activity studies revealed that some of the synthesized compounds have shown significant activity.Conclusion: The observed results proved that pyrimidines are found to be interesting lead molecules for the synthesis of anti-inflammatory and cytotoxic agents

Phytochemical and pharmacological aspects of Nothapodytes nimmoniana. An overview

2013 ◽  
Vol 59 (1) ◽  
pp. 53-66 ◽  
Author(s):  
Nazeerullah Khan ◽  
Ennus Tajuddin Tamboli ◽  
V.K. Sharma ◽  
Sunil Kumar
Keyword(s):  
Wide Spectrum ◽  
Pharmacological Activities ◽  
Nothapodytes Nimmoniana ◽  
Jammu And Kashmir ◽  
Medicinal Uses ◽  
Anti Cancer ◽  
Anti Oxidant ◽  
Anti Fungal ◽  
Anti Hiv ◽  
Important Medicinal Plant

Summary Nothapodytes nimmoniana (J. Graham) (Icacinaceae), commonly known as Amruta is found in India particularly in Maharashtra, Goa, Kerala, Assam, Jammu and Kashmir as well as Tamilnadu areas. It is an important medicinal plant, the major source of a potent alkaloid, namely camptothecin, of a wide spectrum of pharmacological activities like anti-cancer, anti-HIV, antimalarial, antibacterial, anti-oxidant, anti-inflammatory, anti-fungal and also applied in the treatment of anaemia. Camptothecin is still not synthesized, therefore, its production entirely depends on natural sources. N. nimmoniana is one such plant which yields contain camptothecin in significantly high amount. The plant is gaining international recognition due to its diversified medicinal uses. It is subjected to excessive harvest. It has been categorized as a vulnerable and endangered plant. The present review encompasses the phytochemical, analytical, pharmacological, biotechnological, and other specific aspects of N. nimmoniana.

scholarly journals A Review on Natural Plants for Phytochemical Constituents and Pharmacological Activities

2021 ◽  
Vol 11 (2) ◽  
pp. 232-236
Author(s):  
K Muni Raja Lakshmi ◽  
M. Kiran ◽  
K. Sai Prasanna
Keyword(s):  
Medicinal Plants ◽  
Antioxidant Properties ◽  
Volatile Oil ◽  
Calotropis Procera ◽  
Pharmacological Activities ◽  
Antioxidant Agents ◽  
Phytochemical Constituents ◽  
Natural Plants ◽  
Anti Inflammatory ◽  
Anti Fungal

The present review aims for the study of phytoconstituents and pharmacological activities of some natural plants. The traditional medicinal plants have been found to acquire therapeutic activities significantly antimicrobial, anti-inflammatory antibacterial, anti-fungal, antioxidant properties etc. The plant-derived constituents are majorly for the aliments of used skin disease diabetes, bronchitis, asthma, arthritis, dry cough, ulcer and fever. The antimicrobial activity of the following plants like Justicia adathoda, Lantana Camara, Acacia leucophloea, Holoptelea integrifolia, Calotropis Procera, chlorophytum tuberosum, Bombax ceiba, Bacopa monnieri, Wedelia trilobata, Jatropha gossypifolia were obtained from the extraction of either  leaves, stem or flowers by using ethanol, methanol, aqueous, petroleum ether, chloroform. The phytochemical constituents of the extract have been shown the presence of alkaloids, glycosides, cardiac glucosides tannins, proteins, carbohydrates, saponin, quinines, triterpenes, steroids, polyphenolic, volatile oil, phenols, starch sugar, amino acid, resin and organic acids. This study evidenced the possible use of the mentioned plants as a source of natural medicines which are used as an antimicrobial, anti-inflammatory, anti-bacterial, anti-fungal, antioxidant agents. Keywords:  Medicinal plants, Antimicrobial, Anti-inflammatory, Antioxidants.

Dual Acting Isatin-heterocyclic Hybrids: Recent Highlights as Promising Pharmacological Agents

2018 ◽  
Vol 16 (2) ◽  
pp. 220-236 ◽  
Author(s):  
Srinubabu Maddela ◽  
Githa Elizabeth Mathew ◽  
Della Grace Thomas Parambi ◽  
Fakhria Aljoufi ◽  
Bijo Mathew
Keyword(s):  
Single Molecule ◽  
Heterocyclic Compounds ◽  
Structural Modification ◽  
Drug Efficacy ◽  
Biologically Active ◽  
Synergistic Activity ◽  
Pharmacological Activities ◽  
Pharmacological Agents ◽  
Drug Candidates ◽  
Derivatives Of

Background: For the development of suitable lead molecules to different diseases is a highly challenging task for medicinal chemists. Nowadays, hybrid pharmacophore concept has developed as a useful structural modification tool in the drug design of new drug candidates for different diseases. Hybrid pharmacophore approach consists of combination of two or more pharmacophoric moieties from different biologically active compounds with complementary functions or different mechanisms of action into a single molecule. This often results in synergistic activity or enhanced drug efficacy. Objective: To develop the suitable leads for different diseases there will be a lot of scope to study the substitution of heterocyclic moieties on the different positions of isatin ring. The broad and potent activities of the isatin and their derivatives have been established them as pharmacologically significant scaffolds. In this review, an attempt has been made with specifically emphasizing the hybridization of Isatin with different derivatives of heterocyclic compounds on the different positions of the isatin ring (aryl ring, isatin nitrogen and C2/C3 carbonyl moieties). Conclusion: This review highlighted the recent advances of dual acting isatin-heterocyclic hybrids presenting various pharmacological activities viz., anticancer, antitubercular, anti-inflammatory and antimicrobial.

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