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

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.

2019 ◽  
Vol 16 (11) ◽  
pp. 898-905
Author(s):  
Harun Patel ◽  
Rahul Pawara ◽  
Sanjay Surana

Quinazoline is the six-membered heterocyclic ring system reported for its versatile biological activities. This characteristic feature of quinazoline makes it a good template for a lead generation library. Ring opening is one of the major concerns in the synthesis of quinazolin-4(3H)-one that results in diamide formation. Here, alternative fusion strategy is reported, which is a time-saving and costeffective method to overcome the ring opening problem associated with the synthesis of benzo[ d][1,3]oxazin-4-one and quinazolin-4(3H)-one.


2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Amita Verma ◽  
Sunil Joshi ◽  
Deepika Singh

Imidazoles have occupied a unique position in heterocyclic chemistry, and its derivatives have attracted considerable interests in recent years for their versatile properties in chemistry and pharmacology. Imidazole is nitrogen-containing heterocyclic ring which possesses biological and pharmaceutical importance. Thus, imidazole compounds have been an interesting source for researchers for more than a century. The imidazole ring is a constituent of several important natural products, including purine, histamine, histidine, and nucleic acid. Being a polar and ionisable aromatic compound, it improves pharmacokinetic characteristics of lead molecules and thus is used as a remedy to optimize solubility and bioavailability parameters of proposed poorly soluble lead molecules. There are several methods used for the synthesis of imidazole-containing compounds, and also their various structure reactions offer enormous scope in the field of medicinal chemistry. The imidazole derivatives possess extensive spectrum of biological activities such as antibacterial, anticancer, antitubercular, antifungal, analgesic, and anti-HIV activities. This paper aims to review the biological activities of imidazole during the past years.


2021 ◽  
Vol 17 ◽  
Author(s):  
Nidhi Kala ◽  
Kalpana Praveen Rahate

: Triazole is the main five-membered Nitrogen-containing basic heterocyclic ring system reported for their biological activities and compounds with multiple pharmacophores, which fetch together acquaintance of a target with sympathetic types of the molecule that might interact with the target. In addition, healthy, adaptable, and scalable chemistry must be employed to achieve the task. This characteristic feature of triazole would make a good template for a lead cohort library. The current review article focuses on recent advancements in triazole moiety as an anti-cancer agent with their mechanism pathways of synthesized analogues.


2021 ◽  
Vol 18 ◽  
Author(s):  
Meenu Devi ◽  
Shivangi Jaiswal ◽  
Sonika Jain ◽  
Navjeet Kaur ◽  
Jaya Dwivedi

: Nitrogen-containing heterocycles attract the attention of chemists due to their multifarious activities. Amongst all, pyrimidine plays a central role and exhibits a broad spectrum of biological activities. Literature is replete with the various aspects of synthetic development in pyrimidine chemistry for a wide array of applications. It aroused our interest to compile various novel and efficient synthetic approaches towards the synthesis of pyrimidine and its derivatives. Pyrimidine derivatives are broadly useful as therapeutic agents, owing to their high degree of structural diversity. They have been recorded to possess a diverse range of therapeutic activities, viz. anticancer, anti-inflammatory, anti-HIV etc.


Author(s):  
Shivani Mithula ◽  
Adinarayana Nandikolla ◽  
Sankaranarayanan Murugesan ◽  
Venkata GCS Kondapalli

Among all nitrogen-containing heterocycles, the 1,8-naphthyridine scaffold has recently gained an immense amount of curiosity from numerous researchers across fields of medicinal chemistry and drug discovery. This new attention can be ascribed to its versatility of synthesis, its reactiveness and the variety of biological activities it has exhibited. Over the past half-decade, numerous diverse biological evaluations have been conducted on 1,8-naphthyridine and its derivatives in a quest to unravel novel pharmacological facets to this scaffold. Its potency to treat neurodegenerative and immunomodulatory disorders, along with its anti-HIV, antidepressant and antioxidant properties, has enticed researchers to look beyond its broad-spectrum activities, providing further scope for exploration. This review is a consolidated update of previous works on 1,8-naphthyridines and their analogs, focusing on the past 5 years.


INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (4) ◽  
pp. 7-22
Author(s):  
Mayur Porwal ◽  
◽  
Arvind Kumar ◽  
Kamal K. Maheshwari ◽  
Najam A. Khan ◽  
...  

In conventional methods of medication, Marsdenia tenacissima (family: Apocynaceae) is used in the treatment of scurvy, urinary diseases, arthritis, heart disease, skin disease, pruritus, vomiting and intermittent fever. Estimation of biological activities confirmed that M. tenacissima plant shows antipyretic, antioxidant, anticancer and anti-HIV activities. This assessment presents the phytochemical constituents, traditional importance and pharmacological activities accounted for the plant in recent literature and it will be supportive to explore incisive information about M. tenacissima for the researchers.


Author(s):  
Ishwar Bhat K ◽  
Abhishek Kumar

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


2019 ◽  
Vol 15 ◽  
pp. 388-400
Author(s):  
Pedro N Batalha ◽  
Luana da S M Forezi ◽  
Maria Clara R Freitas ◽  
Nathalia M de C Tolentino ◽  
Ednilsom Orestes ◽  
...  

4-Oxoquinolines are a class of organic substances of great importance in medicinal chemistry, due to their biological and synthetic versatility. N-1-Alkylated-4-oxoquinoline derivatives have been associated with different pharmacological activities such as antibacterial and antiviral. The presence of a carboxamide unit connected to carbon C-3 of the 4-oxoquinoline core has been associated with various biological activities. Experimentally, the N-ethylation reaction of N-benzyl-4-oxo-1,4-dihydroquinoline-3-carboxamide occurs at the nitrogen of the oxoquinoline group, in a regiosselective way. In this work, we employed DFT methods to investigate the regiosselective ethylation reaction of N-benzyl-4-oxo-1,4-dihydroquinoline-3-carboxamide, evaluating its acid/base behavior and possible reaction paths.


2020 ◽  
Vol 3 (1) ◽  
pp. 56
Author(s):  
Venelina Popova ◽  
Albena Stoyanova ◽  
Nadezhda Mazova

The main objective of this mini-review was to synthesize recent data about the phytochemical composition, the nutritional properties, and the biological and pharmacological activities of a now cosmopolitan genus, Physalis (Solanaceae), being in the focus of intensive research over the last two decades. Six Physalis species with nutritional and pharmacological promise are considered in particular – P. peruviana L., P. philadelphica Lam., P. ixocarpa Brot. ex Horm., P. angulata L., P. pubescens L., and P. alkekengi L. Summarized contemporary data on the metabolite profile and the biological activities of Physalis species support their century-long use in traditional medicine and human nutrition. The fruit represent a rich source of minerals, vitamins, fibers, carotenoids, proteins, fructose, sucrose esters, pectins, flavonoids, polyphenols, polyunsaturated fatty acids, phytosterols and many other beneficial nutrients. Individual phytochemicals and complex fractions isolated from Physalis plants demonstrate various biological and pharmacological activities, the most promising of which include antimicrobial, antioxidant, anti-diabetic, hepato-renoprotective, anti-cancer, anti-inflammatory, immunomodulatory and others. Most of these activities are associated with the presence of flavonoids, phenylpropanoids, alkaloids, physalins, withanolides, and other bioactive compounds. The accumulated data disclose the potential of Physalis spp. as highly functional foods, as profitable crops for many regions over the world, and as sources of valuable secondary metabolites for phytopharmacy, novel medicine and cosmetics. Information provided by this review is also important for a more intensive promotion of Physalis species in Bulgaria and for future studies on their composition and benefits.


2020 ◽  
Vol 20 (7) ◽  
pp. 532-565 ◽  
Author(s):  
Mahesh S. Vasava ◽  
Manoj N. Bhoi ◽  
Sanjay K. Rathwa ◽  
Divya J. Jethava ◽  
Prachi T. Acharya ◽  
...  

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.


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