Synthetic and Biological Attributes of Pyrimidine Derivatives: A Recent update

2021 ◽  
Vol 18 ◽  
Author(s):  
Meenu Devi ◽  
Shivangi Jaiswal ◽  
Sonika Jain ◽  
Navjeet Kaur ◽  
Jaya Dwivedi
Keyword(s):  
Biological Activities ◽  
Structural Diversity ◽  
Therapeutic Agents ◽  
Pyrimidine Derivatives ◽  
Diverse Range ◽  
Biological Attributes ◽  
Synthetic Approaches ◽  
High Degree ◽  
Therapeutic Activities ◽  
Anti Hiv

: 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.

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.

A Comprehensive Appraisal of Chalcones and Their Heterocyclic Analogs as Antimicrobial Agents

2020 ◽  
Vol 24 (23) ◽  
pp. 2755-2781
Author(s):  
Riddhi Salotra ◽  
Divya Utreja
Keyword(s):  
Antimicrobial Agents ◽  
Biological Activities ◽  
Structural Diversity ◽  
Natural Sources ◽  
Anti Cancer ◽  
Heterocyclic Derivatives ◽  
Synthetic Methodologies ◽  
Microbial Potential ◽  
High Degree ◽  
Therapeutic Profile

Owing to the growing demand for compelling antimicrobial agents, chalcones and their heterocyclic derivatives have engrossed prodigious attention of medicinal chemists as an effective clinical template for the synthesis of such agents on account of their structural diversity and molecular flexibility. Chalcones are considered as a fortunate scaffold in the field of both synthetic as well as natural product chemistry. They are reflected as a remarkable section of logically occurring pharmacophores that possess a comprehensive scale of biological activities, such as anti-cancer, anti-malarial, anti-viral and anti-inflammatory, rendering them with a high degree of assortment and noble therapeutic profile. They act as a crucial intermediate for the synthesis of novel heterocyclic skeletons holding biodynamic behavior. This review emphasizes on different aspects of chalcones including their natural sources, recent synthetic methodologies and evaluation of their anti-microbial potential. It is expected as a persuasive compilation on chalcones that may benefit the experts to design potent and less toxic chalcone referents as medicinal agents.

scholarly journals Chiral Flavonoids as Antitumor Agents

2021 ◽  
Vol 14 (12) ◽  
pp. 1267
Author(s):  
Cláudia Pinto ◽  
Honorina Cidade ◽  
Madalena Pinto ◽  
Maria Elizabeth Tiritan
Keyword(s):  
Antitumor Activity ◽  
Antitumor Agents ◽  
Biological Activities ◽  
Structural Diversity ◽  
Building Blocks ◽  
Inhibitory Effect ◽  
Chiral Molecules ◽  
Growth Inhibitory ◽  
Synthetic Approaches

Flavonoids are a group of natural products with a great structural diversity, widely distributed in plant kingdom. They play an important role in plant growth, development and defense against aggressors. Flavonoids show a huge variety of biological activities such as antioxidant, anti-inflammatory, anti-mutagenic, antimicrobial and antitumor, being able to modulate a large diversity of cellular enzymatic activities. Among natural flavonoids, some classes comprise chiral molecules including flavanones, flavan-3-ols, isoflavanones, and rotenoids, which have one or more stereogenic centers. Interestingly, in some cases, individual compounds of enantiomeric pairs have shown different antitumor activity. In nature, these compounds are mainly biosynthesized as pure enantiomers. Nevertheless, they are often isolated as racemates, being necessary to carry out their chiral separation to perform enantioselectivity studies. Synthetic chiral flavonoids with promising antitumor activity have also been obtained using diverse synthetic approaches. In fact, several new chiral bioactive flavonoids have been synthesized by enantioselective synthesis. Particularly, flavopiridol was the first cyclin-dependent kinase (CDK) inhibitor which entered clinical trials. The chiral pool approaches using amino acid as chiral building blocks have also been reported to achieve small libraries of chrysin derivatives with more potent in vitro growth inhibitory effect than chrysin, reinforcing the importance of the introduction of chiral moieties to improve antitumor activity. In this work, a literature review of natural and synthetic chiral flavonoids with antitumor activity is reported for the first time.

scholarly journals Arylnaphthalene lactones: structures and pharmacological potentials

2021 ◽  
Author(s):  
Soyoung Park ◽  
Seungsu Kim ◽  
Dongyun Shin
Keyword(s):  
Drug Discovery ◽  
Medicinal Plants ◽  
Biological Activities ◽  
Structural Diversity ◽  
Structural Features ◽  
Type I ◽  
Type Ii ◽  
Pharmacological Activities ◽  
Naturally Occurring ◽  
Anti Hiv

AbstractNatural arylnaphthalene lactones are representative lignans that are found in various dietary and medicinal plants. Their unique structural features and significant pharmacological activity have attracted considerable attention from both synthetic and medicinal chemists. Owing to their unique structural features such as relative rigid tetracyclic skeleton, structural diversity of more than five substituents, and no chiral center, arylnaphthalene lactones are recognized as a valuable scaffold for drug discovery, in addition to their significant pharmacological activities. This review covers the structures and isolation of all naturally occurring arylnaphthalene lactone congeners reported. Based on the aryl substituents, they were categorized as Type I and Type II and further classified according to the oxidation state of the ring and glycosylation level. Special attention has been paid to natural arylnaphthalene lactones owing to their broad spectrum of biological activities such as cytotoxic, antiplatelet, antiviral, anti-HIV, antifungal, neuroprotective, and anti-inflammatory properties. All the products were reorganized based on their biological activities, and selected data are presented.

Recent Advancements in Biological Activities of Oxadiazole and their Derivatives: A Review

2020 ◽  
Vol 17 (6) ◽  
pp. 409-429
Author(s):  
Arun Kumar Mishra ◽  
Arvind Kumar ◽  
Jagdish K. Sahu
Keyword(s):  
In Silico ◽  
Biological Activities ◽  
Therapeutic Agents ◽  
Isomeric Form ◽  
Molecular Formula ◽  
Synthetic Analogues ◽  
Oxadiazole Derivatives ◽  
In Silico Models ◽  
Anti Hiv Agents ◽  
Anti Hiv

Oxadiazole moiety, which is one of the heterocyclic aromatic groups of the azole family; with the molecular formula C2H2N2O, exists in four isomeric form; out of which, 1,2,4-oxadiazole; 1,2,5-oxadiazole and 1,3,4-oxadiazole are common isomers. The stable isomeric forms of oxadiazoles are observed in a variety of pharmaceutical important potent drugs including raltegravir, butalamine, fasiplon, oxolamine and pleconaril. An attempt has been made to emphasize the chemistry and pharmacology associated with oxadiazole and its derivatives. A number of oxadiazole derivatives are very popular and common in use as potential therapeutic agents. However, a number of researchers are working and have worked to find out more synthetic analogues for anticancer and antifungal, anti-HIV agents using biological and in-silico models.

scholarly journals Recent Advances on Quinazoline Derivatives: A Potential Bioactive Scaffold in Medicinal Chemistry

2021 ◽  
Vol 5 (4) ◽  
pp. 73
Author(s):  
Ram Karan ◽  
Pooja Agarwal ◽  
Mukty Sinha ◽  
Neelima Mahato
Keyword(s):  
Heterocyclic Compounds ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Therapeutic Agents ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Diverse Range ◽  
Important Group ◽  
Quinazoline Derivatives

This paper intended to explore and discover recent therapeutic agents in the area of medicinal chemistry for the treatment of various diseases. Heterocyclic compounds represent an important group of biologically active compounds. In the last few years, heterocyclic compounds having quinazoline moiety have drawn immense attention owing to their significant biological activities. A diverse range of molecules having quinazoline moiety are reported to show a broad range of medicinal activities like antifungal, antiviral, antidiabetic, anticancer, anti-inflammatory, antibacterial, antioxidant and other activities. This study accelerates the designing process to generate a greater number of biologically active candidates.

Metal-, and Organocatalyst-Free One-Pot Assembly of Chiral Aza-Tricyclic Molecules: Creating Six Contiguous Stereocenters from 2-D-Structures and an Amino Acid

2020 ◽  
Author(s):  
Dung Do
Keyword(s):  
Amino Acid ◽  
Chemical Space ◽  
Structural Diversity ◽  
Therapeutic Agents ◽  
Chiral Molecules ◽  
One Pot ◽  
Complex Molecules ◽  
Chiral Catalyst ◽  
Chiral Complex ◽  
Free Process

<p>Chiral molecules with their defined 3-D structures are of paramount importance for the study of chemical biology and drug discovery. Having rich structural diversity and unique stereoisomerism, chiral molecules offer a large chemical space that can be explored for the design of new therapeutic agents.<sup>1</sup> Practically, chiral architectures are usually prepared from organometallic and organocatalytic processes where a transition metal or an organocatalyst is tailor-made for desired reactions. As a result, developing a method that enables rapid assembly of chiral complex molecules under metal- and organocatalyst-free condition represents a daunting challenge. Here we developed a straightforward route to create a chiral 3-D structure from 2-D structures and an amino acid without any chiral catalyst. The center of this research is the design of a <a>special chiral spiroimidazolidinone cyclohexadienone intermediate</a>, a merger of a chiral reactive substrate with multiple nucleophillic/electrophillic sites and a transient organocatalyst. <a>This unique substrate-catalyst (“subcatalyst”) dual role of the intermediate enhances </a><a>the coordinational proximity of the chiral substrate and catalyst</a> in the key Aza-Michael/Michael cascade resulting in a substantial steric discrimination and an excellent overall diastereoselectivity. Whereas the “subcatalyst” (hidden catalyst) is not present in the reaction’s initial components, which renders a chiral catalyst-free process, it is strategically produced to promote sequential self-catalyzed reactions. The success of this methodology will pave the way for many efficient preparations of chiral complex molecules and aid for the quest to create next generation of therapeutic agents.</p>

Bio-organometallic Peptide Conjugates: Recent Advances in Their Synthesis and Prospects for Biomedical Application

2020 ◽  
Vol 24 (21) ◽  
pp. 2508-2523
Author(s):  
Johana Gómez ◽  
Diego Sierra ◽  
Constanza Cárdenas ◽  
Fanny Guzmán
Keyword(s):  
Amino Acids ◽  
Biomedical Application ◽  
Structural Diversity ◽  
Biological Properties ◽  
Therapeutic Agents ◽  
Organometallic Complexes ◽  
Chemical Behavior ◽  
Metal Compounds ◽  
Bioorganometallic Chemistry ◽  
Pharmacological Control

One area of organometallic chemistry that has attracted great interest in recent years is the syntheses, characterization and study of organometallic complexes conjugated to biomolecules with different steric and electronic properties as potential therapeutic agents against cancer and malaria, as antibiotics and as radiopharmaceuticals. This minireview focuses on the unique structural diversity that has recently been discovered in α- amino acids and the reactions of metallocene complexes with peptides having different chemical behavior and potential medical applications. Replacing α-amino acids with metallocene fragments is an effective way of selectively influencing the physicochemical, structural, electrochemical and biological properties of the peptides. Consequently, research in the field of bioorganometallic chemistry offers the opportunity to develop bioactive metal compounds as an innovative and promising approach in the search for pharmacological control of different diseases.

Synthesis and Biological Activity of Quaternary Quinolinium Salts: A Review

2020 ◽  
Vol 23 (21) ◽  
pp. 2271-2294 ◽  
Author(s):  
Divya Utreja ◽  
Shivali Sharma ◽  
Akhil Goyal ◽  
Komalpreet Kaur ◽  
Sonia Kaushal
Keyword(s):  
Tyrosine Kinases ◽  
Biological Activities ◽  
Polymeric Materials ◽  
Tubulin Polymerization ◽  
Quinoline Derivatives ◽  
Heterocyclic Chemistry ◽  
Biological Profile ◽  
Drug Candidates ◽  
Anti Hiv ◽  
Quinolinium Salts

Heterocyclic chemistry is the only branch of chemistry that has applications in varied areas such as dyes, photosensitizers, coordination compounds, polymeric materials, biological, and many other fields. Quinoline and its derivatives have always engrossed both synthetic chemists and biologists because of their diverse chemical and pharmacological properties as these ring systems can be easily found in various natural products, especially in alkaloids. Among alkaloids, quinoline derivatives i.e. quinolinium salts have attracted much attention nowadays owing to their diverse biological profile such as antimicrobial, antitumor, antifungal, hypotensive, anti-HIV, analgesics and anti-inflammatory, etc. Quinoline and its analogs have recently been examined for their modes of function in the inhibition of tyrosine kinases, proteasome, tubulin polymerization, topoisomerase, and DNA repair. These observations have been guiding scientists for the expansion of new quinoline derivatives with improved and varied biological activities. Quinolinium salts have immense possibilities and scope to investigate these compounds as potential drug candidates. Therefore, we shall present a concise compilation of this work to aid in present knowledge and to help researchers explore an interesting quinoline class having medicinal potential.

Structure and Activity of Pentacyclic Triterpenes Codrugs. A Review

2021 ◽  
Vol 21 ◽  
Author(s):  
Justyna Żwawiak ◽  
Anna Pawełczyk ◽  
Dorota Olender ◽  
Lucjusz Zaprutko
Keyword(s):  
Biological Activities ◽  
Anticancer Activities ◽  
Drug Molecule ◽  
Pentacyclic Triterpene ◽  
Formation Pathway ◽  
Chemical Systems ◽  
Drug Molecules ◽  
Wide Range ◽  
Anti Hiv ◽  
Structure And Activity

: Triterpenes are a wide and important group of compounds that have several promising pharmacological properties, such as hepatoprotective, anti-inflammatory, anti-HIV, antioxidant, or anticancer activities. Such potent substances can be successfully incorporated in more complex chemical systems e.g. codrugs or pro-drugs that have better pharmacological profile. The codrug is connected with a drug formation pathway to chemically cohere at least two drug molecules to improve positive therapeutic efficiency or decrease side effects. The codrug can be cleaved in the organism to generate effective compounds previously used as substrates. This article presents an overview of codrugs that consist of pentacyclic triterpene moiety that is chosen as a basic codrug moiety due to their wide range of vital activities and another drug molecule fragment. It was found that triterpenoid codrugs are characterized by a wide range of biological activities. However, most of them have anticancer potency.

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