scholarly journals Recent Advances in Chalcones: Synthesis, Transformation and Pharmacological Activities

Author(s):  
Oluwaseyi Bukky Ovonramwen ◽  
Bodunde Joseph Owolabi ◽  
Amowie Philip Oviawe

Chalcones are useful intermediates in the synthesis of heterocyclic compound and the unique reagents in organic synthesis. The usual approach to obtain chalcones is through Claisen-Schmidt condensation. Several novel heterocyclic chalcone analogs have emerged. Chalcones are multifunctional molecules that possess promising pharmacological activities. Chalcones are known for anti-cancer, antioxidant, anti-inflammatory, anti-microbial, anti-tubercular, antileishmanial, antimalarial, anthelmintic, osteogenic activities. This review article focuses on recent applications of Claisen-Schmidt condensation reaction employed in the synthesis of chalcone, its transformation to heterocyclic compounds and pharmacological activities.

Author(s):  
Monica Dinodia

Abstract: Nitrogen based heterocycles display an impressive repertoire of biological activities, including antioxidant, antimicrobial, anti-tuberculosis, analgesic, anti-inflammatory, anti-viral, anti-HIV, anti-cancer, anti-helminthic, and other pharmacological activities. Numerous novel nitrogen-based heterocycles have been synthesized, which showed various physiological properties, and their application in medicinal chemistry is ever-growing. The present review will provide an in-depth view of N-heterocyclic compounds that showed biological activities in the last 5 years (2017-2021). This review article will be helpful for the structural design of effective and sustainable N-heterocyclic drugs against diseases with minimal side effects.


Author(s):  
Shukla PK ◽  
Singh MP ◽  
Patel R

Indole and its derivatives have engaged a unique place in the chemistry of nitrogen heterocyclic compounds. The recognition of the plant growthhormone, heteroauxin, the significant amino acids, tryptamine & tryptophan and anti-inflammatory drug, indomethacine are the imperativederivatives of indole which have added stimulus to this review work. Isatin (1H-indole-2,3-dione), an indole derivative of plant origin. Althoughit is a naturally occurring compound, but was synthesized by Erdmann and Laurent in 1840 before it was found in nature. Isatin is a versatileprecursor for many biologically active molecules and its diversified nature makes it a versatile substrate for further modifications. It is concernedin many pharmacological activities like anti-malarial, antiviral, anti-allergic, antimicrobial etc; isatin and its derivatives have been also found todemonstrate promising outcomes against various cancer cell lines. This review provides a brief overview on the recent advances and futureperspectives on chemistry and biological aspects of isatin and its derivatives reported in the recent past.


2020 ◽  
Vol 16 (4) ◽  
pp. 454-486 ◽  
Author(s):  
Smita Verma ◽  
Vishnuvardh Ravichandiran ◽  
Nihar Ranjan ◽  
Swaran J.S. Flora

Nitrogen-containing heterocycles are one of the most common structural motifs in approximately 80% of the marketed drugs. Of these, benzimidazoles analogues are known to elicit a wide spectrum of pharmaceutical activities such as anticancer, antibacterial, antiparasitic, antiviral, antifungal as well as chemosensor effect. Based on the benzimidazole core fused heterocyclic compounds, crescent-shaped bisbenzimidazoles were developed which provided an early breakthrough in the sequence-specific DNA recognition. Over the years, a number of functional variations in the bisbenzimidazole core have led to the emergence of their unique properties and established them as versatile ligands against several classes of pathogens. The present review provides an overview of diverse pharmacological activities of the bisbenzimidazole analogues in the past decade with a brief account of its development through the years.


2021 ◽  
Vol 22 ◽  
Author(s):  
M İhsan Han ◽  
Ş. Güniz Küçükgüzel

: Spreading rapidly in recent years, cancer has become the cause of one of the highest mortality rates after cardiovascular diseases. The reason for cancer development is still not clearly understood despite enormous research activities in this area. Scientists are now working on the biology of cancer, especially on the root cause of cancer development. The aim is to treat the cancer disease, and thus cure the patients. The continuing efforts on the development of novel molecules as potential anti-cancer agents are essential for this purpose. The main aim of this review was to present a survey on the medicinal chemistry of thioethers and to provide practical data on their cytotoxicities against various cancer cell lines. The research articles published between 2001-2020 were consulted in the preparation of this review article, though patent literature was not included here. The thioether-containing heterocyclic compounds may emerge as a new class of potent and effective anti-cancer agents soon.


2019 ◽  
Vol 9 (1-s) ◽  
pp. 505-509 ◽  
Author(s):  
Shaheen Sulthana ◽  
P. Pandian

In recent years heterocyclic compounds analogues and derivatives have attracted wide attention due to their useful biological and pharmacological properties. Indole, Benzothiazole and its analogs are versatile substrates, which can be used for the synthesis of numerous heterocyclic compounds. Indole, Benzothiazole and its derivatives are used in organic synthesis and they are used in evaluating new product that possesses different biological activities. Hence, their extensive structural modification has result in different analogues of Indole and Benzothiazole derivatives depicting wide range of biological and pharmacological activities such as antiviral, anticonvulsant, anti-inflammatory, analgesic, antimicrobial and anticancer. This review article literature survey summarizes the synthesis and pharmacological activities of Indole, Benzothiazole and its derivatives. Keywords: Indole, Benzothiazole, antiviral, anticonvulsant, anti-inflammatory, analgesic, antimicrobial and anticancer


Molecules ◽  
2021 ◽  
Vol 26 (24) ◽  
pp. 7523
Author(s):  
Helen A. Goulart ◽  
Daniela R. Araujo ◽  
Filipe Penteado ◽  
Raquel G. Jacob ◽  
Gelson Perin ◽  
...  

Oxone is a commercially available oxidant, composed of a mixture of three inorganic species, being the potassium peroxymonosulfate (KHSO5) the reactive one. Over the past few decades, this cheap and environmentally friendly oxidant has become becoming a powerful tool in organic synthesis, being extensively employed to mediate the construction of a plethora of important compounds. This review summarizes the recent advances in the Oxone-mediated synthesis of N-, O- and chalcogen-containing heterocyclic compounds, through a wide diversity of reactions, starting from several kinds of substrate, highlighting the main synthetic differences, advantages, the scope and limitations.


Author(s):  
Amala Babu ◽  
Sneha Antony ◽  
Femy Maria KM ◽  
Dr.Vinod B

Pyrazole represents a versatile class among heterocyclic compounds due to its impact in biological and pharmacological field irrespective of its scarcity in nature. From the structural point of view, pyrazoles are rather interesting and chemically it is known as 1,2-Diazoles.Also, it is a five membered heterocyclic compound containing 2 Nitrogen atoms. As per different studies, Pyrazoles and its derivatives own a wide range of biological activities like Antibacterial, Analgesic, Antioxidant etc. The main intention of this review is to run an overview of diverse pharmacological activities of pyrazole moiety especially antimicrobial, anti-inflammatory, antioxidant, analgesic, Hypoglycemic, anticancer and enzyme inhibitory effects.


Author(s):  
Alphonsus D’souza ◽  
K. D. Venuprasad ◽  
Prashant Nayak ◽  
Lisha K. Poonacha

Despite the fact that triazole was first synthesised over a century ago, it continues to unique the interest of chemists, biologists, technologists, and other experts.  Triazoles  have been shown to have antiviral, anti-inflammatory, anti-fertility, anti-tubercular, antimicrobial, anti-cancer, and anti-corrosion properties in recent years. The goal of this review is to describe the structures, synthesis, reactions, and spectral properties of triazoles in order to highlight their potential applications in a variety of bioactive phenomena and analytical applications.


2020 ◽  
Vol 20 (18) ◽  
pp. 2228-2245
Author(s):  
Jyoti Singh ◽  
Amruta Suryan ◽  
Sandeep Kumar ◽  
Shweta Sharma

Phthalazinones are important nitrogen-rich heterocyclic compounds which have been a topic of considerable medicinal interest because of their diversified pharmacological activities. This versatile scaffold forms a common structural feature for many bioactive compounds, which leads to the design and development of novel anticancer drugs with fruitful results. The current review article discusses the progressive development of novel phthalazinone analogues that are targets for various receptors such as PARP, EGFR, VEGFR-2, Aurora kinase, Proteasome, Hedgehog pathway, DNA topoisomerase and P-glycoprotein. It describes mechanistic insights into the anticancer properties of phthalazinone derivatives and also highlights various simple and economical techniques for the synthesis of phthalazinones.


Author(s):  
Zhiwei Chen ◽  
Piaopiao Zeng ◽  
Shuo Zhang ◽  
Jie Sun

: Coumarin is a privileged scaffold which contains the unique 2H-chromen-2-one motif, and its derivatives are widely distributed in nature, especially in plants. In recent years, due to their diverse pharmacological activities and remarkable photochemical properties, much attention has been attracted by scientists, which has also prompted the research on the synthesis approaches and the availability of substrates for these compounds. This article is mainly about a brief description of the methods for the synthesis of various coumarin derivatives via two- or multi-component reactions involving 3-amino or 4-aminocoumarin reported during 2015-2021. This review may help to expand the development of various analogues with coumarin as the basic unit.


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