Recent Progress in the Synthesis of Pyrroles

2020 ◽  
Vol 24 (6) ◽  
pp. 622-657
Author(s):  
Duc Dau Xuan

: Pyrrole derivatives are nitrogen-containing heterocyclic compounds and widely distributed in a large number of natural and non-natural compounds. These compounds possess a broad spectrum of biological activities such as anti-infammatory, antiviral, antitumor, antifungal, and antibacterial activities. Besides their biological activity, pyrrole derivatives have also been applied in various areas such as dyes, conducting polymers, organic semiconductors. : Due to such a wide range of applicability, access to this class of compounds has attracted intensive research interest. Various established synthetic methods such as Paal-Knorr, Huisgen, and Hantzsch have been modified and improved. In addition, numerous novel methods for pyrrole synthesis have been discovered. This review will focus on considerable studies on the synthesis of pyrroles, which date back from 2014.

2020 ◽  
Vol 24 (19) ◽  
pp. 2256-2271
Author(s):  
Dau Xuan Duc

: Benzo[b]thiophenes are aromatic heterocyclic compounds containing benzene and thiophene rings. This class of heterocycles is present in a large number of natural and non-natural compounds. Benzo[b]thiophene derivatives have a broad range of applications in medicinal chemistry such as antimicrobial, anticancer, antioxidant, anti-HIV and antiinflammatory activities. The use of benzo[b]thiophene derivatives in other fields has also been reported. Various benzo[b]thiophenes compounds have been employed as organic photoelectric materials, while several benzo[b]thiophenes have been used as organic semiconductors. Benzo[b]thiophenes have also been used as building blocks or intermediates for the synthesis of pharmaceutically important molecules. : Due to such a wide range of applicability, the synthesis of benzo[b]thiophene derivatives has attracted intensive research. Numerous mild and efficient approaches for the synthesis of benzo[b]thiophenes have been developed over the years. Different catalysts and substrates have been applied for benzo[b]thiophene synthesis. This review will focus on the studies in the construction of benzo[b]thiophene skeleton, which date back from 2012.


Author(s):  
Mohammad Asif ◽  
Mohd. Imran

: Oxazine analog is a vital class of heterocyclic compounds and has attracted synthetic interest owing to their wide range of biological activities. Oxazine analogs are valuable in medicinal organic chemistry and exhibited different varieties of biological activities such as antimicrobial, anticancer, antimalarial, antitubercular, sedative, anticonvulsant, analgesic, anti-inflammatory, antipyretic, etc. Oxazine can be derived from benzene by appropriate substitution of carbon atoms of the ring by nitrogen and oxygen atoms. Nowadays, the development of drug resistance is a key problem, and to defeat this problem, it is crucial to synthesize novel compounds. So novel oxazine analogs may play a crucial role to overcome these problems. Oxazine analogs are prepared by reaction of chalcone derivatives with thiourea in the presence of alcohol and sodium hydroxide. The present aims of this review to give an outline of some different synthetic methods and different types of biological activities of oxazine analogs. We hope that this review will be motivating for researchers concerned with oxazine analogs.


Author(s):  
Adnan Cetin

: The heterocyclic compounds are the building blocks for synthesis of the different biological active compounds in the organic chemistry. Heterocyclic compounds have versatile synthetic applicability and biological activity. Pyrazole carboxylic acid derivatives are significant scaffold structures in heterocyclic compounds due to biologic activities such as antimicrobial, anticancer, inflammatory, antidepressant, antifungal anti-tubercular and antiviral etc. The aim of this mini-review is an overview synthesis of pyrazole carboxylic acid derivatives and their biologic applications. The summarized literature survey presents in detail biological activities of pyrazole carboxylic acid derivatives and their various synthetic methods. This mini-review can be guide to many scientists in medicinal chemistry.


2020 ◽  
Vol 24 (10) ◽  
pp. 1055-1096
Author(s):  
Pradip Kumar Maji

Pyrimidine heterocycles are proven to be biologically active heterocycles, found in many biological systems, displaying a broad spectrum of biological activities including anticancer, anxiolytic, antioxidant, antiviral, antifungal, anticonvulsant, antidepressant and antibacterial activities. Recently, various synthetic approaches, synthetic strategy, the variation of substrates and study devoted towards the evaluation of biological activities for the pyrimidine heterocycles have been reported in the literature. This review article describes the synthesis of various biologically interesting pyrimidine heterocyclic ring systems using various nitrogen building blocks.


2020 ◽  
Vol 26 (8) ◽  
pp. 867-904 ◽  
Author(s):  
Maria Fesatidou ◽  
Anthi Petrou ◽  
Geronikaki Athina

Background: Bacterial infections are a growing problem worldwide causing morbidity and mortality mainly in developing countries. Moreover, the increased number of microorganisms, developing multiple resistances to known drugs, due to abuse of antibiotics, is another serious problem. This problem becomes more serious for immunocompromised patients and those who are often disposed to opportunistic fungal infections. Objective: The objective of this manuscript is to give an overview of new findings in the field of antimicrobial agents among five-membered heterocyclic compounds. These heterocyclic compounds especially five-membered attracted the interest of the scientific community not only for their occurrence in nature but also due to their wide range of biological activities. Method: To reach our goal, a literature survey that covers the last decade was performed. Results: As a result, recent data on the biological activity of thiazole, thiazolidinone, benzothiazole and thiadiazole derivatives are mentioned. Conclusion: It should be mentioned that despite the progress in the development of new antimicrobial agents, there is still room for new findings. Thus, research still continues.


2020 ◽  
Vol 24 (5) ◽  
pp. 473-486 ◽  
Author(s):  
Ligia S. da Silveira Pinto ◽  
Thatyana R. Alves Vasconcelos ◽  
Claudia Regina B. Gomes ◽  
Marcus Vinícius N. de Souza

Azetidin-2-ones (β-lactams) and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, anticancer, anti-diabetic, anti-inflammatory and anticonvulsant. Efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. The present review aimed to highlight some recent discoveries (2013-2019) on the development of novel azetidin-2-one-based compounds as potential anticancer agents.


2020 ◽  
Vol 17 ◽  
Author(s):  
Mohsen A.-M. Gomaa ◽  
Huda A. Ali

Background : The reactivity of 4-(dicyanomethylene)-3-methyl-l-phenyl-2-pyrazoline-5-one DCNP 1 and its derivatives makes it valuable as a building block for the synthesis of heterocyclic compounds like pyrazolo-imidazoles, - thiazoles, spiropyridines, spiropyrroles, spiropyrans and others. As a number of publications have reported on the reactivity of DCNP and its derivatives, we compiled some features of this interesting molecule. Objective: This article aims to review the preparation of DCNP, its reactivity and application in heterocyclic and dyes synthesis. Conclusion: In this review we have provided an overview of recent progress in the chemistry of DCNP and its significance in synthesis of various classes of heterocyclic compounds and dyes. The unique reactivity of DCNP offers unprecedentedly mild reaction conditions for the generation of versatile cynomethylene dyes from a wide range of precursors including amines, α-aminocarboxylic acids, their esters, phenols, malononitriles and azacrown ethers. We anticipate that more innovative transformations involving DCNP will continue to emerge in the near future.


Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 249
Author(s):  
Raquel G. Soengas ◽  
Humberto Rodríguez-Solla

The 1,3-butadiene motif is widely found in many natural products and drug candidates with relevant biological activities. Moreover, dienes are important targets for synthetic chemists, due to their ability to give access to a wide range of functional group transformations, including a broad range of C-C bond-forming processes. Therefore, the stereoselective preparation of dienes have attracted much attention over the past decades, and the search for new synthetic protocols continues unabated. The aim of this review is to give an overview of the diverse methodologies that have emerged in the last decade, with a focus on the synthetic processes that meet the requirements of efficiency and sustainability of modern organic chemistry.


2013 ◽  
Vol 2013 ◽  
pp. 1-4 ◽  
Author(s):  
Vishal Banewar

Pyrazolines are well known and important nitrogen containing 5-membered heterocyclic compounds. In the present investigation, a series of various heteroaryl chalcones and pyrazolines were synthesized by condensing formylquinolines with diverse ketones. The newly synthesized 2-pyrazolines were characterized on the basis of elemental analysis and spectroscopic data. All of the newly synthesized target compounds were selected by the NCI forin vitrobiological evaluation. These active compounds exhibited broad spectrum of various biological activities. Most of the compounds showed potent activity.


2021 ◽  
Vol 4 (2) ◽  
pp. 47-53
Author(s):  
N. Y. Monka ◽  
◽  
N. E. Stadnytska ◽  
I. R. Buchkevych ◽  
K. O. Kaplia ◽  
...  

Benzoquinone and its reduced form hydroquinone belong to phenolic compounds and are found in living organisms in free form or in glycosides. They are active substances of some medicinal plants and have a pharmacological effect on the human body. Accordingly, their derivatives are important objects for chemical synthesis and development of new drugs. This article presents the findings of the structural design of substances with benzoquinone or hydroquinone fragment and sulfur-containing compound. By use of appropriate on-line programs a predictive screening of the biological activity and cytotoxicity of thiosulfonate derivatives of benzoquinone and hydroquinone has been conducted. It has been found that they have immense methodological potential to be synthesized by substances with a wide range of biological activities and a high value of probable activity, which substantiates the feasibility of conducting experimental studies on their biological activity, particularly anticancer.


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