Methyl linked pyrazoles: Synthetic and Medicinal Perspective

2021 ◽  
Vol 21 ◽  
Author(s):  
Tulika Sharma ◽  
Joginder Singh ◽  
Bijender Singh ◽  
Ramesh Kataria ◽  
Vinod Kumar
Keyword(s):  
Medicinal Chemistry ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Review Article ◽  
Present Review ◽  
Pyrazole Derivatives ◽  
High Efficacy ◽  
Depth Analysis ◽  
Synthetic Approaches ◽  
Substituted Pyrazoles

: Pyrazoles, an important and well known class of the azole family, have been found to show a large number of applications in various fields specially of medicinal chemistry. Among pyrazole derivatives, particularly, methyl substituted pyrazoles have been reported as the potent medicinal scaffolds that exhibit a wide spectrum of biological activities. The present review is an attempt to highlight the detailed synthetic approaches for methyl substituted pyrazoles along with in depth analysis of their respective medical significances till March2021. It is hoped that literature sum-up in the form of present review article would certainly be a great tool to assist the medicinal chemists for generating new leads possessing pyrazole nucleus with high efficacy and less microbial resistance.

scholarly journals Pyrazolyl-Ureas as Interesting Scaffold in Medicinal Chemistry

Molecules ◽  
2020 ◽  
Vol 25 (15) ◽  
pp. 3457 ◽  
Author(s):  
Chiara Brullo ◽  
Federica Rapetti ◽  
Olga Bruno
Keyword(s):  
P38 Mapk ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Data ◽  
Biologically Active ◽  
Pyrazole Derivatives ◽  
Intracellular Level ◽  
Active Compounds ◽  
Privileged Scaffold

The pyrazole nucleus has long been known as a privileged scaffold in the synthesis of biologically active compounds. Within the numerous pyrazole derivatives developed as potential drugs, this review is focused on molecules characterized by a urea function directly linked to the pyrazole nucleus in a different position. In the last 20 years, the interest of numerous researchers has been especially attracted by pyrazolyl-ureas showing a wide spectrum of biological activities, ranging from the antipathogenic activities (bacteria, plasmodium, toxoplasma, and others) to the anticarcinogenic activities. In particular, in the anticancer field, pyrazolyl-ureas have been shown to interact at the intracellular level on many pathways, in particular on different kinases such as Src, p38-MAPK, TrKa, and others. In addition, some of them evidenced an antiangiogenic potential that deserves to be explored. This review therefore summarizes all these biological data (from 2000 to date), including patented compounds.

scholarly journals Styrylpyrazoles: Properties, Synthesis and Transformations

Molecules ◽  
2020 ◽  
Vol 25 (24) ◽  
pp. 5886
Author(s):  
Pedro M. O. Gomes ◽  
Pedro M. S. Ouro ◽  
Artur M. S. Silva ◽  
Vera L. M. Silva
Keyword(s):  
Biological Activity ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Review Article ◽  
Pyrazole Derivatives ◽  
Huge Number ◽  
Timely Review ◽  
Methods Of Synthesis ◽  
Reduced Forms ◽  
Over Time

The pyrazole nucleus and its reduced forms, pyrazolines and pyrazolidine, are privileged scaffolds in medicinal chemistry due to their remarkable biological activities. A huge number of pyrazole derivatives have been studied and reported over time. This review article gives an overview of pyrazole derivatives that contain a styryl (2-arylvinyl) group linked in different positions of the pyrazole backbone. Although there are studies on the synthesis of styrylpyrazoles dating back to the 1970s and even earlier, this type of compound has rarely been studied. This timely review intends to summarize the properties, biological activity, methods of synthesis and transformation of styrylpyrazoles; thus, highlighting the interest and huge potential for application of this kind of compound.

Recent advancements on Benzimidazole: A versatile scaffold in medicinal chemistry

2021 ◽  
Vol 21 ◽  
Author(s):  
Zohor Mohammad Mahdi Alzhrani ◽  
Mohammad Mahboob Alam ◽  
Syed Nazreen
Keyword(s):  
Clinical Trials ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Review Article ◽  
Present Review ◽  
Benzimidazole Derivatives ◽  
The Past ◽  
Anti Inflammatory

: Benzimidazole is nitrogen containing fused heterocycle which has been extensively explored in medicinal chemistry. Benzimidizole nucleus has been found to possess various biological activities such as anticancer, antimicrobial, anti-inflammatory, antiviral, antitubercular and antidiabetic. A number of benzimidazoles such as bendamustine, pantoprazole have been approved for the treatment of various illnesses whereas galeterone and GSK461364 are in clinical trials. The present review article gives an overview about the different biological activities exhibited by the benzimidazole derivatives as well as different methods used for the synthesis of benzimidazole derivatives for the past ten years.

Synthetic Investigations On Medicinally Important Quinoxaline Scaffold: A Mini Review.

2020 ◽  
Vol 17 ◽  
Author(s):  
Nitin Kumar ◽  
Niranjan Kaushik ◽  
Shiv Kumar ◽  
Vikas Sharma
Keyword(s):  
Biological Activities ◽  
Review Article ◽  
Synthetic Methods ◽  
Present Review ◽  
The Past ◽  
Quinoxaline Derivatives ◽  
Almost All ◽  
Synthetic Approaches ◽  
Heterocyclic Moiety

: Quinoxaline is a versatile heterocyclic moiety that posses almost all types of biological activities. Present work is a sincere attempt to review synthetic investigations of quinoxaline. A wide plethora of literature is available possessing different synthetic methods utilized for the synthesis of quinoxaline based scaffolds. The present review focuses on the various synthetic approaches of quinoxaline derivatives, which includes a summary of the advancement made over the past years in the synthesis of quinoxaline nucleus and its derivatives. Some of these methods are mentioned in the review article associated with industrial applicability.

Arylpyrazoles: Heterocyclic Scaffold of Immense Therapeutic Application

2020 ◽  
Vol 24 (14) ◽  
pp. 1555-1581
Author(s):  
Garima Tripathi ◽  
Anil Kumar Singh ◽  
Abhijeet Kumar
Keyword(s):  
Biological Activities ◽  
Biologically Active ◽  
Present Review ◽  
Pyrazole Derivatives ◽  
Therapeutic Application ◽  
Diverse Range ◽  
Major Class ◽  
Anti Inflammatory

Among the major class of heterocycles, the N-heterocycles, such as pyrazoles, are scaffolds of vast medicinal values. Various drugs and other biologically active molecules are known to contain these N-heterocycles as core motifs. Specifically, arylpyrazoles have exhibited a diverse range of biological activities, including anti-inflammatory, anticancerous, antimicrobial and various others. For instance, arylpyrazoles are present as core moieties in various insecticides, fungicides and drugs such as Celebrex and Trocoxil. The present review will be highlighting the significant therapeutic importance of pyrazole derivatives developed in the last few years.

scholarly journals Substituted Pyrazoles and Their Heteroannulated Analogs—Recent Syntheses and Biological Activities

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4995
Author(s):  
Mohamed Ramadan ◽  
Ashraf A. Aly ◽  
Lamiaa E. Abd El-Haleem ◽  
Mohammed B. Alshammari ◽  
Stefan Bräse
Keyword(s):  
Medicinal Chemistry ◽  
Biological Activities ◽  
Biologically Active ◽  
Substituted Pyrazoles ◽  
Privileged Scaffolds

Pyrazoles are considered privileged scaffolds in medicinal chemistry. Previous reviews have discussed the importance of pyrazoles and their biological activities; however, few have dealt with the chemistry and the biology of heteroannulated derivatives. Therefore, we focused our attention on recent topics, up until 2020, for the synthesis of pyrazoles, their heteroannulated derivatives, and their applications as biologically active moieties. Moreover, we focused on traditional procedures used in the synthesis of pyrazoles.

scholarly journals Revisiting the Structure and Chemistry of 3(5)-Substituted Pyrazoles

Molecules ◽  
2019 ◽  
Vol 25 (1) ◽  
pp. 42 ◽  
Author(s):  
Alina Secrieru ◽  
Paul Michael O’Neill ◽  
Maria Lurdes Santos Cristiano
Keyword(s):  
Organic Synthesis ◽  
Medicinal Chemistry ◽  
Positive Impact ◽  
Biological Activities ◽  
Experimental Methods ◽  
Synthetic Methods ◽  
Conformational Preferences ◽  
Substituted Pyrazoles ◽  
Present Subject

Pyrazoles are known as versatile scaffolds in organic synthesis and medicinal chemistry, often used as starting materials for the preparation of more complex heterocyclic systems with relevance in the pharmaceutical field. Pyrazoles are also interesting compounds from a structural viewpoint, mainly because they exhibit tautomerism. This phenomenon may influence their reactivity, with possible impact on the synthetic strategies where pyrazoles take part, as well as on the biological activities of targets bearing a pyrazole moiety, since a change in structure translates into changes in properties. Investigations of the structure of pyrazoles that unravel the tautomeric and conformational preferences are therefore of upmost relevance. 3(5)-Aminopyrazoles are largely explored as precursors in the synthesis of condensed heterocyclic systems, namely pyrazolo[1,5-a]pyrimidines. However, the information available in the literature concerning the structure and chemistry of 3(5)-aminopyrazoles is scarce and disperse. We provide a revision of data on the present subject, based on investigations using theoretical and experimental methods, together with the applications of the compounds in synthesis. It is expected that the combined information will contribute to a deeper understanding of structure/reactivity relationships in this class of heterocycles, with a positive impact in the design of synthetic methods, where they take part.

Advances on Quinazoline Based Congeners for Anticancer Potential

2021 ◽  
Vol 25 ◽  
Author(s):  
Parul Grover ◽  
Monika Bhardwaj ◽  
Garima Kapoor ◽  
Lovekesh Mehta ◽  
Roma Ghai ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
Anticancer Compounds ◽  
In Vivo Models ◽  
Appropriate Treatment

: The heterocyclic compounds have a great significance in medicinal chemistry because they have extensive biological activities. Cancer is globally the leading cause of death and it is a challenge to develop an appropriate treatment for the management of cancer. Continuous efforts are being made to find a suitable medicinal agent for cancer therapy. Nitrogen-containing heterocycles have received noteworthy attention due to their wide and distinctive pharmacological activities. One of the most important nitrogen-containing heterocycles in medicinal chemistry is ‘quinazoline’ that possesses a wide spectrum of biological properties. This scaffold is an important pharmacophore and is considered a privileged structure. The various substituted quinazolines displayed anticancer activity against different types of cancer. This review highlights the recent advances in quinazoline based molecules as anticancer agents. Several in-vitro and in-vivo models used along with the results are also included. A subpart briefing natural quinazoline containing anticancer compounds is also incorporated in the review.

scholarly journals Coumarin sulfonamide derivatives: An emerging class of therapeutic agents

2020 ◽  
Vol 26 (1) ◽  
pp. 46-59 ◽  
Author(s):  
Ali Irfan ◽  
Laila Rubab ◽  
Mishbah Ur Rehman ◽  
Rukhsana Anjum ◽  
Sami Ullah ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Structural Features ◽  
Therapeutic Agents ◽  
Review Article ◽  
Structural Motif ◽  
Structure Activity ◽  
Anti Cancer ◽  
Novel Therapeutic

AbstractCoumarin sulfonamide is a heterocyclic pharmacophore and an important structural motif which is a core and integral part of different therapeutic scaffolds and analogues. Coumarin sulfonamides are privileged and pivotal templates which have a broad spectrum of applications in the fields of medicine, pharmacology and pharmaceutics. Coumarin sulfonamide exhibited versatile and myriad biomedical activities such as anti-bacterial, antiviral, antifungal, anti-inflammatory and anti-cancer. This review article focuses on the structural features of coumarin sulfonamide derivatives in the treatment of different lethal diseases on the basis of structure-activity relationships (SAR). The plethora of research cited in this review article summarizes and discusses the various substitutions around the coumarin sulfonamide nucleus which have provided a wide spectrum of biological activities and therapeutic potential that has proved attractive to many researchers looking to exploit the coumarin sulfonamide skeleton for drug discovery and the development of novel therapeutic agents.

scholarly journals A CONCISE OVERVIEW ON HETEROCYCLIC COMPOUNDS EXHIBITING PESTICIDAL ACTIVITIES

2021 ◽  
Vol 9 (08) ◽  
pp. 989-1004
Author(s):  
Shailendra Yadav ◽  
◽  
Sushma Singh ◽  
Chitrasen Gupta ◽  
◽  
...  
Keyword(s):  
Organic Compounds ◽  
Heterocyclic Compounds ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Review Article ◽  
Diverse Group ◽  
Concise Overview ◽  
Physiological Properties ◽  
Pharmaceutical Industries

Heterocyclic compounds are numerous and diverse group of organic compounds. Heterocycles are abundantly found in nature and express various physiological properties. Heterocycles are intricately linked to all aspects of life. There are many heterocyclic compounds currently known, and the number is constantly rising owing to extensive synthetic development and their applications. Heterocyclic compounds are used significantly in a number of areas, including biochemistry and medicinal chemistry, and some others. They are predominantly synthesized in agrochemical and pharmaceutical industries due to their potential biological activities. This review article focuses on recently synthesized heterocyclic compounds and their different pesticidal activities such as antifungal, antibacterial, antiviral, nematocidal, insecticidal, acaricidal, and herbicidal.

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