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.

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.

Cryptic Host Defense Peptides: Multifaceted Activity and Prospects for Medicinal Chemistry

2020 ◽  
Vol 20 (14) ◽  
pp. 1274-1290
Author(s):  
Bruna de Oliveira Costa ◽  
Octávio Luiz Franco
Keyword(s):  
Host Defense ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Proteolytic Processing ◽  
Biologically Active ◽  
Host Defense Peptides ◽  
Clinical Phase ◽  
Evolutionarily Conserved ◽  
Defense Peptides ◽  
Endogenous Precursor

Host defense peptides (HDPs) comprise a heterogeneous group of evolutionarily conserved and biologically active small molecules that are produced by different organisms. HDPs are widely researched because they often have multiple biological activities, for example antimicrobial, immunomodulatory and anticancer activity. In this context, in this review we focus on cryptic HDPs, molecules derived specifically from proteolytic processing of endogenous precursor proteins. Here, we explore the biological activity of such molecules and we further discuss the development of optimized sequences based on these natural cryptic HDPs. In addition, we present clinical-phase studies of cryptic HDPs (natural or optimized), and point out the possible applicability of these molecules in medicinal chemistry.

Biological Significance of Imidazole-based Analogues in New Drug Development

2020 ◽  
Vol 17 (5) ◽  
pp. 574-584 ◽  
Author(s):  
Pratiksha N. Chopra ◽  
Jagdish K. Sahu
Keyword(s):  
Medicinal Chemistry ◽  
Biological Activities ◽  
Biological Significance ◽  
Water Soluble ◽  
Biologically Active ◽  
Bioactive Molecules ◽  
Ring Structures ◽  
Antibacterial And Antifungal ◽  
Therapeutic Compounds ◽  
Synthetic Medicinal

In the field of heterocyclic medicinal chemistry, especially five-membered ring structures containing a nitrogen atom, imidazole core is an imperative aromatic heterocycle which is usually present in naturally occurring products and synthetic bioactive molecules. The occurrence of imidazole moiety in therapeutic compounds may be beneficial in terms of improving water-soluble properties due to its two nitrogen atoms which leads to the creation of hydrogen bonds. The imidazole nucleus has also been recognized as an important isostere of triazole, pyrazole, thiazole, tetrazole, oxazole, amide etc. for the purpose of designing and development of various biologically active molecules. Moreover, imidazole core as an attractive binding site could interact with diverse cations and anions as well as biomolecules through different reactions in the human biological system thus displaying extensive biological activities. This effort thoroughly provides a wide-ranging assessment in current drug discovery and developments of imidazolebased analogues in the entire series of synthetic medicinal chemistry as antibacterial and antifungal, anticancer, anti-tubercular, analgesic and anti-inflammatory, anti-neuropathic, antihypertensive, anti-allergic, anti-parasitic, antiviral, antidepressant, anti-obesity and so on, altogether with their prospective approaches in diagnostic and pathological field. It is expected that the present review will be supportive on behalf of new opinions in the search for rational strategies of more efficacious and less toxic medicinal agents and drugs containing imidazole core.

scholarly journals An Overview of the Synthesis and Antimicrobial, Antiprotozoal, and Antitumor Activity of Thiazole and Bisthiazole Derivatives

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 624
Author(s):  
Anca-Maria Borcea ◽  
Ioana Ionuț ◽  
Ovidiu Crișan ◽  
Ovidiu Oniga
Keyword(s):  
Antitumor Activity ◽  
Pharmacological Activity ◽  
Medicinal Chemistry ◽  
Scientific Literature ◽  
Biological Activities ◽  
Biologically Active ◽  
Synthetic Compounds ◽  
Current Review ◽  
Heteroaromatic Ring ◽  
Extensive Range

Thiazole, a five-membered heteroaromatic ring, is an important scaffold of a large number of synthetic compounds. Its diverse pharmacological activity is reflected in many clinically approved thiazole-containing molecules, with an extensive range of biological activities, such as antibacterial, antifungal, antiviral, antihelmintic, antitumor, and anti-inflammatory effects. Due to its significance in the field of medicinal chemistry, numerous biologically active thiazole and bisthiazole derivatives have been reported in the scientific literature. The current review provides an overview of different methods for the synthesis of thiazole and bisthiazole derivatives and describes various compounds bearing a thiazole and bisthiazole moiety possessing antibacterial, antifungal, antiprotozoal, and antitumor activity, encouraging further research on the discovery of thiazole-containing drugs.

scholarly journals Special Issue “Recent Advances in the Synthesis, Functionalization and Applications of Pyrazole-Type Compounds”

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4989
Author(s):  
Vera L. M. Silva ◽  
Artur M. S. Silva
Keyword(s):  
Molecular Weight ◽  
Physicochemical Properties ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Reduced Form ◽  
Low Molecular Weight ◽  
Special Issue ◽  
Recent Advances ◽  
Low Molecular Weight Compounds ◽  
Privileged Scaffolds

Pyrazoles and their reduced form, pyrazolines, are considered privileged scaffolds in medicinal chemistry, owing to their remarkable biological activities, physicochemical properties and occurrence in many low-molecular-weight compounds present in several marketed drugs (e [...]

One-pot Synthesis of Pyrano[2,3-c]pyrazole Derivatives via Multicomponent Reactions (MCRs) and their Applications in Medicinal Chemistry

2021 ◽  
Vol 19 ◽  
Author(s):  
Swapan Kumar Biswas ◽  
Debasis Das
Keyword(s):  
Multicomponent Reactions ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Biologically Active ◽  
Pyrazole Derivatives ◽  
One Pot ◽  
Discovery Research ◽  
Drug Discovery Research ◽  
Biological Interest ◽  
Derivatives Of

Background: Many pyrano[2,3-c]pyrazole derivatives display diverse biological activities and some of them are known as anticancer, analgesic, anticonvulsant, antimicrobial, anti-inflammatory, and anti-malarial agents. In recent years, easy convergent, multicomponent reactions (MCRs) have been adopted to make highly functionalizedpyrano[2,3-c]pyrazole derivatives of biological interest. The synthesis of 1,4-dihydropyrano[2,3-c]pyrazole (1,4-DHPP, 2), 2,4-dihydropyrano[2,3-c]pyrazole (2,4-DHPP, 3), 4-hydroxypyrano[2,3-c]pyrazole (4-HPP, 4) derivatives, 1,4,4-substitied pyranopyrazole (SPP, 5) were reported via two-, three-, four- and five-component reactions (MCRs). Methods: This review article compiles the preparation of pyrano[2,3-c]pyrazole derivatives, and it highlights the applications of various pyrano[2,3-c]pyrazole derivatives in medicinal chemistry. Results: Varieties of pyrano[2,3-c]pyrazole derivatives were achieved via “One-pot” multicomponent reactions (MCRs). Different reaction conditions in the presence of a catalyst or without catalysts were adapted to prepare the pyrano[2,3-c]pyrazole derivatives. Conclusion: Biologically active pyrano[2,3-c]pyrazole derivatives were prepared and used in drug discovery research.

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.

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.

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