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.

Coumarin: A Promising Scaffold for Design and Development of Bioactive Agents

2020 ◽  
Vol 16 (6) ◽  
pp. 837-852 ◽  
Author(s):  
Hanan M. Alshibl ◽  
Ebtehal S. Al-Abdullah ◽  
Hamad M. Alkahtani
Keyword(s):  
Biological Activities ◽  
Biologically Active ◽  
Present Review ◽  
Coumarin Derivatives ◽  
Design And Development ◽  
Strong Potential ◽  
Starting Point ◽  
Wide Range ◽  
Anti Inflammatory ◽  
Bioactive Agents

Background: As coumarin derivatives are known to prevent and treat various diseases, they have attracted the attention of medicinal chemists. They have strong potential as drugs because their benzopyrone structure can interact noncovalently with numerous enzymes and receptors. Methods: The aim of this review was to summarize the most recently published literature on coumarin derivatives in terms of their antioxidant, antimicrobial, anti-inflammatory, anticancer, and other miscellaneous properties. Results: Coumarin derivatives have a wide range of biological activities. They exhibit antioxidant, antimicrobial, anti-inflammatory, anticancer, anti-coagulant, and anti-Alzheimer effects. Conclusion: The coumarin nucleus is an interesting starting point for the design and development of novel bioactive agents. The present review may help medicinal chemists design biologically active molecules based on the coumarin nucleus.

A Brief Review on the Development of Novel Potentially Active Azetidin-2-ones Against Cancer

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
Keyword(s):  
Side Effects ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Present Review ◽  
Pharmacological Properties ◽  
Important Group ◽  
Wide Range ◽  
Anti Inflammatory

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.

The Molecular Diversity Scope of Urazole in the Synthesis of Organic Compounds

2019 ◽  
Vol 16 (7) ◽  
pp. 953-967 ◽  
Author(s):  
Ghodsi M. Ziarani ◽  
Fatemeh Mohajer ◽  
Razieh Moradi ◽  
Parisa Mofatehnia
Keyword(s):  
Biological Activities ◽  
Biological Properties ◽  
Biologically Active ◽  
Microtubule Assembly ◽  
Heterocyclic Molecules ◽  
Biological Perspective ◽  
Highly Active ◽  
Anti Inflammatory ◽  
High Yields ◽  
Short Time

Background: As a matter of fact, nitrogen as a hetero atom among other atoms has had an important role in active biological compounds. Since heterocyclic molecules with nitrogen are highly demanded due to biological properties, 4-phenylurazole as a compound containing nitrogen might be important in the multicomponent reaction used in agrochemicals, and pharmaceuticals. Considering the case of fused derivatives “pyrazolourazoles” which are highly applicable because of their application for analgesic, antibacterial, anti-inflammatory and antidiabetic activities as HSP-72 induction inhibitors (I and III) and novel microtubule assembly inhibitors. It should be mentioned that spiro-pyrazole also has biological activities like cytotoxic, antimicrobial, anticonvulsant, antifungal, anticancer, anti-inflammatory, and cardiotonic activities. Objective: Urazole has been used in many heterocyclic compounds which are valuable in organic syntheses. This review disclosed the advances in the use of urazole as the starting material in the synthesis of various biologically active molecules from 2006 to 2019. Conclusion: Compounds of urazole (1,2,4-triazolidine-3,5-dione) are the most important molecules which are highly active from the biological perspective in the pharmaceuticals as well as polymers. In summary, many protocols for preparations of the urazole derivatives from various substrates in multi-component reactions have been reported from different aromatic and aliphatic groups which have had carbonyl groups in their structures. It is noted that several catalysts have been synthesized to afford applicable molecules with urazole scaffolds. In some papers, being environmentally friendly, short time reactions and high yields are highlighted in the protocols. There is a room to synthesize new catalysts and perform new reactions by manipulating urazole to produce biologically active compounds, even producing chiral urazole component as many groups of chiral urazole compounds are important from biological perspective.

Chemical Composition of Aegle marmelos: A Review

2021 ◽  
pp. 280-290
Author(s):  
Yogita Chowdhary
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Biologically Active ◽  
Fixed Dose ◽  
Root Bark ◽  
Preclinical Studies ◽  
Aegle Marmelos ◽  
Crude Extracts ◽  
Anti Inflammatory

Aegle marmelos (Bilva) is being used in Ayurveda for the treatment of several inflammatory disorders. The plant is a member of a fixed dose combination of Dashamoola in Ayurveda. However, the usage of roots/root bark or stems is associated with sustainability concerns. Bael (Aegle marmelos (L.) Corr.) is an important medicinal plant of India. Leaves, fruits, stem and roots of A. marmelos have been used in ethno medicine to exploit its' medicinal properties including astringent, antidiarrheal antidysenteric, demulcent, antipyretic and anti-inflammatory activities. Compounds purified from bael have been proven to be biologically active against several major diseases including cancer, diabetes and cardiovascular diseases. Preclinical studies indicate the therapeutic potential of crude extracts of A. marmelos in the treatment of many microbial diseases, diabetes and gastric ulcer. This review covers the biological activities of some isolated chemical constituents of A. marmelos and preclinical studies on some crude extracts and pure compounds to explore novel bioactive compounds for therapeutic application. Aegle marmelos (L.) is a seasonal fruit that contains significant amounts of bioactives like, phenolic acids (gallic acids, 2,3-dihydroxy benzoic acid, chlorogenic acid, p-coumaric acid, vanillic acid), flavonoid (rutin), organic acids (oxalic acid, tartaric acid, malic acid, lactic acid, acetic acid, citric acid, propionic acid, succinic acid, fumaric acid), vitamin C, vitamin B group (thiamine, niacin, pyridoxine, pantothenic acid, biotin, cobalamins, riboflavin), tocopherols (α-tocopherol, β-tocopherol, γ-tocopherol, δ-tocopherol), carotenes (α-carotene, β-carotene, γ-carotene, δ-carotene) and also rich in essential minerals (potassium, calcium, phosphorus, sodium, iron, copper, manganese). Hence the use of aegle plays important role as anti-inflammatory.

A OVERVIEW ON ANTIMICROBIAL AND ANTI-INFLAMMATORY ACTIVITY OF 1, 3, 4-OXADIAZOLES

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (02) ◽  
pp. 9-17
Author(s):  
Satvir Singh ◽  
Manpreet Kaur ◽  
Divya Bhandari ◽  
Mandeep Kaur ◽  
Monika Gupta
Keyword(s):  
Biological Activities ◽  
Present Review ◽  
Inflammatory Activity ◽  
World Population ◽  
Microbial Infections ◽  
Anti Inflammatory

1, 3, 4-oxadiazoles first came into the lime light about 80 years ago. With the increasing world population, the number of microbial infections has increased all over. To overcome the continuously spreading harmful microbial infections, the need for newer and newer drugs has increased tremendously. 1, 3, 4- oxadiazoles have been researched for the above mention purpose, because this nucleus has proven beneficial in a number of microbial infections from time to time. In the present review, we are highlight the biological activities being shown by the 1, 3, 4- oxadiazoles.

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.

A Review: Therapeutic and Biological Activity of Benzothiazole Derivatives

2017 ◽  
Vol 4 (3) ◽  
Author(s):  
Suresh Choudhary ◽  
G Jeyabalan ◽  
Naresh Kalra
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
New Products ◽  
Therapeutic Agents ◽  
Present Review ◽  
Benzothiazole Derivatives ◽  
Anti Inflammatory

The Benzothiazole nucleus is present in compounds involved in research aimed at evaluating new products that possess interesting biological activities, such as antitumor, antimicrobial, anthelmintic, antileishmanial, anticonvulsant and anti-inflammatory. The present review focuses on the benzothiazoles with potential activities that are now in development. The synthesized benzothiazole derivatives could be considered as lead molecule for the development of therapeutic agents.

Health Benefits of Furanocoumarins ‘Psoralidin’ An Active Phytochemical of Psoralea corylifolia: The Present, Past and Future Scenario

2019 ◽  
Vol 15 (4) ◽  
pp. 369-376
Author(s):  
Kanika Patel ◽  
Vikas Kumar ◽  
Amita Verma ◽  
Mahfoozur Rahman ◽  
Dinesh Kumar Patel
Keyword(s):  
Biological Activities ◽  
Modern Medicine ◽  
Present Review ◽  
Psoralea Corylifolia ◽  
Antitumor Activities ◽  
Pharmacological Activities ◽  
Discussion Section ◽  
Medicinal Uses ◽  
Anti Inflammatory ◽  
Analytical Tools

Background: Phytoconstituents of fruits, vegetables, spice and herbs are important for human health. Phytoconstituents play an important role in the growth, development, defensive mechanism, colors, odour and flavors of plants. Psoralea corylifolia Linn (P. corylifolia) commonly known as ‘Bakuchi’ belongs to Leguminosae family widely distributed in China and Southeastern Asian countries. Methods: Various electronic databases such as PubMed, Science Direct, Scopus and Google were searched to collect the data of the present review. Further, all the collected information was categorized into different section as per the aim of the paper. Moreover, analyzed data were also presented in the graphical abstract. Results: Seventy-two research and review papers have been collected and were included in the present review. Nineteen papers contained general information’s of P. corylifolia, Psoralens and psoralidin whereas thirty paper data were presented in the pharmacological activities sections and remaining in the Analytical tools and discussion section. From these databases, we can say that P. corylifolia possesses antibacterial, anti-inflammatory, antifungal, antioxidant, antiflarial, estrogenic, antitumour, and immunomodulatory activities. Psoralens are mainly used in the treatment of psoriasis, vitiligo and dermatitis. Topical or oral psoralens followed by UVA radiation exposure are one of the best treatments of leucoderma. Psoralidin exhibits antioxidant, anti-apoptotic, anti-inflammatory and antitumor activities. Conclusion: This review summarizes an overview of P. corylifolia, psoralen and its derivative psoralidin with respects to their pharmacological activities, medicinal uses, biological activities and bioanalytical aspects. These data will be helpful in the translation of information from traditional to the modern medicine of psoralidin.

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.

Anti-Inflammatory Steroids, Lysosomal Stabilization and Parachor

1975 ◽  
Vol 53 (10) ◽  
pp. 1047-1053 ◽  
Author(s):  
Parvez Ahmad ◽  
Colin A. Fyfe ◽  
Alan Mellors
Keyword(s):  
Partition Coefficients ◽  
Biological Activities ◽  
Biologically Active ◽  
Structure Activity ◽  
Assay Methods ◽  
Anti Inflammatory ◽  
Direct Proportionality ◽  
In Vivo Administration

Parachor is an additive constitutive property of a molecule and is related to the molar volume and the surface tension. The parachor of a steroid can be calculated from its constituent atoms and bonds. The parachor of a biologically active molecule is related to the ability of that molecule to permeate hydrophobic regions of cells, especially cellular membranes. An examination of the parachor values of a large number of steroids shows that these values are correlated with a number of different biological activities, from independent sources. The ability of steroids to release lysosomal enzymes from isolated lysosomes in vitro is inversely related to the parachor of the steroid. A similar relationship holds for the release of lysosomal β-glucuronidase (EC 3.2.1.31) from isolated lysosomes of rat preputial gland following in vivo administration of steroids. The relative anti-inflammatory potencies of steroids by several assay methods are directly proportional to their parachors. The relative ability of corticosteroids to uncouple oxidative phosphorylation and to swell isolated mitochondria in vitro show a direct proportionality with the steroidal parachor. The percutaneous absorptions of steroids show good correlation with parachors, stratum corneum – water partition coefficients and amylcaproate–water partition coefficients; but not with hexadecane–water partition coefficients. The application of parachor as a structure–activity correlation parameter in drug design is likely to yield useful information. The advantages and limitations of the calculated parachor method are discussed.

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