A Review: Therapeutic and Biological Activity of Benzothiazole Derivatives

Author(s):  
Suresh Choudhary ◽  
G Jeyabalan ◽  
Naresh Kalra

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.

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 24 (14) ◽  
pp. 1555-1581
Author(s):  
Garima Tripathi ◽  
Anil Kumar Singh ◽  
Abhijeet Kumar

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.


Plants ◽  
2020 ◽  
Vol 10 (1) ◽  
pp. 32
Author(s):  
Hosakatte Niranjana Murthy ◽  
Guggalada Govardhana Yadav ◽  
Yaser Hassan Dewir ◽  
Abdullah Ibrahim

Many underutilized tree species are good sources of food, fodder and possible therapeutic agents. Balanites aegyptiaca (L.) Delile belongs to the Zygophyllaceae family and is popularly known as “desert date”, reflecting its edible fruits. This tree grows naturally in Africa, the Middle East and the Indian subcontinent. Local inhabitants use fruits, leaves, roots, stem and root bark of the species for the treatment of various ailments. Several research studies demonstrate that extracts and phytochemicals isolated from desert date display antioxidant, anticancer, antidiabetic, anti-inflammatory, antimicrobial, hepatoprotective and molluscicidal activities. Mesocarp of fruits, seeds, leaves, stem and root bark are rich sources of saponins. These tissues are also rich in phenolic acids, flavonoids, coumarins, alkaloids and polysterols. Some constituents show antioxidant, anticancer and antidiabetic properties. The objective of this review is to summarize studies on diverse bioactive compounds and the beneficial properties of B. aegyptiaca.


Author(s):  
Jyothi M ◽  
Ramchander Merugu

Benzoxazoles being structurally similar to bases adenine and guanine interact with biomolecules present in living systems. These compounds possess antimicrobial, central nervous system activities, antihyperglycemic potentiating activity, analgesic, and anti-inflammatory activity. It can also be used as starting material for other bioactive molecules. Modifications in structure and the biological profiles of new generations of benzoxazoles were found to be more potent with enhanced biological activity. Considering all these, we have prepared this review and discussed the synthesis and biological activities of benzoxazoles.


INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (02) ◽  
pp. 9-17
Author(s):  
Satvir Singh ◽  
Manpreet Kaur ◽  
Divya Bhandari ◽  
Mandeep Kaur ◽  
Monika Gupta

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.


2008 ◽  
Vol 3 (11) ◽  
pp. 1934578X0800301
Author(s):  
Alejandro F. Barrero ◽  
M. Mar Herrador ◽  
Pilar Arteaga ◽  
Julieta V. Catalán

Dittrichia viscosa is a plant widely distributed in the Mediterranean region. This species and its components present a broad range of biological activities (for example, anti-inflammatory, antifungal, antiulcer, antiviral, antiparasitic), which are reviewed. Extracts of the species are particularly rich in terpenoids, in particular eudesmane acids, notably ilicic acid (45) and α-costic acid (44). Flavonoids are also abundant, especially during flowering.


2017 ◽  
Vol 59 (3) ◽  
Author(s):  
Eman A. Ahmed

Reaction of (<em>Z</em>)-4-((dimethylamino)methylene)-1-phenylpyrazolidine-3,5-dione (<strong>1</strong>) with different nucleophiles is described. Treatment of enaminone <strong>1 </strong>with phenylhydrazine led to 3-oxo-<em>N’</em>,2-diphenyl-2,3-dihydro-1<em>H</em>-pyrazole-4-carbohydrazide <strong>7</strong>. New enaminone derivatives <strong>2–6 </strong>and <strong>12–14 </strong>were conveniently obtained in high yields via nucleophilic substitution of the dimethylamino group in enaminone <strong>1 </strong>when reacted with <em>o</em>-aminophenol, <em>o</em>-aminothiophenol, ethanolamine, cysteamine hydrochloride, piperidine, morpholine, 2-aminopyridine and glycine. Reaction of enaminone <strong>1 </strong>with diaza-nucleophiles, such as hydrazine hydrate, ethylenediamine and <em>o</em>-phenylenediamine, afforded the corresponding <em>bis</em>-enaminones <strong>9–11</strong>. Anti-inflammatory and antimicrobial activities of some new products were evaluated. Compounds <strong>1, 2, 4, 7, 12a</strong>, and <strong>12b </strong>showed high anti- inflammatory activity compared with indomethacin as the reference, while the highest antimicrobial effect was observed in the case of compound <strong>3</strong>.


2020 ◽  
Vol 17 ◽  
Author(s):  
Tanvi Sahni ◽  
Sunita Sharma ◽  
Diksha Verma ◽  
Pardeep Kaur

Abstract: Coumarin is a heterocyclic scaffold and its derivatives namely Schiff bases, esters, and hydrazides, etc, play an important role in the field of agrochemical and pharmaceutical industry due to its structure. Over the years, various biological activities like antifungal, antimicrobial, anti-viral, anti-cancerous, anti-tumor, anti-inflammatory, anti-filarial, enzyme inhibitors, anti-aflatoxigenic, analgesics, antioxidant and Oestrogenic, etc had been analyzed. This review covers the latest literature and knowledge on the synthetic procedures for various coumarin and its derivatives, biological and pharmacological applications.


Author(s):  
Sumit Kumar ◽  
Arvind Kumar ◽  
Amit Verma ◽  
Arun Kumar Mishra

Background:: The benzothiazole and its derivatives reported an extremely key duty in the progress of commercially important intermediary molecules, which are wanted for the manufacture of various pharmacologically active agents. Introduction:: As a necessary element of ongoing examination for the synthesis of new Nonsteroidal anti-inflammatory agents (NSAIDs), a number of new benzothiazole derivatives were taken under thought for synthesis and were computationally studied along with biological activity. Methods:: Obtainable benzothiazole derivatives were synthesized by the condensing of 2-(4-aminophenoxy)-N- (benzo[d]thiazol-2-yl)acetamide with substituted acetophenones in ethanol in the presence of catalytic amount of glacial acetic acid. The structures of newly synthesized compounds were characterized by IR, NMR spectroscopy and elemental analysis techniques. Several molecular properties of these derivatives were computed in order to estimate their drug like candidates. Molecular docking was performed to these synthesized derivatives with particular reference to cyclooxygenase- 2 (COX-2) enzyme. The synthesized derivatives were screened for their biological activity, including analgesic and antiinflammatory activity as COX-2 inhibitors. Results and Discussion:: From all data, it established that among all target compounds, S-4 (N-(benzo[d]thiazol-2-yl)-2-(4- ((1-(3-nitrophenyl)ethylidene)amino) phenoxy)acetamide) displayed the highest anti-inflammatory and analgesic effects. Conclusion:: All these findings recommended that S-4 might be utilized as a promising new lead compound for Nonsteroidal anti-inflammatory drug (NSAIDs) development.


2019 ◽  
Vol 15 (4) ◽  
pp. 369-376
Author(s):  
Kanika Patel ◽  
Vikas Kumar ◽  
Amita Verma ◽  
Mahfoozur Rahman ◽  
Dinesh Kumar Patel

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.


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