Synthesis and Functionalization of Coumarin-Pyrazole Scaffold: Recent Development, Challenges and Opportunities

2021 ◽  
Vol 18 ◽  
Author(s):  
Nitin K. Jadhav ◽  
Balkrishna R. Kale ◽  
Mohammad S. Alam ◽  
Vishwas B. Gaikwad ◽  
Virendra Prasad ◽  
...  
Keyword(s):  
Heterocyclic Compounds ◽  
Structural Motif ◽  
Pharmacological Properties ◽  
Lead Compounds ◽  
Drug Molecules ◽  
Dna And Rna ◽  
Biological Studies ◽  
Challenges And Opportunities ◽  
First Time ◽  
Made In

: Heterocycles are the main structural motif of DNA and RNA and play crucial role in various chemical reactions of metabolisms. Therefore, heterocyclic compounds show good physiological and pharmacological properties. Coumarin and pyrazole scaffold present in many commercial drug molecules and natural products. This review gives first time gives an overview of the progress made in the synthesis and functionalization of coumarin-pyrazole hybrid heterocycle. It also includes discussion on the possible reactive sites of heterocycles, functionalization and mechanistic pathways to incorporate pyrazole pharmacophore unit in synthesis. Several synthesis and biological studies revealed that combination of coumarin-pyrazole moiety is a prominent structural motif to find lead compounds in drug discovery.

scholarly journals Biological Potential and Chemical Properties of Pyridine and Piperidine Fused Pyridazine Compounds: Pyridopyridazine a Versatile Nucleus

2016 ◽  
Vol 1 (1) ◽  
pp. 29 ◽  
Author(s):  
Mohammad Asif
Keyword(s):  
Nitrogen Atom ◽  
Structural Feature ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Chemical Properties ◽  
Pharmacological Properties ◽  
Drug Molecules ◽  
Biological Potential ◽  
Different Types ◽  
And Chemical Properties

Pyridopyridazine compounds are important nitrogen atom containing heterocyclic compounds due to their pharmacological versatility. This heterocycle system characterized a structural feature for different types of bioactive compounds that exhibiting various types of biological activities which make it an attractive scaffold for the design and development of new drug molecules. This article provided information about the pharmacological properties of pyridopyridazines derivatives.

scholarly journals Bugs as Cancer Drugs: Challenges and Opportunities

2019 ◽  
Vol 39 (15) ◽  
Author(s):  
Phillip J. Daschner ◽  
Avraham Rasooly ◽  
Jeffrey D. White
Keyword(s):  
Cancer Therapy ◽  
Solid Tumors ◽  
National Cancer Institute ◽  
Recent Progress ◽  
Cancer Therapies ◽  
Challenges And Opportunities ◽  
Bacterial Therapy ◽  
Funding Opportunities ◽  
First Time ◽  
Made In

ABSTRACT The first nonsurgical cancer therapy was bacterial therapy introduced in 1891 to treat solid tumors. Because in many cases it was harmful and ineffective, and with the emergence of radiotherapy and chemotherapy, bacterial therapy was discontinued. Motivated by the need to improve targeting of solid tumors and in light of recent progress made in developing microbial therapies, the National Cancer Institute has for the first time issued funding opportunities to stimulate research on bacterium-based cancer therapies for conditions under which current cancer therapies are inadequate.

Site-Selective Shpol'skii Spectrometry of Sulfur-, Oxygen-, and Nitrogen-Containing Aromatic Compounds in Complex Samples

1988 ◽  
Vol 42 (5) ◽  
pp. 731-740 ◽  
Author(s):  
A. E. Elsaiid ◽  
R. Walker ◽  
S. Weeks ◽  
A. P. D'Silva ◽  
V. A. Fassel
Keyword(s):  
Aromatic Compounds ◽  
Heterocyclic Compounds ◽  
Direct Determination ◽  
Emission Spectra ◽  
Complex Samples ◽  
Biological Studies ◽  
Polycyclic Aromatic ◽  
Site Selective ◽  
First Time ◽  
Derivatives Of

Laser excited Shpol'skii spectrometry (LESS) was utilized to directly determine nitrogen (N-), oxygen (O-), and sulfur (S-) heterocyclic compounds in solvent refined coal (SRC-II), petroleum crude oil, and carbon black. Characteristic quasilinear LESS excitation and emission spectra of the heterocyclic compounds are presented for the first time under site-selective conditions. Deuterated analogs of dibenzothiophene and dibenzofuran were utilized for quantitation. Site-selective fluorescence spectra of aminopyrene derivatives of polycyclic aromatic compounds (PAC) are also presented for the first time. The potential for utilizing the LESS technique in critical environment and biological studies for the direct determination of N-, O-, and S-heterocyclic compounds and substitutional derivatives of parent PAC has been demonstrated.

Recent Advances in β-lactam Derivatives as Potential Anticancer Agents

2020 ◽  
Vol 20 (16) ◽  
pp. 1468-1480
Author(s):  
Xinfen Zhang ◽  
Yanshu Jia
Keyword(s):  
Anticancer Agents ◽  
Mechanisms Of Action ◽  
Pharmacological Properties ◽  
Drug Resistant ◽  
Therapeutic Application ◽  
Lead Compounds ◽  
Potential Therapeutic Application ◽  
Made In ◽  
Critical Aspects ◽  
Control And Eradication

Cancer, accounts for around 10 million deaths annually, is the second leading cause of death globally. The continuous emergency of drug-resistant cancers and the low specificity of anticancer agents are the main challenges in the control and eradication of cancers, so it is imperative to develop novel anticancer agents. Immense efforts have been made in developing new lead compounds and novel chemotherapeutic strategies for the treatment of various forms of cancers in recent years. β-Lactam derivatives constitute versatile and attractive scaffolds for the drug discovery since these kinds of compounds possess a variety of pharmacological properties, and some of them exhibited promising potency against both drug-sensitive and drug-resistant cancer cell lines. Thus, β-lactam moiety is a useful template for the development of novel anticancer agents. This review will provide an overview of β-lactam derivatives with the potential therapeutic application for the treatment of cancers covering articles published between 2000 and 2020. The mechanisms of action, the critical aspects of design and structureactivity relationships are also discussed.

A Mini-Review on Pharmacological Importance of Benzothiazole Scaffold

2020 ◽  
Vol 17 ◽  
Author(s):  
Mohammad Asif ◽  
Mohd. Imran
Keyword(s):  
Heterocyclic Compounds ◽  
Biologically Active ◽  
Pharmacological Properties ◽  
Pharmacological Activities ◽  
Structural Alterations ◽  
Benzothiazole Derivatives ◽  
Drug Molecules ◽  
Anti Inflammatory ◽  
Almost All

: Heterocyclic compounds are important because they have almost all types of pharmacological properties. Due to these properties of heterocyclic compounds, they attracted the researchers for the development of more effective newer drug molecules. In this review, we are focused on benzothiazole and its derivatives, which are used for the synthesis of various biologically active molecules. Benzothiazole derivatives have been possessed the various type of pharmacological activities like antimicrobial, anti-inflammatory, analgesic, anticonvulsant, antiviral, anthelmintic, antioxidant, anticancer, and other anticipated activities. Hence, structural alterations have resulted in different benzothiazole derivatives that illustrated a wide variety of pharmacological activities.

scholarly journals Gene identification and genome annotation in Caenorhabditis briggsae by high throughput 5' RNA end determination

2021 ◽  
Author(s):  
Nikita Jhaveri ◽  
Wouter van den Berg ◽  
Byung Joon Hwang ◽  
Hans-Michael Muller ◽  
Paul W Sternberg ◽  
...  
Keyword(s):  
Caenorhabditis Briggsae ◽  
Spliced Leader ◽  
C Elegans ◽  
Functional Studies ◽  
Biological Studies ◽  
Trans Splicing ◽  
Substantial Progress ◽  
End Sequences ◽  
First Time ◽  
Made In

The nematode Caenorhabditis briggsae is routinely used in comparative and evolutionary studies involving its well-known cousin C. elegans. The C. briggsae genome sequence has accelerated research by facilitating the generation of new resources, tools, and functional studies of genes. While substantial progress has been made in predicting genes and start sites, experimental evidence is still lacking in many cases. Here, we report an improved annotation of the C. briggsae genome using the Trans-spliced Exon Coupled RNA End Determination (TEC-RED) technique. In addition to identifying 5' ends of expressed genes, the technique has enabled the discovery of operons and paralogs. Application of TEC-RED yielded 10,243 unique 5' end sequences with matches in the C. briggsae genome. Of these, 6,395 were found to represent 4,252 unique genes along with 362 paralogs and 52 previously unknown exons. The method also identified 493 operons, including 334 that are fully supported by tags. Additionally, two SL1-type operons were discovered. Comparisons with C. elegans revealed that 40% of operons are conserved. Further, we identified 73 novel operons, including 12 that entirely lack orthologs in C. elegans. Among other results, we found that 14 genes are trans-spliced exclusively in C. briggsae compared with C. elegans. Altogether, the data presented here serves as a rich resource to aid biological studies involving C. briggsae. Additionally, this work demonstrates the use of TEC-RED for the first time in a non-elegans nematode and suggests that it could apply to other organisms with a trans-splicing reaction from spliced leader RNA.

Mosses and lichens of Shokalsky Island (Kara Sea, Yamal-Nenets Autonomous Area)

2020 ◽  
Vol 54 (2) ◽  
pp. 497-513 ◽  
Author(s):  
L. N. Beldiman ◽  
I. N. Urbanavichene ◽  
V. E. Fedosov ◽  
E. Yu. Kuzmina
Keyword(s):  
Plant Communities ◽  
Species Distribution ◽  
Arctic Tundra ◽  
Kara Sea ◽  
Lichenicolous Fungi ◽  
South West ◽  
West Part ◽  
First Time ◽  
Nenets Autonomous ◽  
Made In

We studied in detail a moss-lichen component of Shokalsky Island vegetation for the first time and identified 79 species of mosses and 54 species and 2 subspecies of lichens and lichenicolous fungi. All species of mosses and 23 species and 2 subspecies of lichens and lichenicolous fungi are recorded for the first time for the island. The study is based on collections made in South West part of the island, in arctic tundra. We also explored the participation of the mosses and lichens in the main types of plant communities and the species distribution in 10 ecotopes. The paper describes the noteworthy findings (Abrothallus parmeliarum, Aongstroemia longipes, Arthonia peltigerea, Caloplaca caesiorufella, Catillaria stereocaulorum, Ceratodon heterophyllus, Lecanora leptacinella, Sphagnum concinnum, S. olafii) and features of bryo- and lichenoflora of Shokalsky Island.

Biologically Active 2,5-Disubstituted-1,3,4-Oxadiazoles

2009 ◽  
Vol 2 (1) ◽  
pp. 390-406
Author(s):  
Harish Rajak ◽  
Murli Dhar Kharya ◽  
Pradeep Mishra
Keyword(s):  
Heterocyclic Compounds ◽  
Medical Literature ◽  
Biological Activities ◽  
Biologically Active ◽  
Pharmacological Properties ◽  
Clinical Use ◽  
Synthetic Drugs ◽  
Physiologic Activity ◽  
Pharmacologically Active

There are vast numbers of pharmacologically active heterocyclic compounds in regular clinical use. The presence of heterocyclic structures in diverse types of compounds is strongly indicative of the profound effects such structure exerts on physiologic activity, and recognition of this is abundantly reflected in efforts to find useful synthetic drugs. The 1,3,4-oxadiazole nucleus has emerged as one of the potential pharmacophore responsible for diverse pharmacological properties. Medical Literature is flooded with reports of a variety of biological activities of 2,5-Disubstituted-1,3,4-oxadiazoles. The present work is an attempt to summarize and enlist the various reports published on biologically active 2,5-disubstituted-1,3,4-oxadiazoles.

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.

Synthesis and Biological Potentials of Quinoline Analogues: A Review of Literature

2019 ◽  
Vol 16 (7) ◽  
pp. 653-688 ◽  
Author(s):  
Leena Kumari ◽  
Salahuddin ◽  
Avijit Mazumder ◽  
Daman Pandey ◽  
Mohammad Shahar Yar ◽  
...  
Keyword(s):  
Biological Activity ◽  
Heterocyclic Compounds ◽  
Building Blocks ◽  
Vital Role ◽  
Review Of Literature ◽  
Drug Discovery Process ◽  
Active Compounds ◽  
Lead Compounds ◽  
Synthetic Approaches ◽  
Derivatives Of

Heterocyclic compounds are well known for their different biological activity. The heterocyclic analogs are the building blocks for synthesis of the pharmaceutical active compounds in the organic chemistry. These derivatives show various type of biological activity like anticancer, antiinflammatory, anti-microbial, anti-convulsant, anti-malarial, anti-hypertensive, etc. From the last decade research showed that the quinoline analogs plays a vital role in the development of newer medicinal active compounds for treating various type of disease. Quinoline reported for their antiviral, anticancer, anti-microbial and anti-inflammatory activity. This review will summarize the various synthetic approaches for synthesis of quinoline derivatives and to check their biological activity. Derivatives of quinoline moiety plays very important role in the development of various types of newer drugs and it can be used as lead compounds for future investigation in the field of drug discovery process.

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