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.

scholarly journals Co-Microencapsulation of Anthocyanins from Black Currant Extract and Lactic Acid Bacteria in Biopolymeric Matrices

Molecules ◽  
2020 ◽  
Vol 25 (7) ◽  
pp. 1700 ◽  
Author(s):  
Iuliana Maria Enache ◽  
Aida Mihaela Vasile ◽  
Elena Enachi ◽  
Vasilica Barbu ◽  
Nicoleta Stănciuc ◽  
...  
Keyword(s):  
Lactic Acid ◽  
Lactic Acid Bacteria ◽  
Biological Activities ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Confocal Laser ◽  
In Vitro Digestibility ◽  
Black Currant ◽  
Active Compounds ◽  
Food Ingredients

Anthocyanins from black currant extract and lactic acid bacteria were co-microencapsulated using a gastro-intestinal-resistant biocomposite of whey protein isolate, inulin, and chitosan, with an encapsulation efficiency of 95.46% ± 1.30% and 87.38% ± 0.48%, respectively. The applied freeze-drying allowed a dark purple stable powder to be obtained, with a satisfactory content of phytochemicals and 11 log colony forming units (CFU)/g dry weight of powder (DW). Confocal laser microscopy displayed a complex system, with several large formations and smaller aggregates inside, consisting of biologically active compounds, lactic acid bacteria cells, and biopolymers. The powder showed good storage stability, with no significant changes in phytochemicals and viable cells over 3 months. An antioxidant activity of 63.64 ± 0.75 mMol Trolox/g DW and an inhibitory effect on α-amylase and α-glucosidase of 87.10% ± 2.08% and 36.96% ± 3.98%, respectively, highlighted the potential biological activities of the co-microencapsulated powder. Significantly, the in vitro digestibility profile showed remarkable protection in the gastric environment, with controlled release in the intestinal simulated environment. The powder was tested by addition into a complex food matrix (yogurt), and the results showed satisfactory stability of biologically active compounds when stored for 21 d at 4 °C. The obtained results confirm the important role of microencapsulation in ensuring a high degree of protection, thus allowing new approaches in developing food ingredients and nutraceuticals, with enhanced functionalities.

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.

Quinoline: an attractive scaffold in drug design

2021 ◽  
Vol 21 ◽  
Author(s):  
Lucas F. E. Moor ◽  
Thatyana R. A. Vasconcelos ◽  
Raisa da R. Reis ◽  
Ligia S. S. Pinto ◽  
Thamires M. da Costa
Keyword(s):  
Side Effects ◽  
Drug Design ◽  
Heterocyclic Compounds ◽  
Rational Design ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Bioactive Molecules ◽  
Pharmacological Properties ◽  
Important Group ◽  
Wide Range

: Quinoline and its derivatives comprise an important group of heterocyclic compounds that exhibits a wide range of pharmacological properties such as antibacterial, antiviral, anticancer, antiparasitic, anti-Alzheimer and anticholesterol. In fact, the quinoline nucleus is found in the structure of many drugs and in rational design in medicinal chemistry for the discovery of novel bioactive molecules. Persistent efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. This review highlights some discoveries on the development of quinoline-based compounds in recent years (2013-2019) focusing on their biological activities, including anticancer, antitubercular, antimalarial, anti-ZIKV, anti-DENV, anti-Leishmania and anti-Alzheimer’s disease.

scholarly journals Bioactive Phytochemicals: Bioactivity, Sources, Preparations, and/or ModificationsviaSilver Tetrafluoroborate Mediation

2015 ◽  
Vol 2015 ◽  
pp. 1-22 ◽  
Author(s):  
Matthew C. Achilonu ◽  
Dennis O. Umesiobi
Keyword(s):  
Biological Activities ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Bioactive Phytochemicals ◽  
Effective Reaction

This review provides an overview of the biological activities, natural occurrences, and the silver tetrafluoroborate- (AgBF4-) mediated synthesis of proanthocyanidins, glycosides, N-heterocyclic alkaloid analogues (of pyrrole, morphine, quinoline, isoquinoline, and indole), furan analogues, and halocompounds. AgBF4has been reviewed as an effective reaction promoter, used extensively in the synthesis of relevant biologically active compoundsviacarbon-carbon and carbon-heteroatom bonds formation. The literatures from 1979 to April 2014 were reviewed.

scholarly journals 2,3-Dihydroquinazolin-4(1H)-one as a privileged scaffold in drug design

RSC Advances ◽  
2018 ◽  
Vol 8 (37) ◽  
pp. 20894-20921 ◽  
Author(s):  
Mariateresa Badolato ◽  
Francesca Aiello ◽  
Nouri Neamati
Keyword(s):  
Drug Design ◽  
Structural Component ◽  
Heterocyclic Compounds ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Privileged Scaffold

2,3-Dihydroquinazolin-4-one (DHQ) belongs to the class of nitrogen-containing heterocyclic compounds representing a core structural component in various biologically active compounds.

A comprehensive review on pyranoindole-containing agents

2021 ◽  
Vol 28 ◽  
Author(s):  
Alessia Catalano ◽  
Domenico Iacopetta ◽  
Jessica Ceramella ◽  
Carmela Saturnino ◽  
Maria Stefania Sinicropi
Keyword(s):  
Natural Products ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Therapeutic Agents ◽  
Biologically Active ◽  
Bioactive Molecules ◽  
Structural Motif ◽  
Huge Number ◽  
Naturally Occurring ◽  
Active Natural

: A huge number of nitrogen-containing heterocyclic compounds are ubiquitous in natural products, pharmaceuticals, and bioactive molecules. Among these, the pyranoindole represents an important structural motif, as it constitutes the central subunit in both the biologically active natural products and therapeutic agents. Talathermophilins, notoamides, norgeamides, carneamides, and versicamides are examples of naturally occurring pyranoindoles, while the well-known etodolac and pemedolac are a tetrahydropyrano[3,4-b]indole deriving from synthetic procedures. Besides the well-known antiinflammatory and fibrinolytic activity, molecules comprising the pyranoindole framework have been demonstrated to exhibit various biological activities, such as antiulcer, antidepressant, analgesic, and antiproliferative. Herein, we report the most common natural and synthetic products bearing a pyranoindole nucleus, their syntheses, and biological activities.

Electrophile Promoted Cyclization of ortho-Aryl Substituted Ynamides: Construction of 3-Amino-4-Halo- or 4-Seleno-Isocoumarin Derivatives

2021 ◽  
Author(s):  
Isabelle Gillaizeau ◽  
Loic Habert ◽  
Iryna Diachenko ◽  
Pascal Retailleau
Keyword(s):  
Medicinal Chemistry ◽  
Building Blocks ◽  
Biologically Active Compounds ◽  
Core Structure ◽  
Biologically Active ◽  
Active Compounds ◽  
The Core

Isocoumarins are important building blocks in medicinal chemistry. They are widespread in the core structure of biologically active compounds. Here we report the development of an efficient and highly reactive...

Recent Developments in the Synthetic Uses of Silyl-protected Enoldiazoacetates for Heterocyclic Syntheses

2014 ◽  
Vol 67 (3) ◽  
pp. 365 ◽  
Author(s):  
Xinfang Xu ◽  
Michael P. Doyle
Keyword(s):  
Heterocyclic Compounds ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Diazo Compounds ◽  
Cycloaddition Reactions ◽  
Insertion Reactions ◽  
Active Compounds ◽  
The Core ◽  
Recent Developments ◽  
Metal Catalyzed

Diazo compounds have been used as precursors to a wide variety of heterocyclic compounds that represent the core structural subunits in many biologically active compounds. Various methodologies have been established for their synthesis via metal-catalyzed carbene transformations. Although the advantages of vinyldiazoacetates have been known for many years, realization of the synthetic use of enoldiazoacetates has been more recent. This review covers advances in the utility of silyl-protected enoldiazoacetates in heterocycle syntheses that include X–H insertion reactions, ylide rearrangements, formal [3+3]- and [4+3]-cycloaddition reactions, and other traditional and unusual metal carbene transformations.

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