ChemInform Abstract: Recent Developments on Chemistry and Biological Activity of Nucleoside Analogues with an Extra Heteroatom in the Sugar Ring.

ChemInform ◽  
2010 ◽  
Vol 33 (13) ◽  
pp. no-no
Author(s):  
Pedro Merino ◽  
Santiago Franco ◽  
Francisco L. Merchan ◽  
Tomas Tejero
Keyword(s):  
Biological Activity ◽  
Nucleoside Analogues ◽  
Recent Developments ◽  
Sugar Ring

scholarly journals Recent developments of synthesis and biological activity of sultone scaffolds in medicinal chemistry

2021 ◽  
Vol 14 (4) ◽  
pp. 103037
Author(s):  
Yingying Xu ◽  
Ziwen Zhang ◽  
Jingbo Shi ◽  
Xinhua Liu ◽  
Wenjian Tang
Keyword(s):  
Biological Activity ◽  
Medicinal Chemistry ◽  
Recent Developments

scholarly journals Recent developments in the synthesis and biological activity of acridine/acridone analogues

RSC Advances ◽  
2017 ◽  
Vol 7 (26) ◽  
pp. 15776-15804 ◽  
Author(s):  
Monika Gensicka-Kowalewska ◽  
Grzegorz Cholewiński ◽  
Krystyna Dzierzbicka
Keyword(s):  
Biological Activity ◽  
The World ◽  
Recent Developments

Many people in the world struggle with cancer or bacterial, parasitic, viral, Alzheimer's and other diseases.

Synthesis and Biological Activity of a Series of Methylene-Expanded Oxetanocin Nucleoside Analogues

2002 ◽  
Vol 133 (4) ◽  
pp. 499-520 ◽  
Author(s):  
Michael E. Jung ◽  
Akemi Toyota ◽  
Erik de Clercq ◽  
Jan Balzarini
Keyword(s):  
Biological Activity ◽  
Nucleoside Analogues

scholarly journals Biologically active collagen-based scaffolds: advances in processing and characterization

2010 ◽  
Vol 368 (1917) ◽  
pp. 2123-2139 ◽  
Author(s):  
I. V. Yannas ◽  
D. S. Tzeranis ◽  
B. A. Harley ◽  
P. T. C. So
Keyword(s):  
Biological Activity ◽  
Pore Size ◽  
Type I Collagen ◽  
Biologically Active ◽  
Wound Contraction ◽  
Type I ◽  
Structural Determinants ◽  
Ligand Density ◽  
Freeze Dried ◽  
Recent Developments

A small number of type I collagen–glycosaminoglycan scaffolds (collagen–GAG scaffolds; CGSs) have unusual biological activity consisting primarily in inducing partial regeneration of organs in the adult mammal. Two of these are currently in use in a variety of clinical settings. CGSs appear to induce regeneration by blocking the adult healing response, following trauma, consisting of wound contraction and scar formation. Several structural determinants of biological activity have been identified, including ligands for binding of fibroblasts to the collagen surface, the mean pore size (which affects ligand density) and the degradation rate (which affects the duration of the wound contraction-blocking activity by the scaffold). Processing variables that affect these determinants include the kinetics of swelling of collagen fibres in acetic acid, freezing of the collagen–GAG suspension and cross-linking of the freeze-dried scaffold. Recent developments in the processing of CGSs include fabrication of scaffolds that are paucidisperse in pore size, scaffolds with gradients in physicochemical properties (and therefore biological activity) and scaffolds that incorporate a mineral component. Advances in the characterization of the pore structure of CGSs have been made using confocal and nonlinear optical microscopy (NLOM). The mechanical behaviour of CGSs, as well as the resistance to degradative enzymes, have been studied. Following seeding with cells (typically fibroblasts), contractile forces in the range 26–450 nN per cell are generated by the cells, leading to buckling of scaffold struts. Ongoing studies of cell-seeded CGSs with NLOM have shown an advantage over the use of confocal microscopy due to the ability of the former method to image the CGS surfaces without staining (which alters its surface ligands), reduced cell photodamage, reduced fluorophore photobleaching and the ability to image deeper inside the scaffold.

scholarly journals Synthesis and Preliminary Evaluation of Biological Activity of Glycoconjugates Analogues of Acyclic Uridine Derivatives

Molecules ◽  
2018 ◽  
Vol 23 (8) ◽  
pp. 2017 ◽  
Author(s):  
Roman Komor ◽  
Gabriela Pastuch-Gawolek ◽  
Ewelina Krol ◽  
Wieslaw Szeja
Keyword(s):  
Biological Activity ◽  
Bovine Milk ◽  
Nucleoside Analogues ◽  
Preliminary Evaluation ◽  
Synthetic Compounds ◽  
Enzyme Action ◽  
Enzyme Substrates ◽  
Donor Type ◽  
Natural Enzyme ◽  
Activity Of Enzymes

Herein we present the methodology for obtaining glycosyltransferase inhibitors, analogues of natural enzyme substrates of donor-type: UDP-glucose and UDP-galactose. The synthesis concerned glycoconjugates, nucleoside analogues containing an acyclic ribose mimetic linked to a uracil moiety in their structure. The biological activity of the synthesised compounds was determined on the basis of their ability to inhibit the model enzyme action of β-1,4-galactosyltransferase from bovine milk. The obtained results allowed to expand and supplement the existing library of synthetic compounds that are able to regulate the biological activity of enzymes from the GT class.

scholarly journals Investigation of 5’-Norcarbocyclic Nucleoside Analogues as Antiprotozoal and Antibacterial Agents

Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3433 ◽  
Author(s):  
Anastasia Khandazhinskaya ◽  
Elena Matyugina ◽  
Pavel Solyev ◽  
Maggie Wilkinson ◽  
Karen Buckheit ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Biological Activity ◽  
Antibacterial Agents ◽  
Structure Activity Relationship ◽  
Nucleoside Analogues ◽  
Activity Relationship ◽  
Carbocyclic Nucleosides ◽  
Structure Activity ◽  
Small Structure ◽  
Relationship Study

Carbocyclic nucleosides have long played a role in antiviral, antiparasitic, and antibacterial therapies. Recent results from our laboratories from two structurally related scaffolds have shown promising activity against both Mycobacterium tuberculosis and several parasitic strains. As a result, a small structure activity relationship study was designed to further probe their activity and potential. Their synthesis and the results of the subsequent biological activity are reported herein.

Recent advances of thiazole hybrids in biological applications

2019 ◽  
Vol 11 (15) ◽  
pp. 1979-1998 ◽  
Author(s):  
Mehmet Gümüş ◽  
Mehmet Yakan ◽  
İrfan Koca
Keyword(s):  
Biological Activity ◽  
Heterocyclic Compounds ◽  
Chemical Reactivity ◽  
Biological Properties ◽  
The Other ◽  
Hybrid Structures ◽  
Thiazole Ring ◽  
Biological Applications ◽  
Recent Advances ◽  
Recent Developments

Thiazoles have attracted much synthetic interest due to their wide variety of biological properties and are important members of heterocyclic compounds. In recent years, studies on the synthesis of thiazole compounds have been increasing because of the properties of this core. In particular, the hybrid structures in which the thiazole ring and the other nuclei are linked have gained popularity. Hybrid structures are formed by the combination of different groups of chemical reactivity and biological activity characteristics. In this review, we highlight recent developments related to hybrid structures containing a thiazole core, recently developed as anticancer, antibacterial, anti-inflammatory, analgesic, anti-tubercular, antialzheimer and antidiabetic compounds.

Recent developments in the synthesis of tetrazoles and their pharmacological relevance

2020 ◽  
Vol 24 ◽  
Author(s):  
Socorro Leyva-Ramos ◽  
Jaime Cardoso-Ortiz
Keyword(s):  
Biological Activity ◽  
Heterogeneous Catalysts ◽  
Raw Materials ◽  
Antioxidant Properties ◽  
Clinical Importance ◽  
Azide Group ◽  
Organic Azides ◽  
Recent Developments ◽  
Synthetic Routes ◽  
Tetrazole Derivatives

Abstract:: The heterocycle ring tetrazole is an important moiety relevant to medicinal chemistry since it is present in some drugs with clinical importance. Its primary biological activity is being a bioisosteric analogue of the carboxylic acid and cisamide groups. Its metabolic stability and other physicochemical properties make it an attractive structure for designing and synthesizing new pharmaceuticals. The biological activity of tetrazoles is quite extensive and includes antiviral, antibacterial, anticancer, antifungal, and antioxidant properties; all of them are discussed in this review. The most effective way to obtain tetrazoles is by azide derivatives, either in the starting materials like the cycloaddition [3 + 2] of organic azides and nitriles or by preparing a reactive imidoyl azide intermediate. The nucleophilic behavior of the azide group is discussed when the raw materials include isocyanides. Some other methods include alternative synthetic routes like thermoslysis. This review also highlights some of the developments regarding the use of different heterogeneous catalysts to synthesize different tetrazole derivatives.

Synthesis of α-exo-Methylene-γ-butyrolactone: Recent Developments and Applications in Natural Product Synthesis

Synthesis ◽  
2021 ◽  
Author(s):  
Weilong Liu ◽  
Nicolas Winssinger
Keyword(s):  
Natural Products ◽  
Biological Activity ◽  
Total Synthesis ◽  
Natural Product ◽  
Natural Product Synthesis ◽  
Vast Array ◽  
The Past ◽  
New Approaches ◽  
Recent Developments

The α-exo-methylene-γ-butyrolactone moiety is present in a vast array of structurally diverse natural products and is often central to their biological activity. In this review, we summarize new approaches to α-exo-methylene-γ-butyrolactones developed over the past decade as well as their applications in total synthesis.

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