scholarly journals Thiomonosaccharide Derivatives from D-Mannose

2020 ◽  
Vol 3 (1) ◽  
pp. 28
Author(s):  
Marcos Díaz-Fernández ◽  
M. Soledad Pino-González
Keyword(s):  
Biological Activities ◽  
Cyano Group ◽  
Structural Identification ◽  
Spectroscopic Techniques ◽  
Synthetic Route ◽  
Group A ◽  
Subsequent Cyclization ◽  
Anomeric Carbon ◽  
Sulfur Containing

Sulfur-containing monosaccharide derivatives can be highly valuable for obtaining compounds with biological activities. In this work, a synthetic route starting from D-mannose has been designed. After a convenient hydroxyl protection and anomeric carbon functionalization in a cyano group, a new carbohydrate analogue has been obtained with sulfur in the ring. The heteroatoms have been introduced by an SN2 mechanism, with subsequent cyclization. Structural identification has been performed by different spectroscopic techniques.

Chalcones: As potent α-amylase enzyme inhibitors; synthesis, in vitro, and in silico studies

2020 ◽  
Vol 16 ◽  
Author(s):  
Mahboob Ali ◽  
Momin Khan ◽  
Khair Zaman ◽  
Abdul Wadood ◽  
Maryam Iqbal ◽  
...  
Keyword(s):  
In Silico ◽  
Enzyme Inhibitors ◽  
Biological Activities ◽  
Condensation Reaction ◽  
Type Ii Diabetes Mellitus ◽  
Spectroscopic Techniques ◽  
Chalcone Derivatives ◽  
In Silico Studies ◽  
Wide Range

: Background: The inhibition of α-amylase enzyme is one of the best therapeutic approach for the management of type II diabetes mellitus. Chalcone possesses a wide range of biological activities. Objective: In the current study chalcone derivatives (1-17) were synthesized and evaluated their inhibitory potential against α-amylase enzyme. Method: For that purpose, a library of substituted (E)-1-(naphthalene-2-yl)-3-phenylprop-2-en-1-ones was synthesized by ClaisenSchmidt condensation reaction of 2-acetonaphthanone and substituted aryl benzaldehyde in the presence of base and characterized via different spectroscopic techniques such as EI-MS, HREI-MS, 1H-, and 13C-NMR. Results: Sixteen synthetic chalcones were evaluated for in vitro porcine pancreatic α-amylase inhibition. All the chalcones demonstrated good inhibitory activities in the range of IC50 = 1.25 ± 1.05 to 2.40 ± 0.09 μM as compared to the standard commercial drug acarbose (IC50 = 1.34 ± 0.3 μM). Conclusion: Chalcone derivatives (1-17) were synthesized, characterized, and evaluated for their α-amylase inhibition. SAR revealed that electron donating groups in the phenyl ring have more influence on enzyme inhibition. However, to insight the participation of different substituents in the chalcones on the binding interactions with the α-amylase enzyme, in silico (computer simulation) molecular modeling analyses were carried out.

scholarly journals Steroid Glycosides Hyrcanoside and Deglucohyrcanoside: On Isolation, Structural Identification, and Anticancer Activity

Foods ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 136
Author(s):  
Silvie Rimpelová ◽  
Tomáš Zimmermann ◽  
Pavel B. Drašar ◽  
Bohumil Dolenský ◽  
Jiří Bejček ◽  
...  
Keyword(s):  
Drug Repositioning ◽  
Biological Activities ◽  
Cancer Therapeutics ◽  
Structural Identification ◽  
Induce Cell Cycle Arrest ◽  
Cycle Arrest ◽  
Steroid Glycosides ◽  
In Silico Modeling ◽  
M Phase ◽  
Atpase Inhibition

Cardiac glycosides (CGs) represent a group of sundry compounds of natural origin. Most CGs are potent inhibitors of Na+/K+-ATPase, and some are routinely utilized in the treatment of various cardiac conditions. Biological activities of other lesser known CGs have not been fully explored yet. Interestingly, the anticancer potential of some CGs was revealed and thereby, some of these compounds are now being evaluated for drug repositioning. However, high systemic toxicity and low cancer cell selectivity of the clinically used CGs have severely limited their utilization in cancer treatment so far. Therefore, in this study, we have focused on two poorly described CGs: hyrcanoside and deglucohyrcanoside. We elaborated on their isolation, structural identification, and cytotoxicity evaluation in a panel of cancerous and noncancerous cell lines, and on their potential to induce cell cycle arrest in the G2/M phase. The activity of hyrcanoside and deglucohyrcanoside was compared to three other CGs: ouabain, digitoxin, and cymarin. Furthermore, by in silico modeling, interaction of these CGs with Na+/K+-ATPase was also studied. Hopefully, these compounds could serve not only as a research tool for Na+/K+-ATPase inhibition, but also as novel cancer therapeutics.

scholarly journals Sulfated and Sulfur-Containing Steroids and Their Pharmacological Profile

Marine Drugs ◽  
2021 ◽  
Vol 19 (5) ◽  
pp. 240
Author(s):  
Tatyana A. Pounina ◽  
Tatyana A. Gloriozova ◽  
Nick Savidov ◽  
Valery M. Dembitsky
Keyword(s):  
Antitumor Activity ◽  
Confidence Level ◽  
Biological Activities ◽  
Marine Sponges ◽  
Bioactive Lipids ◽  
Pharmacological Profile ◽  
Wide Range ◽  
Sulfated Steroids ◽  
Strong Antitumor Activity ◽  
Sulfur Containing

The review focuses on sulfated steroids that have been isolated from seaweeds, marine sponges, soft corals, ascidians, starfish, and other marine invertebrates. Sulfur-containing steroids and triterpenoids are sourced from sedentary marine coelenterates, plants, marine sediments, crude oil, and other geological deposits. The review presents the pharmacological profile of sulfated steroids, sulfur-containing steroids, and triterpenoids, which is based on data obtained using the PASS program. In addition, several semi-synthetic and synthetic epithio steroids, which represent a rare group of bioactive lipids that have not yet been found in nature, but possess a high level of antitumor activity, were included in this review for the comparative pharmacological characterization of this class of compounds. About 140 steroids and triterpenoids are presented in this review, which demonstrate a wide range of biological activities. Therefore, out of 71 sulfated steroids, thirteen show strong antitumor activity with a confidence level of more than 90%, out of 50 sulfur-containing steroids, only four show strong antitumor activity with a confidence level of more than 93%, and out of eighteen epithio steroids, thirteen steroids show strong antitumor activity with a confidence level of 91% to 97.4%.

scholarly journals Non-Nucleoside Agonists of the Adenosine Receptors: An Overview

2019 ◽  
Vol 12 (4) ◽  
pp. 150 ◽  
Author(s):  
Dal Ben ◽  
Lambertucci ◽  
Buccioni ◽  
Martí Navia ◽  
Marucci ◽  
...  
Keyword(s):  
Adenosine Receptors ◽  
Biological Activities ◽  
Great Majority ◽  
Synthetic Route ◽  
Wide Range ◽  
Pharmacological Interest ◽  
Molecular Modeling Studies ◽  
Synthetic Routes ◽  
Alternative Set ◽  
Structural Classes

Potent and selective adenosine receptor (AR) agonists are of pharmacological interest for the treatment of a wide range of diseases and conditions. Among these derivatives, nucleoside-based agonists represent the great majority of molecules developed and reported to date. However, the limited availability of compounds selective for a specific AR subtype (i.e., A2BAR) and a generally long and complex synthetic route for largely substituted nucleosides are the main drawbacks of this category of molecules. Non-nucleoside agonists represent an alternative set of compounds able to stimulate the AR function and based on simplified structures. This review provides an updated overview on the structural classes of non-nucleoside AR agonists and their biological activities, with emphasis on the main derivatives reported in the literature. A focus is also given to the synthetic routes employed to develop these derivatives and on molecular modeling studies simulating their interaction with ARs.

Carbohydrazide analogues: a review of synthesis and biological activities

2021 ◽  
Vol 21 ◽  
Author(s):  
Ebuka Leonard Onyeyilim ◽  
Mercy Amarachi Ezeokonkwo ◽  
David Izuchukwu Ugwu ◽  
Chiamaka Peace Uzoewulu ◽  
Florence Uchenna Eze ◽  
...  
Keyword(s):  
Organic Chemistry ◽  
Inorganic Chemistry ◽  
Schiff Bases ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Important Class ◽  
Synthetic Route ◽  
Structure Activity

: Carbohydrazides and their Schiff bases are important class of heterocycles that are not only employed in the area of organic chemistry, but also have tremendous applications in physical and inorganic chemistry. A series of potential bioactive compounds, containing carbohydrazide functionality and their hydrazone derivatives have been synthesized and screened for antibacterial, anticancer, antifungal and anti-inflammatory etc. This brief review discloses some synthetic route to so many reported carbohydrazides, their Schiff bases, their biological activities and their structure activity relationship.

scholarly journals A New Bioactive Steroidal Saponin from Leaves of Furcraea gigantea

2006 ◽  
Vol 61 (9) ◽  
pp. 1153-1157 ◽  
Author(s):  
Bernadete P. da Silva ◽  
José P. Parente
Keyword(s):  
Nmr Spectra ◽  
Capillary Permeability ◽  
Structural Identification ◽  
2D Nmr ◽  
In Vitro Assays ◽  
Steroidal Saponin ◽  
Spectroscopic Techniques ◽  
C Nmr

Abstract A new bidesmosidic furostanol saponin was isolated from leaves of Furcraea gigantea Vent. Its structure was established as 3-[(O-6-deoxy-α-L-mannopyranosyl-(1→4)-O-β -D-glucopyranosyl-( 1→3)-O-[O-β -D-glucopyranosyl-(1→3)-β -D-glucopyranosyl-(1→2)-O-β -D-glucopyranosyl- (1→4)-β -D-galactopyranosyl)oxy]-(3β ,5α,15α,22α,25R)-26-(β -D-glucopyranosyloxy)-15,22-dihydroxy- furost-12-one. Its structural identification was performed using detailed analyses of 1H and 13C NMR spectra including 2D NMR spectroscopic techniques (DEPT, COSY, HETCOR and COLOC) and chemical conversions. The steroidal saponin showed no haemolytic effects in the in vitro assays and demonstrated inhibition of the capillary permeability activity.

scholarly journals Novel 5,6-Dihydropyrrolo[2,1-a]isoquinolines as Scaffolds for Synthesis of Lamellarin Analogues

2011 ◽  
Vol 2011 ◽  
pp. 1-6 ◽  
Author(s):  
Shao Han Liao ◽  
Dai Hua Hu ◽  
Ai Ling Wang ◽  
De Peng Li
Keyword(s):  
Melting Point ◽  
Ir Spectrum ◽  
Biological Activities ◽  
Synthetic Route ◽  
H Nmr ◽  
C Nmr

As core skeletons of lamellarins: 5,6-Dihydropyrrolo[2,1-a]isoquinolines are one of the important alkaloids that exhibit significant biological activities, in this study, an efficient synthetic route was described for two novel compounds, 5,6-dihydropyrrolo[2,1-a]isoquinolinesIandII. CompoundIwas synthesized from isovanillin with 28.3% overall yield by a six-step reaction whileIIfrom 2-(3,4-dimethoxyphenyl) ethanamine was with 61.6% overall yield by a three-step reaction. And the structures of these two compounds were confirmed by means of IR spectrum,1H NMR,13C NMR, MS, HRMS, and melting point measurements.

scholarly journals Synthesis, spectral characterization and biological activities of Ag(I), Pt(IV) and Au(III) complexes with novel azo dye ligand (N,N,O) derived from 2-amino-6-methoxy benzothiazole

2022 ◽  
Author(s):  
Hussein A. K. Kyhoiesh ◽  
Khalid J. Al-Adilee
Keyword(s):  
Crystal Structure ◽  
Endometrial Cancer ◽  
Nitrogen Atom ◽  
Metal Complexes ◽  
Cancer Cells ◽  
Azo Dye ◽  
Biological Activities ◽  
Antifungal Drugs ◽  
Azo Compounds ◽  
Spectroscopic Techniques

Abstract The novel ligand 2-[2'-(6-methoxybenzothiazolyl)azo]-3,5-dimethyl benzoic acid (6-MBTAMB), derived from 2-amino-6-methoxy benzothiazole, has been used to synthesize a series of new metal complexes of Ag(I), Pt(IV) and Au(III). The metal complexes were characterized by elemental analyses (CHNS), molar conductivity, crystal structure (XRD), spectroscopic techniques: FT-IR, 1H NMR, 13C NMR, UV-Vis, mass spectra, thermal analysis (TG-DTA), FE-SEM and magnetic properties. Results confirmed that the azo dye ligand behaves a tridentate and coordinates to the metal ion via nitrogen atom of azomethine group of heterocyclic benzothiazole ring, nitrogen atom of the azo group which is the farthest of the benzothiazole molecule and carboxylic oxygen. Antimicrobial properties of all newly synthesized azo compounds are also demonstrated against bacterial pathogenic organisms and fungi. These complexes are more effective against bacteria and less effective against fungi compared to standard antibacterial drugs (Novobiocin) and antifungal drugs (Cycloheximide). By using the DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging test, it was discovered that the complexes had good antioxidant properties. In addition, the (6-MBTAMB) and metal complexes were docked with the crystal structure of FGF Receptor 2 (FGFR2) kinase domain harboring the pathogenic gain of function K659E mutation identified in endometrial cancer using the Molecular Operating Environment module (MOE). In vitro studies on human endometrial cancer cell lines (MFE-296) as well as healthy human umbilical vein endothelial cells (HUVEC) show uptake of the intact compounds by the cancer cells and increased activity against the cancer cells.

scholarly journals Synthesis of substituted pyridine based sulphonamides as an antidiabetic agent

2021 ◽  
Vol 12 (3) ◽  
pp. 279-283
Author(s):  
Gautam Sadawarte ◽  
Samadhan Jagatap ◽  
Mukesh Patil ◽  
Vasant Jagrut ◽  
Jamatsing Darbarsing Rajput
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Research Work ◽  
Synthetic Methods ◽  
Alpha Amylase ◽  
Spectroscopic Techniques ◽  
Inhibition Activity ◽  
Antidiabetic Agent ◽  
Biological Functions ◽  
Ir Spectroscopic

This research work describes the synthesis of a new series of heterocyclic compounds, namely sulfonamide derivatives. Sulfonamides are a diverse class of organic compounds having significant and potent biological activities. Diverse synthetic methods have been engaged to build up its various derivatives for different biological functions. In this study, the production of novel pyridine-based heterocyclic compounds having sulfonamide moieties has been elaborated. The obtained sulfonamide-based pyridine scaffold was used to investigate their alpha-amylase inhibition activity. The structures of freshly prepared compounds were described using 1H NMR, 13C NMR, and IR spectroscopic techniques. The molecular docking of sulfonamides performed against porcine pancreatic alpha-amylase using PDB file 1LP was used for generation of grid. All the new synthesized compounds were shown notable anti-diabetic activity.

scholarly journals Synthesis, Characterization and Study of Antimicrobial Activities of Mannich Bases Incorporating 1,2,4-Triazole Nucleus

2021 ◽  
Vol 2 (01) ◽  
pp. 19-27
Author(s):  
Rhambus Rawat ◽  
Prem Shankar Deo ◽  
Bhushan Shakya
Keyword(s):  
Schiff Base ◽  
Heterocyclic Compounds ◽  
Environmental Science ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Mannich Bases ◽  
New Drugs ◽  
Spectroscopic Techniques ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

Heterocyclic compounds containing triazole moiety have great importance in the field of medicine, pharmaceuticals, biochemistry, biology, therapeutics, environmental science, and industry. Triazoles and their derivatives have been extensively used in the development of new drugs. Biological activities of Schiff bases are highly investigated, but Mannich bases are on the verge of their development, and they are being synthesized in large number nowadays. In this work, Mannich bases are synthesized by incorporation 1,2,4-triazole moiety through Schiff base using different amines. Mannich bases are found to exhibit highly effective antibacterial and antifungal activities. The formation of synthesized compounds - 1,2,4-triazole-5-thione, Schiff base (4) and Mannich bases (5a and 5b) - are confirmed and characterized by spectroscopic techniques like UV, FTIR 1H-NMR and 13C-NMR. The activity of the synthesized compounds was tested against bacterial and fungal strain.

Sign in / Sign up

Export Citation Format

Share Document