Search results for "DISCOVERY"
showing 10 items of 4119 documents
Chemical and antifungal investigations of six Lippia species (Verbenaceae) from Brazil
2012
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Bioactive Steroidal Saponins from Smilax medica
2006
Two new spirostanol saponins ( 1 and 2) were isolated from the roots of Smilax medica, together with the known smilagenin 3-O-beta-D-glucopyranoside (3). Their structures were determined by spectroscopic methods including 1D- and 2D-NMR experiments. Compounds 1 and 2 exhibited antifungal activity against the human pathogenic yeasts Candida albicans, C. glabrata and C. tropicalis (MICs between 6.25 and 50 microg/mL) whereas 3 was inactive.
Recent Trends in the Pharmacological Activity of Isoprenyl Phenolics
2012
Abstract A number of prenylated phenols, mainly flavonoids, have been identified as active constituents of medicinal plants. Due to their beneficial effects on human health, this class of compounds has received a great deal of attention, not only from the pharmaceutical industry, but also from other areas of applied sciences, including the food, brewing, and cosmetics industries. The addition of prenyl residues through the activity of isoprenyltransferases, the key biosynthetic enzymes for these plant metabolites, endows flavonoids with a variety of biological activities, mostly due to improved interaction with membranes and proteins. The role of prenylated flavonoids in plants correlates w…
DHFR Inhibitors: Reading the Past for Discovering Novel Anticancer Agents.
2019
Dihydrofolate reductase inhibitors are an important class of drugs, as evidenced by their use as antibacterial, antimalarial, antifungal, and anticancer agents. Progress in understanding the biochemical basis of mechanisms responsible for enzyme selectivity and antiproliferative effects has renewed the interest in antifolates for cancer chemotherapy and prompted the medicinal chemistry community to develop novel and selective human DHFR inhibitors, thus leading to a new generation of DHFR inhibitors. This work summarizes the mechanism of action, chemical, and anticancer profile of the DHFR inhibitors discovered in the last six years. New strategies in DHFR drug discovery are also provided, …
Novel isoquinoline derivatives as antimicrobial agents.
2013
The wide variety of potent biological activities of natural and synthetic isoquinoline alkaloids encouraged us to develop novel antimicrobial isoquinoline compounds. We synthesized a variety of differently functionalized 1-pentyl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines (THIQs), including dihydroisoquinolinium salts (2 and 5), methyl pentanoate-THIQ (6), 1-pentanol-THIQ (7), ester derivatives (8-15) and carbamate derivatives (16-23). We employed classic intramolecular Bischler-Napieralski cyclodehydration to generate the isoquinoline core. All the structures were characterized by nuclear magnetic resonance and mass spectrometry. The bactericide and fungicide activities were evaluated f…
Studies on puupehenone-metabolites of a Dysidea sp.: structure and biological activity
2007
[EN] Puupchenone (1) and a series of its congeners (2-6) have been isolated from a Dysidea sponge. The unprecedented 20-acetoxyhater-unnadienone (2) exhibiting a five-membered contracted ring, has been characterized. In addition, stereochemical assignment of two previously reported acetone adducts of puupehenone (5 and 6) has been made. Finally, the inhibition of mitochondrial respiratory chain as well as antibacterial and antifungal activities of all compounds has been evaluated. (c) 2006 Elsevier Ltd. All rights reserved.
QuBiLs-MAS method in early drug discovery and rational drug identification of antifungal agents
2015
The QuBiLs-MAS approach is used for the in silico modelling of the antifungal activity of organic molecules. To this effect, non-stochastic (NS) and simple-stochastic (SS) atom-based quadratic indices are used to codify chemical information for a comprehensive dataset of 2478 compounds having a great structural variability, with 1087 of them being antifungal agents, covering the broadest antifungal mechanisms of action known so far. The NS and SS index-based antifungal activity classification models obtained using linear discriminant analysis (LDA) yield correct classification percentages of 90.73% and 92.47%, respectively, for the training set. Additionally, these models are able to correc…
Steroidal saponins from the roots of Smilax aspera subsp. mauritanica
2008
Two new steroidal saponins (1, 2) were isolated from the roots of Smilax aspera subsp. mauritanica (POIR.) ARCANG. (Liliaceae), together with the known curillin G (3), asparagoside E (4), asparoside A (5), asparoside B (6) and the phenolic compound resveratrol (7). Their structures were established mainly on the basis of 600 MHz 2D-NMR spectral data. 3 exhibited antifungal activity against the human pathogenic yeasts Candida albicans, C. glabrata and C. tropicalis (minimum inhibitory concentrations of 25, 25 and 50 microg/ml, respectively) whereas the other compounds were inactive.
Ag+ Complexes as Potential Therapeutic Agents in Medicine and Pharmacy
2019
Silver is a non-essential element with promising antimicrobial and anticancer properties. This work is a detailed summary of the newest findings on the bioinorganic chemistry of silver, with a special focus on the applications of Ag+ complexes and nanoparticles. The coordination chemistry of silver is given a reasonable amount of attention, summarizing the most common silver binding sites and giving examples of such binding motifs in biologically important proteins. Possible applications of this metal and its complexes in medicine, particularly as antibacterial and antifungal agents and in cancer therapy, are discussed in detail. The most recent data on silver nanoparticles are also summari…
Stilbene-based anticancer agents: Resveratrol analogues active toward HL60 leukemic cells wit a non-specific phase mechanism
2006
Several stilbenes, related to known resveratrol, have been synthesized and tested for their anticancer effect on HL60 leukemia cell line, taking particular care of the cell cycle analysis. The most potent compound was the known (Z)-3,4',5-trimethoxystilbene (6b) which was active as apoptotic agent at 0.24 microM. Differently from other stilbenes (including resveratrol) that induced a prevalent recruitment of cells in S phase of cell cycle, we found a peculiar behavior of 6b that caused a decrease of cells in all phases of cell cycle (G0-G1, S, and G2-M) and a proportional increase of apoptotic cells. The potent pro-apoptotic activity shown by compound 6b and its effects on cell cycle make t…