Synthesis of amino juglone derivatives with adjuvant activity against clinical isolated methicillin-resistant staphylococcus aureus strains.

1,4-naphthoquinones hydroxyderivatives belong to an important class of natural products and have been known as a favored scaffold in medicinal chemistry due to their multiple biological properties. Juglone is one of the most important 1,4-naphthoquinone extracted from juglandaceae family showing a good antibacterial activity. In this study, we report the synthesis of aminojuglone derivatives through Michael addition reaction using Cerium (III) chloride heptahydrate (CeCl·7HO) as catalyst.

Synergistic effect of tryptamine-urea derivatives to overcome the chromosomally-mediated colistin resistance in Klebsiella pneumoniae.

Colistin is considered as the last-resort antibiotics to treat multi-drug resistant Gram-negative bacterial infections in humans. However, the clinical use of colistin was limited because of the apparition of chromosomal mutations and mobile colistin resistance genes in bacterial isolates. One promising strategy is to combine existing antibiotics with promising non-antibiotics to overcome the widespread emergence of antibiotic-resistant pathogens.

Antibacterial Activity and Untargeted Metabolomics Profiling of Poepp.

The search for potent antimicrobial compounds is critical in the face of growing antibiotic resistance. This study explores Poepp. (), a Caribbean plant traditionally used for disease treatment.

Isolation and Identification of Flavones Responsible for the Antibacterial Activities of Extracts.

Plants are an everlasting inspiration source of biologically active compounds. Among these medicinal plants, the biological activity of extracts from some species of the genus has been studied, but the phytochemistry of the hardy species remains unknown. The aim of the present study was to perform the first phytochemical study of and to identify the compounds responsible for the antibacterial activity of extracts.

Extraction and Identification of Volatile Organic Compounds in Scentless Flowers of 14 Species Using HS-SPME/GC-MS.

VOCs emitted by flowers play an important role in plant ecology. In the past few years, the genus has been scarcely studied according to the VOCs emitted by flowers. Hence, we decided to enlarge the VOCs composition study already undergone in our laboratory on fragrant 3 species to 12 unscented and 2 faint-scented species and hybrids.

Catalyst-Free Site Selective Hydroxyalkylation of 5-Phenylthiophen-2-amine with α-Trifluoromethyl Ketones through Electrophilic Aromatic Substitution.

An original and effective approach for achieving trifluoromethyl hydroxyalkylation of 5-phenylthiophen-2-amine using α-trifluoromethyl ketones is described. In the last few years, reaction of Friedel-Crafts had been widely used to realize hydroxyalkylation on heterocycles such as indoles or thiophenes by means of Lewis acid as catalyst. Additionally, amine functions are rarely free when carbonyl reagents are used because of their tendency to form imines.

Synthesis, Structure Elucidation, Antibacterial Activities, and Synergistic Effects of Novel Juglone and Naphthazarin Derivatives Against Clinical Methicillin-Resistant Strains.

Infections caused by drug-resistant bacteria are a serious threat to human and global public health. Moreover, in recent years, very few antibiotics have been discovered and developed by pharmaceutical companies. Therefore, there is an urgent need to discover and develop new antibacterial agents to combat multidrug-resistant bacteria.

Development of a HS-SPME/GC-MS Method for the Extraction and Identification of the Volatile Compounds Emitted by Flowers of .

is a genus belonging to the Bromeliaceae family, most of which are epiphytes. The flowers of some of the species are very fragrant, but the volatile composition has been scarcely reported. In this report, we studied the chemical composition of volatile compounds emitted by the flowers of using the HS-SPME/GC-MS method.

Critical parameters in surface plasmon resonance biosensor development: The interaction between estrogen receptor and estrogen response element as model.

Estrogenic compounds are contaminants that may be active at low concentrations and are a major concern for environmental quality. They interact with organisms via Estrogen Receptors (ER). Some detection methods which have been developed use the ability of ER to interact with short consensus DNA sequences known as Estrogen Response Elements (ERE).

Ethynylglycine synthon, a useful precursor for the synthesis of biologically active compounds: an update. Part II: synthetic uses of ethynylglycine synthon.

The ethynylglycine synthon {(R)-2,2-dimethyl-3-(tert-butoxycarbonyl)-4-ethynyl-oxazolidine} is a chiral compound with valuable synthetic interest. An update (covering literature from 2005 to 2017) on the different synthetic utilities is reviewed and discussed.

The Rational Design, Synthesis, and Antimicrobial Properties of Thiophene Derivatives That Inhibit Bacterial Histidine Kinases.

The emergence of multidrug-resistant bacteria emphasizes the urgent need for novel antibacterial compounds targeting unique cellular processes. Two-component signal transduction systems (TCSs) are commonly used by bacteria to couple environmental stimuli to adaptive responses, are absent in mammals, and are embedded in various pathogenic pathways. To attenuate these signaling pathways, we aimed to target the TCS signal transducer histidine kinase (HK) by focusing on their highly conserved adenosine triphosphate-binding domain.

Advances in the synthesis of α-quaternary α-ethynyl α-amino acids.

α-Quaternary α-ethynyl α-amino acids are an important class of non-proteinogenic amino acids that play an important role in the development of peptides and peptidomimetics as therapeutic agents and in the inhibition of enzyme activities. This review provides an overview of the literature concerning synthesis and applications of α-quaternary α-ethynyl α-amino acids covering the period from 1977 to 2015.

Synthesis of 1,4-disubstituted 1,2,3-triazole Derivatives Using Click Chemistry and their Src Kinase Activities.

Background: Tyrosine kinases (TK) are enzymes that catalyze the phosphorylation of tyrosine residues on proteins by the transfer of phosphate moiety of ATP. TK are key regulators of various cell functions, such as cellular growth, proliferation, migration, differentiation, and apoptosis. Src mutations and/or overexpression has been correlated with tumor growth, metastasis, and angiogenesis [4,5].

Ethynylglycine synthon, a useful precursor for the synthesis of biologically active compounds: an update: part I: preparations of ethynylglycine synthon.

The ethynylglycine synthon {(R)-2,2-dimethyl-3-(tert-butoxycarbonyl)-4-ethynyloxazolidine} is a chiral compound with valuable synthetic interest. An update on the different routes for its synthesis is reviewed and discussed.

Impact of biochemical design on estrogen receptor/estrogen response element interaction by surface plasmon resonance technology.

The estrogen receptor (ER) is a transcription factor that binds under 17-β-estradiol (E2) stimulation as homodimer to a short DNA consensus sequence named estrogen response element (ERE). The ER/ERE interaction has been assessed by several research groups through different methodologies notably by surface plasmon resonance (SPR) techniques. The biochemical parameters and conditions (solvent, ER concentration, salt, time and temperature) used to prepare samples before analysis were very different from one study to another.