Improvement of humic acid (HA) removal using a new inorganic-organic composite coagulant: α-costic acid as a modifier of polyaluminum chloride properties.

In this work, α-costic acid (αCA), a plant sesquiterpenoid from Dittrichia viscosa, was grafted into polyaluminum chloride (PAC), forming a new eco-sustainable composite coagulant PAC-αCA with improved functionality. The α-costic acid fraction grafted into the PAC and the distribution of aluminum forms in the composite coagulant were evaluated for their effectiveness in removing bentonite and humic acid from synthetic water. The interaction mechanism between PAC and α-CA was examined by the Al-Ferron time spectrophotometric method, density functional theory (DFT), and FTIR analysis.

Access and Modulation of Substituted Pyrrolo[3,4-]pyrazole-4,6-(2,5)-diones.

The first access to polyfunctionnalized pyrrolo[3,4-]pyrazole-4,6-(2,5)-dione derivatives is reported. The series were generated from diethyl acetylenedicarboxylate and arylhydrazines, which afforded the key intermediates bearing two functional positions. The annellation to generate the maleimide moiety of the bicycle was studied.

Efficient Synthesis of 1-Benzo[4,5]imidazo[1,2-][1,3]oxazin-1-one Derivatives Using AgCO/TFA-Catalyzed 6- Cyclization: Reaction Scope and Mechanistic Study.

A small library of 1-benzo[4,5]imidazo[1,2-][1,3]oxazin-1-one derivatives was prepared in good to excellent yields, involving a AgCO/TFA-catalyzed intramolecular oxacyclization of -2-alkynylbenzimidazole substrates. In all experiments, the 6-- cyclization was exclusively achieved since the possible heterocycle was not observed, indicating the high regioselectivity of this process. The scope and limitations of the silver catalyzed cyclization of --2-alkynylbenzimidazoles as substrates, bearing various substituents, were investigated.

D-π-A-Type Pyrazolo[1,5-]pyrimidine-Based Hole-Transporting Materials for Perovskite Solar Cells: Effect of the Functionalization Position.

Donor−acceptor (D−A) small molecules are regarded as promising hole-transporting materials for perovskite solar cells (PSCs) due to their tunable optoelectronic properties. This paper reports the design, synthesis and characterization of three novel isomeric D-π-A small molecules PY1, PY2 and PY3. The chemical structures of the molecules consist of a pyrazolo[1,5-a]pyrimidine acceptor core functionalized with one 3,6-bis(4,4′-dimethoxydiphenylamino)carbazole (3,6-CzDMPA) donor moiety via a phenyl π-spacer at the 3, 5 and 7 positions, respectively.

A simple synthesis of α-Costic acid analogue with antibacterial potential, DFT and molecular docking.

Natural products extracted from plants has been recognized as the most efficient starting materials to synthesize new derivatives of medicinal interest. Our research focuses on the isolation and characterization of sesquiterpene derivatives from , as well as their hemisynthesis. To that end, a phytochemical study of leaves was conducted in order to obtain a sesquiterpenoid, α -Costic acid, which will be further transformed to γ -Costic acid with high yield using simple processes.

Molecular Characterization of Gene-Mediated Resistance and Susceptibility of ESKAPE Clinical Isolates to L. and L. Extracts.

Background: Multidrug resistance (MDR) and extensively drug-resistant (XDR) are now the biggest threats to human beings. Alternative antimicrobial regimens to conventional antibiotic paradigms are extensively searched. Although extracts have long been used for infections in traditional folk medicines around the world, their efficacy against resistant bacteria still needs to be elucidated.

Antifungal and Cytotoxic Activity of Diterpenes and Bisnorsesquiterpenoides from the Latex of Berg.

latex has been extensively utilized in traditional medicine due to its range of bioactivities. Chromatographic separations on silica gel of ethanol extract of latex led to the development of a new procedure for isolating resiniferatoxin () via dried latex and the identification of nine compounds. Among these, catechol (), protocatechuic acid () and 3,4-dihydroxyphenylacetic acid (), known phenolic compounds, were identified for the first time in latex.

Design, Synthesis, and Biological Evaluation of Novel Tomentosin Derivatives in NMDA-Induced Excitotoxicity.

N-methyl-D-aspartate (NMDA) receptor stimulation may lead to excitotoxicity, which triggers neuronal death in brain disorders. In addition to current clinical therapeutic approaches, treatment strategies by phytochemicals or their derivatives are under investigation for neurodegenerative diseases. In the present study, novel amino and 1,2,3-triazole derivatives of tomentosin were prepared and tested for their protective and anti-apoptotic effects in NMDA-induced excitotoxicity.

Near-Infrared Emitting Poly(amidoamine) Dendrimers with an Anthraquinone Core toward Versatile Non-Invasive Biological Imaging.

Today, there is a very strong demand for versatile near-infrared (NIR) imaging agents suitable for non-invasive optical imaging in living organisms ( imaging). Here, we created a family of NIR-emitting macromolecules that take advantage of the unique structure of dendrimers. In contrast to existing fluorescent dendrimers bearing fluorophores at their periphery or in their cavities, a NIR fluorescent structure is incorporated into the core of the dendrimer.

A AgCO/TFA-catalyzed intramolecular annulation approach to imidazo[1,2-][1,3]oxazin-5-one derivatives.

A series of 2,7-disubstituted 3-methylimidazo[1,2-][1,3]oxazin-5-ones were synthesized in good yields AgCO/TFA-mediated intramolecular annulation of -Boc-2-alkynyl-4-bromo(alkynyl)-5-methylimidazoles. This methodology was carried out in the presence of a catalytic amount of silver carbonate and trifluoroacetic acid in dichloroethane at 60 °C. In all experiments, only the six-membered ring product was obtained since the possible five-membered compound was not observed, proving the high regioselectivity of this approach.

Chemical composition, antibacterial, antioxidant and insecticidal activities of moroccan essential oil.

Introduction: The use of chemical products to neutralize microorganisms has always been a subject of discussion and research for alternative solutions, indeed, the use of essential oils has been a promising natural methodology.

Methods: In our study we used the essential oils from different parts of (Apiaceae), obtained by hydrodistillation, were identified and using Gas chromatography-mass spectrometry (GC-MS) and Gas Chromatography-Flame Ionization Detection (GC/FID) methods and evaluated against several bacteria of Gram- and Gram + bacteria. Disk diffusion, Minimum Inhibitory Concentration (MIC) and Minimum Microbicidal Concentration (MMC) methods have been used.

A Review on sp.: Phytochemical and Antimicrobial Activities.

Resistance to drugs is reaching alarming levels and is placing human health at risk. With the lack of new antimicrobials drugs, infectious diseases are becoming harder to treat. Hence, there is an increasing awareness of active phytochemicals with therapeutic functions.

Design, synthesis, and evaluation of cytotoxic activities of arylnaphthalene lignans and aza-analogs.

A concise and versatile synthetic strategy for the total synthesis of arylnaphthalene lignans and aza-analogs was developed. The main objective was to develop synthetic tactics for the creation of the lactone and lactam unit that would give access to an array of synthetic, natural, and/or bioactive compounds through rather simple chemical manipulation. The flexibility and potentiality of these new processes were further illustrated by the total synthesis of retrojusticidin B (13b), justicidin C (14b), and methoxy-vitedoamine A (22a).

A regioselective C7 bromination and C7 palladium-catalyzed Suzuki-Miyaura cross-coupling arylation of 4-substituted NH-free indazoles.

A direct and efficient regioselective C7-bromination of 4-substituted 1-indazole has been achieved. Subsequently, a successful palladium-mediated Suzuki-Miyaura reaction of C7-bromo-4-substituted-1-indazoles with boronic acids has been performed under optimized reaction conditions. A series of new C7 arylated 4-substituted 1-indazoles was obtained in moderate to good yields.

Efficient microwave-assisted Suzuki-Miyaura cross-coupling reaction of 3-bromo pyrazolo[1,5-]pyrimidin-5(4)-one: towards a new access to 3,5-diarylated 7-(trifluoromethyl)pyrazolo[1,5-]pyrimidine derivatives.

A convenient and efficient synthetic route to C3-arylated 7-trifluoromethylpyrazolo[1,5-]pyrimidin-5-one derivatives has been reported starting from 3-bromo-7-(trifluoromethyl)pyrazolo[1,5-]pyrimidin-5-one through a Suzuki-Miyaura cross-coupling reaction. The arylation (heteroarylation) strategy can be performed using a wide variety of aryl and heteroaryl boronic acids and requiring a tandem catalyst XPhosPdG2/XPhos to avoid the debromination reaction. These optimized conditions were successfully extended to the synthesis of 7-, 8- and 9-arylated pyrimido[1,2-]indazol-2-ones from their corresponding brominated starting materials.

Valorization of Pads and Steel Industry FeCl-Rich Rejection for Removing Surfactant and Phenol from Oil Refinery Wastewater Through Coagulation-Flocculation.

Background: Refinement of crude vegetable oil generates a large amount of wastewater and is a source of water pollution due to the presence of surfactants and phenols. Phenols are toxic aromatic compounds that can be lethal to fauna and flora, entraining the deceleration or blocking of the self-purification of biological treatments. In addition, surfactants can limit biological processes by inhibiting microorganisms that degrade organic matter.

"On Water" Palladium Catalyzed Direct Arylation of 1Indazole and 1-7-Azaindazole.

The C3 direct arylation of 1-indazole and 1-7-azaindazole has been a significant challenge due to the lack of the reactivity at this position. In this paper, we describe a mild and an efficient synthesis of new series of C3-aryled 1-indazoles and C3-aryled 1-7-azaindazoles via a C3 direct arylation using water as solvent. On water, PPh was effective as a ligand along with a lower charge of the catalyst Pd(OAc) (5 mol%) at 100 °C, leading to C3-aryled 1-indazoles or C3-aryled 1-7-azaindazoles in moderate to good yields.

Efficient Access to 3,5-Disubstituted 7-(Trifluoromethyl)pyrazolo[1,5-]pyrimidines Involving SAr and Suzuki Cross-Coupling Reactions.

An efficient and original synthesis of various 3,5-disubstituted 7-(trifluoromethyl)pyrazolo[1,5-]pyrimidines is reported. A library of compounds diversely substituted in C-3 and C-5 positions was easily prepared from a common starting material, 3-bromo-7-(trifluoromethyl)pyrazolo[1,5-]pyrimidin-5-one. In C-5 position, a SAr type reaction was achieved by first activating the C-O bond of the lactam function with PyBroP (Bromotripyrrolidinophosphonium hexafluorophosphate), followed by the addition of amine or thiol giving monosubstituted derivatives, whereas in C-3 position, arylation was performed via Suzuki-Miyaura cross-coupling using the commercially available aromatic and heteroaromatic boronic acids.

Synthesis and Biological Evaluation of New Naphthoquinones Derivatives.

Unlabelled: New substituted 1,4-naphthoquinones have been prepared in good overall yields through the naphthol route. The cytotoxicity of these compounds was tested in vitro on MCF-7 breast tumor cells. The most active compound 14 displayed an IC50 of 15μM.

Unusual rearrangement of imidazo[1,5-]imidazoles and imidazo[1,2-]pyrazoles into imidazo[1,5-]pyrimidines and pyrazolo[1,5-]pyrimidines.

A multicomponent reaction giving easy and cheap access to a variety of bicyclic 5,5-fused hetero-rings has been developed. Then, an usual rearrangement of imidazo[1,5-]imidazoles or imidazo[1,2-]pyrazoles leading to bi-heterocyclic imidazo- and pyrazolo[1,5-]pyrimidines in the presence of a specific amount of I in THF at room temperature has been achieved. This new method enables the hitherto unreported synthesis of functionalized imidazo- and pyrazolo[1,5-]pyrimidines.

Regioselective Synthesis of New 2,4-(Het)aryl-3H-pyrido[1',2':1,5]pyrazolo[4,3-d]pyrimidines Involving Palladium-Catalyzed Cross-Coupling Reactions.

The design of some novel di-(het)arylated-3-pyrido[1',2':1,5]pyrazolo[4,3-]pyrimidine derivatives is reported. The series was developed from 1-aminopyridinium iodide, which afforded the key intermediate bearing two thiomethyl and amide functions, each of them useful for palladium catalyzed cross coupling reactions by alkyl sulfur release and C-O activation, respectively. The two regioselective and successive cross-coupling reactions were first carried out in C-4 by in situ C-O activation and next in C-2 by a methylsulfur release.

Efficient synthesis and first regioselective C-6 direct arylation of imidazo[2,1-c][1,2,4]triazine scaffold and their evaluation in HO-induced oxidative stress.

Oxidative stress and apoptosis are both associated with various acute and chronic disorders. Thus, the aim of the present study is to synthesize imidazo[2,1-c][1,2,4]triazines derivatives and to evaluate their effects in HO-induced oxidative stress in human neuroblastoma cell line (SH-SY5Y cells). The effects of the compounds on cell viability were measured by MTT assay and the changes in stress and apoptosis-related proteins were investigated by PathScan Stress and Apoptosis Signaling Antibody Array kit and Western Blot technique.

Three successive and regiocontroled palladium cross-coupling reactions to easily synthesize novel series of 2,4,6-tris(het)aryl pyrido[1',2':1,5]pyrazolo[3,4-]pyrimidines.

The first access to tris(het)arylated pyrido[1',2':1,5]pyrazolo[3,4-]pyrimidine derivatives is reported. The series were generated from 4-chloroaminopyridinium, which afforded the key intermediate bearing three leaving groups, a C-2 methylsulfanyl, a lactame carbonyl group in C-4 and a chlorine atom in C-6. The regioselective reactions led to the tris(het)aryl derivatives with satisfying to high yields.

Modification of Natural Eudesmane Scaffolds via Mizoroki-Heck Reactions.

The Mizoroki-Heck reaction was applied to substrates derived from isocostic and ilicic acids, important sesquiterpene components of L. Greuter that were extracted directly from plant material collected in Morocco. After optimization of the metallo-catalysis conditions, various aryl-groups were successfully introduced on the exocyclic double bond with an exclusive -configuration and without racemization.

Synthetic Modification of 9α- and 9β-Hydroxyparthenolide by Heck or Acylation Reactions and Evaluation of Cytotoxic Activities.

Motivated by the widely reported anticancer activity of parthenolides and their derivatives, a series of new substituted parthenolides was efficiently synthesized. Structural modifications were performed at the C-9 and C-13 positions of 9- and 9-hydroxyparthenolide, which were isolated from the aerial parts of . Twenty-one derivatives were synthesized and evaluated for their cytotoxic activity against HS-683, SK-MEL-28, A549, and MCF-7 human cancer cell lines using the MTT colorimetric assay.