A visible-light-promoted highly selective and efficient strategy for the trifluoromethyl-thiocyanation of alkenes under transition-metal-, photocatalyst- and additive-free conditions has been ...reported using stable and recyclable Umemoto reagent II as the CF
3
source and inexpensive ammonium thiocyanate as the thiocyanating agent. This economical and environmentally benign protocol is suitable for styrenes, acrylates and unactivated alkenes and delivers various trifluoromethyl-thiocyanates in good to excellent yields. In addition, trifluoromethyl-selenocyanation of alkenes is also demonstrated for the first time using this protocol with potassium selenocyanate.
Photocatalyst- and additive-free trifluoromethyl-thio(seleno)cyanation of alkenes using visible light as the sole promoter is reported.
Coumarin is a benzopyrone which is widely used as an anti-coagulant, anti-oxidant, anti-cancer and also to cure arthritis, herpes, asthma and inflammation. Here, we studied the binding of synthesized ...coumarin derivatives with human serum albumin (HSA) at physiological pH 7.2 by using fluorescence spectroscopy, circular dichroism spectroscopy, molecular docking and molecular dynamics simulation studies. By addition of coumarin derivatives to HSA the maximum fluorescence intensity was reduced due to quenching of intrinsic fluorescence upon binding of coumarin derivatives to HSA. The binding constant and free energy were found to be 1.957±0.01×10(5) M(-1), -7.175 Kcal M(-1) for coumarin derivative (CD) enamide; 0.837±0.01×10(5) M(-1), -6.685 Kcal M(-1) for coumarin derivative (CD) enoate, and 0.606±0.01×10(5) M(-1), -6.49 Kcal M(-1) for coumarin derivative methylprop (CDM) enamide. The CD spectroscopy showed that the protein secondary structure was partially unfolded upon binding of coumarin derivatives. Further, the molecular docking studies showed that coumarin derivatives were binding to HSA at sub-domain IB with the hydrophobic interactions and also with hydrogen bond interactions. Additionally, the molecular dynamics simulations studies contributed in understanding the stability of protein-drug complex system in the aqueous solution and the conformational changes in HSA upon binding of coumarin derivatives. This study will provide insights into designing of the new inspired coumarin derivatives as therapeutic agents against many life threatening diseases.
Celotno besedilo
Dostopno za:
DOBA, IZUM, KILJ, NUK, PILJ, PNG, SAZU, SIK, UILJ, UKNU, UL, UM, UPUK
A new class of bis heterocycles‐benzimidazolyl pyrazoles were prepared from the Michael acceptor (E)‐3‐(1H‐benzimidazol‐2‐yl)‐1‐aryl‐prop‐2‐en‐1‐one. The thiamide group was exploited to develop ...thiazole ring on treatment with p‐fluorophenacyl bromide to get tris heterocycles. All the lead compounds were tested for antimicrobial activity. The compound 7d having nitro substituent on the aromatic ring showed greater antimicrobial activity particularly against Pseudomonas aeruginosa and Penicillium chrysogenum.
New Methods for Synthesis of 1,2,3-Triazoles: A Review Nemallapudi, Bakthavatchala Reddy; Guda, Dinneswara Reddy; Ummadi, Nagarjuna ...
Polycyclic Aromatic Compounds,
07/2022, Letnik:
42, Številka:
6
Book Review, Journal Article
Recenzirano
1,2,3-Triazole is one of a pair of isomeric chemical compounds with molecular formula C
2
H
3
N
3
, called triazoles, which have a five-membered ring of two carbon atoms and three nitrogen atoms. ..."1,2,3-Triazole is a basic aromatic heterocyclic scaffold." Substituted 1,2,3-triazoles can be produced using the azide alkyne Huisgen cycloaddition in which an azide and an alkyne undergo a 1,3-dipolar cycloaddition reaction. "This moiety is also useful in material science because of its structural character." Synthesis of this moiety from the easily available chemicals is desirable due to its tremendous use in the chemistry. Here, we report "a review" on the synthesis of this scaffold employing different strategies.
Celotno besedilo
Dostopno za:
BFBNIB, DOBA, GIS, IJS, IZUM, KILJ, KISLJ, NUK, PILJ, PNG, SAZU, UILJ, UKNU, UL, UM, UPUK
The one-pot, three component and facile synthesis of diethyl ((4-isopropylphenyl) (substitutedphenylamino)methyl)phosphonate
4a
–
4j
has been achieved from the reaction of 4-isopropylbenzaldehyde
1
...with various substituted amines
2a
–
2j
and diethyl phosphite
3
using Kabachnik–Fields reaction under room temperature and solvent free conditions using nano Cu
2
O as a stable, noncorrosive, low-cost, recyclable, eco-friendly heterogeneous catalyst. Furthermore, melting point, IR, NMR, and mass spectra were used to interpret this new series of compounds. The newly synthesized formulations were evaluated
in vitro
for antioxidant and antimicrobial activity, and they executed well when compared to the standard.
Carbazole derivatives are widely used to make highly efficient optoelectronic materials. In this context, we developed a method for synthesizing conjugated carbazole derivatives using bimetallic ...Pd-Cu nanoparticles (NPs) immobilized on reduced graphene oxide (rGO) sheets. Pd-Cu NPs were synthesised in a one-pot wet chemical process with ascorbic acid as the reducing agent. The Pd-Cu NPs have an average diameter of 3.8 ± 1.2 nm. X-ray diffraction, SEM, TEM, EDS, and cyclic voltammetry were used to characterise the structure and morphology of the Pd-Cu@rGO NPs.
N
-Protected-3-aryl/heteroaryl carbazoles were efficiently synthesized using the Pd-Cu@rGO catalyst, which enabled the Suzuki-Miyaura (SM) cross-coupling reaction between
N
-protected-3-bromo-carbazoles and a range of aryl/heteroaryl boronic acids. The prepared compounds were characterized by NMR (
1
H &
13
C) and HRMS spectra. For the SM reaction, the catalytic performance of the monometallic Pd@rGO and bimetallic Pd-Ni@rGO and Pd-Cu@rGO catalysts were studied with various metal loadings. In comparison to the monometallic Pd@rGO and bimetallic Pd-Ni@rGO catalysts, the bimetallic Pd-Cu@rGO heterogeneous catalyst (
L3
) demonstrated improved catalytic performance with yields of up to 98%. The material exhibits excellent recyclability and can be reused up to five times without experiencing any decline in its effectiveness. The electronic structure modification offered by the Pd-Cu ensemble on rGO may be responsible for its higher catalytic efficiency. UV and fluorescence spectra were used to investigate the optoelectronic properties of the produced carbazole compounds. Among the compounds studied,
5f
,
5n
, and
5h
exhibited superior UV absorption and fluorescence emission due to the presence of auxochromes and extended conjugation. This study explores the efficacies of the reduced graphene oxide-supported Pd-Cu bimetallic system with different weight% for milder SM reactions.
Different wt% of Pd@rGO, Pd-Cu@rGO and Pd-Ni@rGO catalysts were prepared from a one-pot wet chemical method for the synthesis of various conjugated carbazole derivatives
via
Suzuki-Miyaura cross-coupling reaction and their photophysical properties were screened.
A simple and efficient one pot synthesis of 2-amino-4H-chromen-4-yl phosphonate derivatives has been accomplished by the condensation of salicylaldehyde, malononitrile/ethylcyanoacetate and triethyl ...phosphite/trimethyl phosphite in the presence of molecular iodine as catalyst in water at room temperature. All the reactions were very clean and the products were obtained in very good to excellent yields. The title compounds are characterized by IR, 1H-, 13C-, 31P-NMR and mass spectra, also studied their antimicrobial and antioxidant activity.
A simple and highly efficient multicomponent one-pot synthesis of a series of pharmaceutically interesting functionalized tetrahydropyridine phosphonate derivatives has been developed based on ...low-cost and environmentally benign ceric ammonium nitrate (CAN) catalyst via tandem reactions of 1,3-dicarbonyl compounds, diethylphosphoramidate and various aromatic aldehydes in acetonitrile at room temperature. High atom economy, good yields, eco-friendliness and mild reaction conditions are some of the important features of this protocol.
Studies on green biosynthesis of newly engineered nanoparticles for their prominent medicinal applications are being the torch-bearing concerns of the state-of-the-art research strategies. In this ...concern, we have engineered the biosynthesized Luffa acutangula silver nanoparticles of flavonoid O-glycosides in the anisotropic form isolated from aqueous leave extracts of Luffa acutangula, a popular traditional and ayurvedic plant in south-east Asian countries. These were structurally confirmed by Ultraviolet-visible (UV-Vis), Fourier transform infrared spectroscopy accessed with attenuated total reflection (FTIR-ATR) spectral analyses followed by the scanning electron microscopic (SEM) and the X-ray diffraction (XRD) crystallographic studies and found them with the face-centered cubic (fcc) structure. Medicinally, we have explored their significant antioxidant (DPPH and ABTS assays), antibacterial (disc diffusion assay on E. coli, S. aureus, B. subtilis, S. fecilis, and S. boydii), and anticancer (MTT assay on MCF-7, MDA-MB-231, U87, and DBTRG cell lines) potentialities which augmented the present investigation. The molecular docking analysis of title compounds against 3NM8 (DPPH) and 1DNU (ABTS) proteins for antioxidant activity; 5FGK (Gram-Positive Bacteria) and 1AB4 (Gram-Negative Bacteria) proteins for antibacterial activity; and 4GBD (MCF-7), 5FI2 (MDA-MB-231), 1D5R (U87), and 5TIJ (DBTRG) proteins for anticancer activity has affirmed the promising ligand-protein binding interactions among the hydroxy groups of the title compounds and aspartic acid of the concerned enzymatic proteins. The binding energy varying from -9.1645 to -7.7955 for Cosmosioside (1, Apigenin-7-glucoside) and from -9.2690 to -7.8306 for Cynaroside (2, Luteolin-7-glucoside) implies the isolated compounds as potential bioactive compounds. In addition, the performed studies like QSAR, ADMET, bioactivity properties, drug scores, and toxicity risks confirmed them as potential drug candidates and aspartic acid receptor antagonists. This research auxiliary augmented the existing array of phytological nanomedicines with new drug candidates that are credible with multiple bioactivities.
A facile one-pot, three component, convenient approach for the synthesis of 4,4'-((substituted phenyl)methylene)bis(3-methyl-1H-pyrazol-5-ol) derivatives (3a-l) has been accomplished from the ...reaction of two moles of 5-methyl-2,4-dihydro-3H-pyrazol-3-one (1), with one mole various aromatic aldehydes (2a-l) in the presence ZnO nanoparticles as an efficient heterogeneous catalyst under microwave irradiation (MWI) and solvent-free conditions in good to excellent yields. The major advantages of the present method are, short reaction times, magnetically recyclable catalyst and high yields. The newly synthesized compounds were synthesized and characterized by melting point, IR, NMR, mass spectra. Furthermore the compounds were evaluated for their antioxidant and antimicrobial activities which showed good activities when compared to standards.
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