Month: November 2022

Yi, Qiao-Yan published the artcileAnticancer and antibacterial activity in vitro evaluation of iridium(III) polypyridyl complexes, Synthetic Route of 100-70-9, the main research area is iridium polypyridyl complexes apoptosis cell cycle anticancer antibacterial; Antibacterial activity; Apoptosis; Cell cycle distribution; Iridium(III) complexes; Western blot.

Three iridium(III) polypyridyl complexes [Ir(ppy)2(PYTA)](PF6) (1) (ppy = 2-phenylpyridine), [Ir(bzq)2(PYTA)](PF6) (2) (bzq = benzo[h]quinolone) and [Ir(piq)2(PYTA)](PF6) (3) (piq = 1-phenylisoquinoline, PYTA = 2,4-diamino-6-(2′-pyridyl)-1,3,5-triazine) were synthesized and characterized by elemental anal., IR, 1H NMR and 13C NMR. The cytotoxic activity of the complexes toward cancer SGC-7901, Eca-109, A549, HeLa, HepG2, BEL-7402 and normal LO2 cell lines was investigated by 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. Complex 3 shows the most effective on inhibiting the above cell growth among these complexes. The complexes locate at the lysosomes and mitochondria. AO/EB, Annex V and PI and comet assays indicate that the complexes can induce apoptosis in SGC-7901 cells. Intracellular ROS and mitochondrial membrane potential were examined under fluorescence microscopy. The results demonstrate that the complexes increase the intracellular ROS levels and induce a decrease in the mitochondrial membrane potential. The complexes can enhance intracellular Ca2+ concentration and cause a release of cytochrome c. The autophagy was studied using MDC staining and western blot. Complexes 1-3 can effectively inhibit the cell invasion with a concentration-dependent manner. Addnl., the complexes target tubules and inhibit the polymerization of tubules. The antimicrobial activity of the complexes against S. aureus, E. coli, Salmonella and L. monocytogenes was explored. The mechanism shows that the complexes induce apoptosis in SGC-7901 cells through ROS-mediated lysosomal-mitochondrial, targeting tubules and damage DNA pathways. Three iridium(III) complexes [Ir(N-C)2(PYTA)](PF6) (N-C = ppy, 1; bzq, 2; piq, 3) were synthesized and characterized. The anticancer activity of the complexes against SGC-7901 cells was studied by apoptosis, comet assay, autophagy, ROS, mitochondrial membrane potential, intracellular Ca2+ levels, release of cytochrome c, tubules and western blot anal. The antibacterial activity in vitro was also assayed.

JBIC, Journal of Biological Inorganic Chemistry published new progress about Antibacterial agents. 100-70-9 belongs to class nitriles-buliding-blocks, name is Picolinonitrile, and the molecular formula is C6H4N2, Synthetic Route of 100-70-9.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Onyedibe, Kenneth I. published the artcileSF5- and SCF3-substituted tetrahydroquinoline compounds as potent bactericidal agents against multidrug-resistant persister Gram-positive bacteria, SDS of cas: 1885-29-6, the main research area is pentafluorosulfanyl trifluoromethylthio substituted tetrahydroquinoline multidrug resistance; gram pos bacteria persister bactericidal agent.

Bacteria persister cells are immune to most antibiotics and hence compounds that are active against persister bacteria are needed. We screened a chem. library of SF5- and SCF3-substituted tetrahydroquinoline compounds, synthesized via the Povarov reaction, for antibacterial activity and identified active compounds that displayed good activities against many Gram-pos. bacteria, including persisters. The most potent of these compounds, HSD1835, inhibited the growth of drug-resistant Gram-pos. bacterial pathogens (including clin. strains) at concentrations ranging from 1 μg mL-1 to 4 μg mL-1. Several of the SCF3- and SF5-containing compounds were active against methicillin-resistant Staphylococcus aureus (MRSA) and against the two most fatal strains of vancomycin-resistant Enterococcus (VRE), VRE faecalis and VRE faecium. The compounds showed bactericidal activity against stationary phase persister MRSA in time-kill assays. Mechanistic studies showed that HSD1835 acts by disrupting bacterial membranes. SEM (SEM) was used to confirm bacterial membrane disruption. Interestingly, in a 30 day serial exposure experiment, MRSA remained susceptible to low-dose HSD1835 while resistance to ciprofloxacin and mupirocin emerged by day 10. Analogs of HSD1835, which did not bear the SF5 or SCF3 moieties, were inactive against bacteria. Recent reports (G.A.Naclerio, N.S.Abutaleb, K.I.Onyedibe, M.N.Seleem and H.O.Sintim, RSC Med.Chem. 2020, 11, 102-110 and G.A.Naclerio, N.S.Abutaleb, D.Li, M.N.Seleem and H.O.Sintim, J.Med.Chem. 2020, 63(20), 11934-11944) also demonstrated that adding the SF5 or SCF3 groups to a different scaffold (oxadiazoles) enhanced the antibacterial properties of the compounds, so it appears that these groups are privileged moieties that enhance the antimicrobial activities of compounds Naclerio, N. S. Abutaleb, D. Li, M. N. Seleem and H. O. Sintim, J. Med. Chem. 2020, 63(20), (11934-11944) also demonstrated that adding the SF5 or SCF3 groups to a different scaffold (oxadiazoles) enhanced the antibacterial properties of the compounds, so it appears that these groups are privileged moieties that enhance the antimicrobial activities of compounds

RSC Medicinal Chemistry published new progress about Antibacterial agents. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, SDS of cas: 1885-29-6.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Qian, Deyun published the artcileLigand-Controlled Regiodivergent Hydroalkylation of Pyrrolines, Computed Properties of 100-70-9, the main research area is pyridine oxazoline ligand preparation; alkyalated pyrrolidine preparation regioselective; pyrroline halide hydroalkylation pyridine oxazoline ligand nickel catalyst; alkenes; heterocycles; hydroalkylation; nickel; reaction mechanisms.

Two series of C-alkylated pyrrolidines I [R = Boc, Cbz; R1 = i-Pr, cyclopentyl, indol-1-yl, etc.] and II [R2 = CO2Ph, Boc, Cbz; R3 = cyclohexyl, (CH2)3Ph, 2-thienyl, etc.] were synthesized via ligand controlled nickel-catalyzed regiodivergent hydroalkylation of 3-pyrrolines with alkyl/aryl halides. This method demonstrated broad scope and high functional-group tolerance and could be applied in late-stage functionalizations.

Angewandte Chemie, International Edition published new progress about Alkylation catalysts. 100-70-9 belongs to class nitriles-buliding-blocks, name is Picolinonitrile, and the molecular formula is C6H4N2, Computed Properties of 100-70-9.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Gorvin, John H. published the artcileAromatic nitro-group displacement reactions. Part 4. The action of cyanide and halide ions on compounds containing strongly activated nitro groups, Computed Properties of 34133-58-9, the main research area is nitro group displacement reaction; cyanide reaction nitroarom compound; halide reaction nitroarom compound.

Routes for the reaction of cyanide or halide ions in dipolar aprotic solvents with aromatic compounds, e.g., 2-nitroisophthalonitrile, containing strongly activated nitro groups comprise (a) direct displacement of NO2, (b) ring-substitution coupled with hydroxydenitration and (c) (for CN-) fragmentation of NO2 without substitution.

Journal of Chemical Research, Synopses published new progress about Substitution reaction. 34133-58-9 belongs to class nitriles-buliding-blocks, name is 4-Hydroxyisophthalonitrile, and the molecular formula is C8H4N2O, Computed Properties of 34133-58-9.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Kulkarni, Bheemashankar A. published the artcileA solid-phase equivalent of van Leusen’s TosMIC, and its application in oxazole synthesis, Application of 4-(5-Oxazolyl)benzonitrile, the main research area is solid phase synthesis aryloxazole; oxazole aryl solid phase synthesis.

Polystyrene-SH resin, prepared from Merrifield resin in two steps, was converted to polystyrene-SO2-CH2-NC in three steps. This resin functions as a solid-phase equivalent of p-tolylsulfonylmethyl isocyanide (TosMIC). Thus, reaction with aromatic aldehydes and tetrabutylammonium hydroxide as base yields 5-aryloxazoles.

Tetrahedron Letters published new progress about Solid phase synthesis. 87150-13-8 belongs to class nitriles-buliding-blocks, name is 4-(5-Oxazolyl)benzonitrile, and the molecular formula is C10H6N2O, Application of 4-(5-Oxazolyl)benzonitrile.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Bauer, R. published the artcileEnantioselective hydrolysis of racemic 2-phenylpropionitrile and other (R,S)-2-arylpropionitriles by a new bacterial isolate, Agrobacterium tumefaciens strain d3, COA of Formula: C16H13NO, the main research area is Agrobacterium phenylpropionitrile arylpropionitrile enantioselective hydrolysis; nitrile hydratase enantioselectivity Agrobacterium; amidase enantioselectivity Agrobacterium.

Bacteria were enriched from soil samples with succinate as C source and racemic 2-phenylpropionitrile as sole N source. One of the isolates, strain d3, converted (R,S)-2-phenylpropionitrile with high enantioselectivity to (S)-2-phenylpropionic acid. Strain d3 was identified as Agrobacterium tumefaciens. Resting cells hydrolyzed 2-phenylpropionitrile via 2-phenylpropionamide to 2-phenylpropionic acid. Racemic 2-phenylpropionitrile as well as 2-phenylpropionamide were converted to (S)-2-phenylpropionic acid with an enantiomeric excess >96%. The nitrile hydratase and the amidase preferentially both converted the S enantiomer of their resp. substrates. These 2 enzymes were induced in the presence of (R,S)-2-phenylpropionitrile but only in the absence of NH3. In addition to 2-phenylpropionitrile, strain d3 utilized various aliphatic and aromatic nitriles as N sources. Resting cells of strain d3 also converted (R,S)-2-phenylbutyronitrile, ibuprofen nitrile, ketoprofen nitrile, and α-aminophenylacetonitrile with high enantioselectivity. The nitrile- and amide-converting enzyme activities were also found in cell-free extracts

Applied Microbiology and Biotechnology published new progress about Rhizobium radiobacter. 42872-30-0 belongs to class nitriles-buliding-blocks, name is 2-(3-Benzoylphenyl)propanenitrile, and the molecular formula is C16H13NO, COA of Formula: C16H13NO.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Asskar, Ghada published the artcileGlutaconaldehyde as an Alternative Reagent to the Zincke Salt for the Transformation of Primary Amines into Pyridinium Salts., Product Details of C7H6N2, the main research area is pyridinium salt preparation primary amine glutaconaldehyde zincke.

In the presence of amines, the degradation of glutaconaldehyde in acidic medium can be prevented. By exploiting this behavior, primary amines are transformed into their corresponding pyridinium salts, including those substrates that remain unreactive toward the Zincke salt-the reagent typically used to perform this transformation. The use of glutaconaldehyde also allows controlling the nature of the counterion of the pyridinium with no need for addnl. salt metathesis reaction.

Journal of Organic Chemistry published new progress about Microwave irradiation. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Product Details of C7H6N2.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Kuznetsova, Aleksandra S. published the artcileMicrowave-assisted synthesis and sublimation enthalpies of hemiporphyrazines, HPLC of Formula: 91-15-6, the main research area is hemiporphyrazine preparation microwave irradiation.

It was established that microwave irradiation solvent-free processing of 2,6-diaminopyridine or 1,3-phenylenediamine with phthalonitrile or 4-tert-butylphthalonitrile led to corresponding hemiporphyrazines I (X = N, CH; Y = H, t-Bu; X = CH, Y = t-Bu, Z = H; X = CH, Y = H, Z = t-Bu) with sufficiently high yields and a huge reduction in the time required for synthesis, from 8-12 h to 20 min. The Knudsen effusion method with mass spectrometric control of vapor composition was applied. The mass spectrometric investigations established that the macrocyclic compounds I give a stable stream of particles and their enthalpies of sublimation were estimated by the second law of thermodn.

Journal of Porphyrins and Phthalocyanines published new progress about Microwave irradiation. 91-15-6 belongs to class nitriles-buliding-blocks, name is Phthalonitrile, and the molecular formula is C8H4N2, HPLC of Formula: 91-15-6.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Roscales, Silvia published the artcileSynthesis of Flufenamic Acid: An Organic Chemistry Lab Sequence Using Boronic Acids and Nitrosoarenes under Transition-Metal-Free Conditions, Category: nitriles-buliding-blocks, the main research area is flufenamic boronic acid organic chem laboratory sequence nitrosoarene review.

A method for the synthesis of flufenamic acid, a nonstereoidal anti-inflammatory drug (NSAID) of the anthranilate family (fenams), is described as an experiment for the upper-division undergraduate organic chem. laboratory The key step is the formation of the diarylamine moiety of flufenamic acid by a novel reaction consisting of the coupling of nitrosobenzenes with boronic acids under transition-metal-free conditions. On the one hand, students can compare the performance of two different methods for the preparation of nitrosobenzenes (oxidation of amines and ipso-SEAr reaction on potassium organotrifluoroborates). On the other hand, they compare the yields of two complementary examples for the coupling of nitrosobenzenes with boronic acids. The reactions are followed by thin layer chromatog., and the products are purified by percolation or by column chromatog. Students are also tasked with the confirmation of the structure of the products based on m.p., IR, 1H NMR, 13C NMR, and 19F NMR spectroscopy, and MS spectrometry.

Journal of Chemical Education published new progress about Liquid chromatography. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Category: nitriles-buliding-blocks.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Amirsoleimani, Mina published the artcileNano-sized clinoptilolite as a green catalyst for the rapid and chemoselective N-formylation of amines, Safety of 2-Aminobenzonitrile(Flakes or Chunks), the main research area is clinoptilolite catalyst chemoselective formylation green chem.

An ultrasound-assisted, simple, fast and efficient method reported for the chemoselective N-formylation of amines with formic acid in the presence of nanozeolite clinoptilolite (nano-CP) under solvent-free reaction conditions to give the corresponding formamides. The ultrasound increased the rate of the reaction and afforded excellent yields at room temperature This method has the advantages of high yields, mild conditions, simple methodol., easy work up and short reaction times. The catalyst was characterized by different techniques, was recovered and reused several times without the significant loss of its catalytic performance.

Reaction Kinetics, Mechanisms and Catalysis published new progress about Formylation catalysts. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Safety of 2-Aminobenzonitrile(Flakes or Chunks).

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts