Seven novel N-arylsulfonyl-3-(2-yl-ethanone)-6-methylindole derivatives 4a–f and 6 were readily synthesized and have been identified as inhibitors of human immunodeficiency virus type-1 (HIV-1) replication. Initial biological studies indicated that a...
The synthesis of a set of 1-aryl-2-aryl(3-pyridyl)ethanones 1-5 and thecorresponding ketoximes 6-9 is reported. Structural studies of oximes 6, 7 and 9 wereperformed in solution using 1H-NMR and in the solid state by X-ray crystallography,providing e...
1-(2,6-Dihydroxy-4-methoxyphenyl)-2-(4-hydroxyphenyl) ethanone (DMHE) was isolated from the ethyl acetate fraction of Phaleria macrocarpa (Scheff.) Boerl fruits and the structure confirmed by GC-MS (gas chromatography-mass spectrometry) and NMR (nucl...
Polymyxins are considered to be the last-line antibiotics that are used to treat infections caused by multidrug-resistant (MDR) gram-negative bacteria; however, the plasmid-mediated transferable colistin resistance gene (mcr-1) has rendered polymyxin...
Background/Objectives: Reference materials are essential for ensuring the accuracy and traceability of measurements in the quality control of medicinal products. This study explores new principles for the preparation of impure materials of active pha...
1-(8-Chloro-3-methyl-1H-pyrazolo[4,3-c]cinnolin-1-yl)-2-(2-chlorophenyl)ethanone 2 has been synthesized through condensation of 3-acetyl-6-chloro-1H-cinnolin-4-one 1 with 2-(2-chlorophenyl)acetohydrazide in polar aprotic solvent containing catalytic...
The crystal and molecular structure of the title compound, viz., (2Z)-2-[3-(4-methoxybenzoyl)-4,4-dimethyl-1,2,-oxazolidin-2-ylidene]-1-(4-methoxyphenyl)ethanone (4), is reported. Compound 4 crystallises from toluene/hexanes mixtures in the P21/c spa...
In this study, 12 new 1-aryl-2-(3,5-dimethylpyrazol-1-yl)ethanone oxime ether derivatives were designed and synthesized to investigate their cytotoxic effects. The in vitro cytotoxic activities of the compounds were evaluated against cervix, colon, b...
SH-1242, a novel inhibitor of heat shock protein 90 (HSP90), is a synthetic analog of deguelin: It was previously reported that the treatment of SH-1242 led to a strong suppression of hypoxia-mediated retinal neovascularization and vascular leakage i...
A number of uracil amides cleave poly (ADP-ribose) polymerase and therefore novel thiouracil amide compounds were synthesized and screened for the loss of cell viability in a human-estrogen-receptor-positive breast cancer cell line. The synthesized c...
In this study a series ofnew1-(2-aryl-5-phenethyl-1,3,4-oxadiazol-3(2H)-yl)ethanones 2a-e was synthesized by the cyclization of imines 1a-e using acetic anhydride. The products were evaluated for anti-bacterial and anti-fungal activity. Among the new...
An electron-transfer chain reaction between 2-nitropropane anion and α-bromoketones derived from nitrobenzene and nitrothiophene was demonstrated by mechanistic study and a specific convenient synthetic protocol. Thus, 2-bromo-1-(5-nitrothiophen-2-yl...
(R)-2-Chloro-1-(2,4-dichlorophenyl) ethanol is a chiral intermediate of the antifungal agent Miconazole. A bacterial strain, ZJPH1806, capable of the biocatalysis of 2-chloro-1-(2,4-dichlorophenyl) ethanone, to (R)-2-chloro-1-(2,4-dichlorophenyl) eth...
To anhydrous AlCl3 (27.35 g, 205 mmol) and anisole (24.11 g, 223 mmol) in dry chloroform (300 mL) 2-bromobenzeneacetyl chloride [1] (43.4 g, 186 mmol) in dry chloroform (100 mL) was added over 30 min at 0 °C and stirred at ambient temperature for 15...
Diazoketone 2 was prepared using 2,4,6-trichloro-1,3,5-triazine (cyanuric chloride) as coupling reagent allowing for the efficient transfer of diazomethane to commercially available carboxylic acid 1 [1].[...]
The steric hindrance in molecules of 1-(2,4,6-trimethylphenyl)ethanone and 1-(2,4,6-triisopropylphenyl)ethanone were shown to substantially differentiate the options of synthesis of the respective alcohols. The former was obtained with a yield of 12%...
Friedel-Craft acylation at 100 °C of 2,5,9,9-tetramethyl-6,7,8,9-tetrahydro-5H-benzocycloheptene [ar-himachalene (1)], a sesquiterpenic hydrocarbon obtained by catalytic dehydrogenation of α-, β- and γ-himachalenes, produces a mixture of two compound...
The novel heterocyclization of 5-(2-aminophenyl)-1Н-tetrazole with potassium ethylxanthogenate or carbon disulfide was proposed. The potassium salt of the tetrazolo[1,5-c]quinazoline-5-thione was subsequently modified by alkylation with proper haloge...
Rhus potaninii Maxim, a type of sumac, is an economically important tree widely cultivated in mountainous areas of western and central China. A gall, called the bellied gallnut, induced by the aphid, Kaburagia rhusicola Takagi, is important in the fo...
Antifungal N-phenacyl derivatives of 4,6- and 5,6-dibromobenzimidazoles are interesting substrates in the synthesis of new antimycotics. Unfortunately, their application is limited by the low synthesis yields and time-consuming separation procedure....
Here, we report the Cu(II)-photocatalysed hydrocarboxylation of imines (C=N) from a series of synthesized Schiff Base derivatives, namely (E)-1-(4-((4-methylbenzylidene)amino)phenyl)ethanone, (E)-1-(3-((5-bromo-2-hydroxybenzylidene)amino)phenyl)ethan...
A newly synthetized series of N-phenacyl derivatives of 2-mercaptobenzoxazole, including analogues of 5-bromo- and 5,7-dibromobenzoxazole, were screened against Candida strains and the action mechanism was evaluated. 2-(1,3-benzoxazol-2-ylsulfanyl)-1...
Treatment of 1-(5-acetyl-3,4-dimethythieno[2,3-b]thiophene-2yl)ethanone (1) with dimethylformamide dimethyl acetal afforded enaminone derivative 2, which reacted with amino derivatives to give the corresponding bis-pyrimidine, bis-pyrazole, bis-triaz...
A new member of the 2-acetylpyridine family has been prepared and characterized. Its synthesis is a two-step process starting from a pyridyl-alcohol in which the ketone moiety is protected as a cyclic acetal. Alkylation of the alcohol followed by hyd...
Three polyhydroxyl-bridged tetranuclear MnIII complexes [Mn4(L1a)2(μ3-OMe)2(μ2-OMe)2(MeOH)2] (1), [Mn4(L2a)2(μ3-OMe)2(μ2-OMe)2(H2O)2] (2), and [Mn4(L3a)2(μ3-OMe)2(μ2-OMe)2(H2O)2] (3) derived from Mnn+-promoted reactivity of Schiff b...
1,4-Dihydropyridines are of interest because some of them exhibit various kinds of pharmaceutical activity [1-3].[...]
Forty-five volatile organic compounds (VOCs) were identified or annotated in the mandibular gland reservoir content (MGRC) of the Southeast Asian ant Colobopsis explodens Laciny and Zettel, 2018 (Hymenoptera: Formicidae), using headspace solid-phase...
Microwave-assisted depolymerization of black-liquor lignin in formic acid was studied, concentrating on the yield of liquid fractions as bio-oil 1 (mainly aromatic monomers) and bio-oil 2 (mainly aromatic oligomers) and the distribution of the specif...
Facile and convenient syntheses of bisdimethylthieno[2,3-b]thiophen-2,5-diyl bis(oxazole-2-amine), bis(1H-imidazol-2-amine), bis((3a)-H-indole),[1,2-a]pyrimidine), bis(1H-imidazo[1,2-b][1,2,4]triazole) and bis(9H-benzo[d]imidazo[1,2-a]imidazole) deri...
The present study explores the potential of four NHC-palladium(II) complexes derived from (Z)- or (E)-styryl-N-alkylbenzimidazolium salts, namely trans-dichloro-[(Z)-1-styryl- 3-benzyl-benzimidazol-2-yliden]pyridine palladium(II) (6), trans-dichloro-...
Vineyards exposed to wildfire generated smoke can produce wines with elevated levels of lignin derived phenols that have acrid, metallic and smoky aromas and flavour attributes. While a large number of phenols are present in smoke affected wines, the...
The product 3 was prepared by the condensation of dienone 2 [1] (1g, 3.11 mmol) with o-phenylenediamine 1 (0.33g, 3.11 mmol) by refluxing an ethanol (50 mL) solution for 1 h.[...]
A mixture of (3,5-dimethyl-1H-pyrazol-1-yl)methanol 1 [1] (1.86 g, 14.8 mmol) and 4-amino-acetophenone 2 (1g, 7.4 mmol) in acetonitrile (50 mL) was stirred in a closed vessel at room temperature for 6 days [2,3,4].[...]
To a solution of dienone 2 [1] (1 g, 3.4 mmol) in absolute ethanol (20 mL) was added 4-methyl o-phenylenediamine 1 (0.41 g, 3.4 mmol) and the mixture was refluxed for 1 hour [2, 3].[...]
A series of chalcone-based diarylpyrazoles containing a phenylsulphone or carbonitrile moiety was synthesized. Thus, 3-acetylpyrazoles 6a–c and 10a–c were used as useful substrates in facile synthesis of functional pyrazoles 7a–f and 11a–f, respectiv...
Four pyrazole compounds, 3-(4-fluorophenyl)-5-phenyl-4,5-dihydro-1H-pyrazole-1-carbaldehyde (1), 5-(4-bromophenyl)-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbaldehyde (2), 1-[5-(4-chlorophenyl)-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazol-1-yl]eth...
A new β-diketone, 2,2,2-trifluoro-1-(4-hydroxy-2H-chromen-3-yl)ethanone (4-TFC), which contains a trifluorinated alkyl group and a rigid chromanone, has been designed and synthesised successfully, and utilized for the synthesis of a new stable Eu3+ i...
The present study evaluated the fumigant effect and potential mechanisms of Chinese prickly ash seed kernel (PSK) against tobacco black shank caused by Phytophthora nicotianae Breda de Haan. The results showed that PSK fumigant increased the soil org...
The product 3 was prepared by the condensation of dienone 2 [1] (1g, 3.1 mmol) with 3,4-diaminotoluene 1 (0.38 g, 3.1 mmol) by refluxing an ethanol (50 mL) solution for 1 h.[...]
The title compound (3) is synthesized by the nucleophilic substitution of 4-chloro-1-isobutyl-1H-imidazo[4,5-c]quinoline 2 with 4-amino acetophenone in n-butanol. Newly prepared imiquimod derivative (3) is characterized by IR, NMR and mass spectral d...
Hydrophobic cryogels with monolithic supermacropores based on poly-trimethylolpropane trimethacrylate (pTrim) containing 1-(2-Hydroxyl-5-nonyphenyl)ethanone oxime (LIX84-I) were successfully prepared by a cryo-polymerization technique using organic s...
Cultivation of the endophytic fungus Penicillium commune, which was isolated from the semi-mangrove plant Hibiscus tiliaceus,afforded one new compound 1-O-(2,4-dihydroxy-6-methylbenzoyl)-glycerol (1) along with thirteen known products, including 1-O-...
Five new 1-(2-(5-nitrofuran-2-yl)-5-(aryl)-1,3,4-oxadiazol-3-(2H)-yl) ethanone compounds 5a–e were synthesized by cyclization of N-acylhydrazones 4a–e with acetic anhydride under reflux conditions. Their structures were fully characterized by IR, 1H-...
In the chemical investigation of marine unicellular bacteria, a new peptide, thalassospiramide G (1), along with thalassospiramides A and D (2–3), was discovered from a large culture of Thalassospira sp. The structure of thalassospiramide G, bearing...
Fragrance is a valuable trait in rice varieties, with its aroma significantly influencing consumer preference. In this study, we conducted comprehensive metabolome and transcriptome analyses to elucidate the genetic and biochemical basis of fragrance...
Indigenous Lactococcus lactis enriched raisins were incorporated in fresh curd cheese in wet, thermally dried, and freeze-dried form to produce a novel probiotic dairy product. Symbiotic cheese represents a rising trend in the global market. The viab...
Porous hydroxyapatite as a drug carrier is very popular and has many clinical applications. However, traditional hydroxyapatite materials have limited osteogenic capacity. Therefore, the development of a new hydroxyapatite drug delivery system is ess...
Three undescribed phenylpropanoid derivatives, including two new bibenzyl constituents (1–2), one new stilbene constituent (3), together with five known compounds stilbostemin F (4), dihydropinosylvin (5), 2-(4-hydroxyphenyl)ethyl benzoate (6),...
Series of novel 3-[(4-methoxyphenyl)amino]propanehydrazide derivatives bearing semicarbazide, thiosemicarbazide, thiadiazole, triazolone, triazolethione, thiophenyltriazole, furan, thiophene, naphthalene, pyrrole, isoindoline-1,3-dione, oxindole, etc...
With 19.3 million new cases and almost 10 million deaths in 2020, cancer has become a leading cause of death today. Curcumin and its analogues were found to have promising anticancer activity. Inspired by curcumin’s promising anticancer activit...
of 2