We have synthesized hyaluronic acid (HA) grafted with polyacrylic acid (PAA) via controlled radical polymerization (CRP) in aqueous media. The grafted HA (HA-g-PAA) showed slow degradation by hyaluronidase compared with unmodified HA as a result of the steric hindrance produced by grafted PAA, a...
Composites of poly(ethylene-co-methacrylic acid) with 5 mass fraction percent of precipitated calcium carbonate nanoparticles were prepared by melt extrusion on a miniature melt-blender and medium-scale production equipment. The composites consisted mostly of isolated particles. The ultimate mec...
Interest in BODIPYs (acronym of boron dipyrromethene) has skyrocketed in recent decades, mainly due to their favourable photophysical properties and the wide range of functionalization methods reported for these organic fluorescent dyes. In this context, a simple and straightforward method for t...
Azidobretylium tosylate (ABT), the p-azido analogue of bretylium tosylate, has been synthesized to serve as a photoaffinity probe for bretylium binding sites. Bretylium tosylate has antiarrhythmic action and also interacts with amiloride-sensitive sodium ion transport sites. Acetylcholinesterase...
A novel phosphonium-type condensing reagent, 1,3-dimethyl-2-(3-nitro-1,2,4-triazol-1-yl)-2-pyrrolidin-1-yl-1,3,2-diazaphospholidinium hexafluorophosphate (MNTP), was designed and synthesized. A 31P NMR study on the condensation reactions of phosphate, alkylphosphonate, boranophosphate, and H-pho...
Based on the advantages of azole molecules and fluoroquinolone drugs, we designed and synthesized 34 clinafloxacin-azole conjugates using fragment-based drug design and drug combination principles. The in vitro activities of the synthesized conjugates against Mycobacterium tuberculosis (H37Rv), ...
Treatment of cancer cells by clinically approved hexyl ester of 5-aminolevulinic acid (ALA-Hex) induces accumulation of fluorescent porphyrins in tumors. This allows fluorescence photodiagnosis (PD) of bladder cancer by blue light illumination. However, PD of other cancers is hampered by acute t...
The synthesis of 11 new N-substituted derivatives of (E)-4′-hydroxy-3′-methoxystilbazoles-4 and their antimicrobial activity are reported. The relationships between structure and antibacterial activity are studied. In particular, compounds 5, 7 and 8 showed good antibacterial activity against ...
The FRET efficiencies in donor/acceptor pairs in the two termini of designed fluorescent pentapeptides depend on the flexibility of two arms of triazolyl amino acid scaffolds positioned in the center of the backbones inducing predominant β-sheet conformations. Flexible N-Terminus of the scaffol...
N-protected dehydroamino acid methyl esters have been converted to α-fluoro-β-halo amino acid derivatives under halofluorination reaction conditions. The influences of the nitrogen protecting group of the substrates and of the halonium electrophile on the reaction outcome and the stability of ...
A novel series of methylsulfonyl phenyl derivatives has been designed and synthesized to evaluate their COX-2 inhibitory activity along with anti-convulsant potential. In-vitro evaluation revealed that two compounds MTL-1 and MTL-2 appeared as most potent and selective COX-2 inhibitors in the en...
Reactions of 5-chloro-2-methylsulfonyl-4-pyrimidinecarboxylic acid with aliphatic amines afford 2-amino-5-chloro-4-pyrimidinecarboxylic acid, whereas 5-chloro-2-methylsulfonyl-4-pyrimidinecarboxylates form 5-amino-2-methylsulfonyl-4-pyrimidinecarboxylates under the same conditions.
The four phosphorus and sulfur stereoisomers of ethyl menthyl (methylsulfinyl)methylphosphonate were obtained by preparing the corresponding sulfides from commercially available diethyl (methylthio)methylphosphonate and subjecting them to a highly diastereoselective hydroperoxide oxidation in th...
The synthesis of new (2-methylsulfinyl)phenylphosphonic acid methyl and dimethyl esters in both racemic and non-racemic forms is reported. Resolution of the racemic phosphonic acid mono-ester 1 was accomplished via diastereomeric salt formation with cinchonine. The absolute stereochemistry of th...
This paper attempted to evaluate chicken freshness using a low-cost colorimetric sensor array with the help of a classification algorithm. We fabricated a novel and low-cost colorimetric sensors array, with a specific colorific fingerprint to volatile compounds, using printing chemically respons...
Two new fluorescent heterocyclic systems dipyrido[1′,2′:1,2]imidazo[4,5-b:4,5-e]pyridine-13-carbonitrile and pyrido[1′,2′:1,2]imidazo[4,5-b]pyrido[2′,1′:2,3]imidazo[4,5-e]pyridine-13-carbonitrile were synthesized by one-pot reaction of imidazo[1,2-a]pyridine with 2-(imidazo[1,2-a]pyridin-3...
Novel 5-aminopyridine-2-tetrazole-functionalized polystyrene resin (APTZ-PS) was prepared by anchoring 5-aminopyridine-2-carbonitrile onto chloromethylated polystyrene beads (CMPS) and subsequently using the cyano-tetrazole conversion reaction. The APTZ-PS resin was characterized by Fourier tran...
Two protocols for synthesis of series of low-molecular-weight di- and tri-substituted pyrimidines bearing a functional group at the 4th position, which rely on a base-mediated condensation of amidines or guanidines with β-alkoxyvinyl α-keto esters, have been developed. This approach allowed fo...
A series of 4-[3-chloro-4-(3-fluorobenzyloxy)anilino]-6-(3-substituted-phenoxy)pyrimidine derivatives were elaborately designed based on the skeleton of Lapatinib, and evaluated for their potential to inhibit epidermal growth factor receptor (EGFR) and ErbB-2 tyrosine kinase activities and antip...
The objective of this study is to investigate the use of coffee waste (CW) to remove the 4-chloro-2-methyl phenoxy acetic acid (MCPA) from aqueous solutions. To prepare CW, it was first washed and boiled to remove color and impurities then it was air dried at room temperature for 48 h. Afterward...
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