A highly regioselective ortho-acetoxylation of N-(2-benzoylphenyl)benzamides has been achieved using a catalytic amount of Pd(OAc)2 (10 mol %) and a stoichiometric amount of PhI(OAc)2 in a mixture of acetic anhydride and acetic acid via C–H activation to produce the corresponding 2-acetoxybenza...
A series of pyrazole-3-carboxylic acid and pyrazole-3,4-dicarboxylic acid derivatives were synthesized, the structures were confirmed by their NMR (1H and 13C) and FT-IR spectra, and elemental analyses. The antibacterial and antifungal activities of the compounds against five bacterial and five ...
Fluorinated diimide-dicarboxylic acid (DIDA, Code: IV), 1,4-bis(4-trimellitimido-2-trifluoromethylphenoxy) benzene, synthesized by reacting 1,4-bis(4-amino-2-trifluoromethyl phenoxy)benzene (I) with trimellitic anhydride in polar solvents (PSv), was found to crystallize easily in amide-type solv...
The relevance of dicarboxylate anions and dicarboxylic acids in biological and industrial processes requires that such species are easily detected and quantified. In this regard, the research about synthetic receptors, which can offer a straightforward analytical signal, has produced significant...
Solid-state 19F-NMR is a valuable tool in structural studies of membrane-associated peptides. Progress in this area became possible after successful design and synthesis of the fluorine-contained amino acids suitable to substitute natural amino acid residues in the peptides without compromising ...
The presented review is an attempt to summarize a huge volume of data on 5-ene-4-thiazolidinones being a widely studied class of small molecules used in modern organic and medicinal chemistry. The manuscript covers approaches to the synthesis of 5-ene-4-thiazolidinone derivatives: modification o...
The quaternary ammonium reagent m-(trifluoromethyl)phenyltrimethylammonium hydroxide (TMTFTH) has gained widespread use for the derivatisation for GCMS analysis of organic materials found in artists’ materials, such as oils, plant resins and waxes. This paper discusses products formed from reac...
The ene reactions of trifluoromethyl carbonyl compounds give products which may be dehydrated to trifluoromethyl dienes; the Diels Alder reaction of these have been investigated. The dienes from trifluoromethyl ketones hardly reacted, probably because the steric effect of the trifluoromethyl gro...
New 4-{[5-arylidene-2-(4-fluorophenylimino)-4-oxothiazolidin-3-yl]methyl}benzoic acids (5) and 2-thioxo-4-thiazolidinone analogues (6) were synthesised as a part of a continuing search for new inhibitors of protein tyrosine phosphatase 1B (PTP1B), an enzyme which is implicated in metabolic disor...
In pursuing our research targeting the identification of potent inhibitors of PTP1B and LMW-PTP, we have identified new 4-[(5-arylidene-2-arylimino-4-oxo-3-thiazolidinyl)methyl]benzoic acids endowed with interesting in vitro inhibitory profiles. Most compounds proved to be inhibitors of PTP1B an...
Myeloperoxidase (MPO) is expressed by myeloid cells for the purpose of catalyzing the formation of hypochlorous acid, from chloride ions and reaction with a hydrogen peroxide-charged heme covalently bound to the enzyme. Most peroxidase enzymes both plant and mammalian are inhibited by benzoic ac...
In this work, the vibrational characteristics of m-trifluoromethyl benzoic acid have been investigated and both the experimental and theoretical vibrational data indicate the presence of functional groups in the title molecule. The density functional theoretical (DFT) computations were performed...
Various transition metal nanoparticles, prepared by microwave-assisted alcohol reduction method were examined for hydrogenation of benzoic acid to cyclohexanecarboxylic acid under solvent-free conditions. Rh metal was the most effective catalyst over other metal catalyst. The catalyst showed mod...
An 8,5-fused bicyclic peptidomimetic ring system generated by a stereoselective ring metathesis reaction was elaborated into potent inhibitors of interleukin-1β converting enzyme (ICE, caspase-1). Multiple compounds were found that exhibited ICE IC50 values
Photo-irradiation of 2',3-0-isopropylidene-8-phenylthioadenosine in the presence of the peroxides afforded the 8,5'-cyclonucleosides, which, after deacetonation, gave 8,5'(S)- and 8,5'(R)-cycloadenosine, the anti-type fixed model of adenosine. The absolute configurations of t...
Two new 2,4′-epoxy-8,5′-neolignans (1 and 2), together with five known 7,9′;7′,9-diepoxylignans (3 − 7), were isolated from an ethyl acetate soluble portion of a hepatoprotective water decoction of Penthorum chinese. Their structures and absolute configurations were elucidated by extensive s...
Three new neolignans (1−3), including one 2,4′-epoxy-8,5′-neolignan and two 2,4′-epoxy-8,3′-neolignan glycosides, were isolated from the EtOAc-soluble portion of the water decoction of Penthorum chinense Pursh. Their structures and absolute configurations were elucidated by comprehensive ana...
To identify structurally novel corticotropin-releasing factor 1 (CRF1) receptor antagonists, a series of bicyclic core analogs pyrrolo[1,2-b]pyridazines and pyrrolo[2,1-f]triazin-4(3H)-ones, which were designed based on a monocyclic core antagonist, was synthesized and evaluated. Among the compo...
A variety of N-acetyl-β-aryl-1,2-didehydroethylamines were synthesized by direct reduction–acetylation of β-aryl-nitroolefins and assayed as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) for the first time. Compound 7a exhibited a TI value of >13.2 with CC50 value of >0.787 m...
Herein, water-soluble nitrogen-doped carbon dots (N-CDs) possessing strong blue fluorescence were synthesized by one-step hydrothermal treatment using citric acid monohydrate(CA)and semicarbazide hydrochloride with NaOH as solvent. What's important in this article is that the N-CDs interact...
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