31770-76-0Relevant academic research and scientific papers
NDM INHIBITOR
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Paragraph 0124-0126, (2014/06/24)
An objective of the present invention is to provide a novel NDM (New Delhi metallo-β-lactamase) inhibitor that functions as a drug for restoring the antibacterial activity of β-lactam antibiotics that have been inactivated as a result of decomposition by NDM. According to the present invention, there is provided an NDM inhibitor contains a compound represented by general formula (I):
Total synthesis of (-)-blepharocalyxin D and analogues
Cons, Benjamin D.,Bunt, Adam J.,Bailey, Christopher D.,Willis, Christine L.
supporting information, p. 2046 - 2049 (2013/06/05)
An efficient strategy for the total synthesis of (-)-blepharocalyxin D and an analogue is described. The key step involves an acid-mediated cascade process in which reaction of methyl 3,3-dimethoxypropanoate with γ,δ- unsaturated alcohols possessing diastereotopic styrenyl groups gives trans-fused bicyclic lactones with the creation of two rings and four stereocenters in one pot.
Metallo-beta-lactamase inhibitors
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Page/Page column 30; 31, (2010/11/30)
A new metallo-β-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of β-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-β-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of β-lactam antibiotics against metallo-β-lactamase producing bacteria by combining the compound of the general formula (I) with β-lactam antibiotics.
Development of an enzyme-linked immunosorbent assay for the pyrethroid insecticide cyhalothrin
Gao, Hongbin,Ling, Yun,Xu, Ting,Zhu, Weiwen,Jing, Hongyu,Sheng, Wei,Li, Qing,Li, Ji
, p. 5284 - 5291 (2007/10/03)
A competitive enzyme-linked immunosorbent assay (ELISA) was developed for detection of the pyrethroid insecticide cyhalothrin. Three haptens with an amine or propanoic acid terminus were synthesized and then conjugated with bovine serum albumin to give immunogens. Eight polyclonal antisera produced by rabbits were screened for titers and affinity using three different coating antigens. The antiserum CWB-C had the highest affinity with cyhalothrin and a low affinity with fenvalerate, fenpropathrin, deltamethrin, and fluvalinate. The half-maximum inhibition concentration for cyhalothrin was 37.2 μg/L, and the limit of detection was 4.7 μg/L. The recoveries of different concentrations of cyhalothrin (0.1-2500 μg/L) from fortified tap water, well water, and wastewater samples as determined with the ELISA were 81-114%.
A simple and effective method for chemoselective esterification of phenolic acids
Guo, Wei,Li, Junfei,Fan, Ningjuan,Wu, Weiwei,Zhou, Peiwen,Xia, Chizhong
, p. 145 - 152 (2007/10/03)
A new method for efficient and chemoselective esterification of phenolic acids in KHCO3/alkyl halide/DMF reaction system is described, by which a series of phenoic acid esters were obtained in excellent yields.
Second Generation of cycloSal-Pronucleotides with Esterase-Cleavable Sites: The "Lock-In"-Concept
Meier, Chris,Ruppel, Manuel F. H.,Vukadinovic, Dalibor,Balzarini, Jan
, p. 89 - 115 (2007/10/03)
A conceptual extension of the cycloSal-pronucleotide approach is presented. The characteristic feature of the new cycloSal-derivatives of the anti-HIV active nucleoside analogue d4T 1 is the incorporation of an enzymatically cleavable carboxylic ester moiety with the intention to trap the triesters inside cells ("lock-in"-concept). CycloSal-triesters bearing different ester groups in the 3-or 5-position of the cycloSal-moiety are described. Surprisingly, only acetyl-and levulinyl esters are cleaved readily in CEM cell extracts while alkyl esters were found to be stable. Nevertheless, in in-vitro anti-HIV assays most of the compounds achieve the thymidine-kinase bypass, thus proving that they act at least as nucleotide delivery systems.
Synthesis of new glycopolymers containing β-d-mannopyranose, and c-2-substituted β-d-mannopyranose residues as a new class of inhibitor
Akai, Shoji,Kajihara, Yasuhiro,Nagashima, Yasuhiko,Kamei, Masugu,Arai, Junko,Bito, Masami,Sato, Ken-Ichi
, p. 121 - 143 (2007/10/03)
New styryl monomers containing β-D-mannopyranose, 2-acetamido-2-deoxy-β-D-mannopyranose, 2-deoxy-2-fluoro-β-D-mannopyranose, and 2-deoxy-β-D-arabino-hexopyranose on their side chains, were efficiently synthesized as a new class of a potent inhibitor resistant to exo-α-mannosidase digestion. The binding affinity of the carbohydrate polymers obtained from those mannopyranosyl styryl monomers by radical polymerization with Concanavalin A were evaluated. A binding assay indicated that the multivalency effect and the affinity enhancement attained by modification at the C-2 position of the β-D-mannopyranoside residue resulted in the.
Development of an Enzyme-Linked Immunosorbent Assay for the Detection of the Pyrethroid Insecticide Fenpropathrin
Wengatz, Ingrid,Stoutamire, Donald W.,Gee, Shirley J.,Hammock, Bruce D.
, p. 2211 - 2221 (2007/10/03)
A competitive enayme-linked immunosorbent assay (ELISA) was developed for the quantitative detection of fenpropathrin [(RS)-α-cyano-3-phenoxybenzyl-2,2,3,3-tetramethylcyclopropanecarboxylate]. Polyclonal antisera were isolated from rabbits immunized with two different fenpropathrin hapten conjugates. One hapten contained an amino function; the other contained a carboxyl group for conjugation to carrier proteins. Mollusk hemocyanins, thyroglobulin, and fetuin were used as carrier proteins. The antisera varied greatly in their affinities for fenpropathrin. A homologous assay system using the coating antigen format was the most sensitive. The IC50 for fenpropathrin was 20 μg/L, and the lower detection limit was 2.5 μg/L. Pyrethroids, such as phenothrin, permethrin, resmethrin, fenvalerate, deltamethrin, cyfluthrin, and cypermethrin, and the pyrethroid metabolites, 3-phenoxybenzoic acid and fenpropathrin acid, did not cross-react significantly in this assay. Ten percent acetone or methanol and a pH of 4 were determined to be optimum assay conditions. Various cationic, anionic, and nonionic detergents had no significant effect on the assay.
