17337-13-2Relevant academic research and scientific papers
Staphylococcus aureus rnpa inhibitors: Computational-guided design, synthesis and initial biological evaluation
Suigo, Lorenzo,Chojnacki, Michaelle,Zanotto, Carlo,Sebastián-Pérez, Victor,Morghen, Carlo De Giuli,Casiraghi, Andrea,Dunman, Paul M.,Valoti, Ermanno,Straniero, Valentina
, (2021/05/04)
Antibiotic resistance is spreading worldwide and it has become one of the most important issues in modern medicine. In this context, the bacterial RNA degradation and processing machinery are essential processes for bacterial viability that may be exploited for antimicrobial therapy. In Staphylococcus aureus, RnpA has been hypothesized to be one of the main players in these mech-anisms. S. aureus RnpA is able to modulate mRNA degradation and complex with a ribozyme (rnpB), facilitating ptRNA maturation. Corresponding small molecule screening campaigns have recently identified a few classes of RnpA inhibitors, and their structure activity relationship (SAR) has only been partially explored. Accordingly, in the present work, using computational modeling of S. aureus RnpA we identified putative crucial interactions of known RnpA inhibitors, and we used this information to design, synthesize, and biologically assess new potential RnpA inhibitors. The present results may be beneficial for the overall knowledge about RnpA inhibitors belonging to both RNPA2000-like thiosemicarbazides and JC-like piperidine carboxamides molecular classes. We evaluated the importance of the different key moieties, such as the dichlorophenyl and the piperidine of JC2, and the semithiocarbazide, the furan, and the i-propylphenyl ring of RNPA2000. Our efforts could provide a foundation for further computational-guided investigations.
COMPOUNDS, COMPOSITIONS, AND METHODS FOR SELECTIVELY INHIBITING β-GLUCURONIDASES AND ALLEVIATING SIDE EFFECTS ASSOCIATED WITH DRUG TREATMENT INDUCED DIARRHEA
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Page/Page column 108, (2019/04/09)
The present disclosure describes compounds and compositions that inhibit β-glucuronidase activity, and methods for attenuating the side effects of one or more drugs and improving the efficacy of drugs by administration of selective β-glucuronidase inhibitors.
MOISTURE-STABLE HOLOGRAPHIC MEDIA
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Paragraph 0188, (2018/01/18)
The invention relates to novel compounds which are especially suitable for use as writing monomers in holographic media. The invention further provides a photopolymer and a holographic medium comprising the inventive compounds, and an optical display, a security document and a holographic optical element comprising an inventive holographic medium.
Palladium-catalyzed synthesis of N-aryl carbamates
Vinogradova, Ekaterina V.,Park, Nathaniel H.,Fors, Brett P.,Buchwald, Stephen L.
supporting information, p. 1394 - 1397 (2013/04/24)
An efficient synthesis of aryl carbamates was achieved by introducing alcohols into the reaction of palladium-catalyzed cross-coupling of ArX (X = Cl, OTf) with sodium cyanate. The use of aryl triflates as electrophilic components in this transformation a
Selective muscarinic antagonists. II. Synthesis and antimuscarinic properties of biphenylylcarbamate derivatives
Naito, Ryo,Takeuchi, Makoto,Morihira, Koichiro,Hayakawa, Masahiko,Ikeda, Ken,Shibanuma, Tadao,Isomura, Yasuo
, p. 1286 - 1294 (2007/10/03)
A novel series of biphenylylcarbamate derivatives were synthesized and evaluated for binding to M1, M2 and M3 receptors and for antimuscarinic activities. Receptor binding assays indicated that biphenyl-2-ylcarbamate derivatives had high affinities for M1 and M3 receptors and good selectivities for M3 receptor over M2 receptor, indicating that the biphenyl-2-yl group is a novel hydrophobic replacement for the benzhydryl group in the muscarinic antagonist field. In this series, quinuclidin-4-yl biphenyl-2-ylcarbamate monohydrochloride (81, YM-46303) exhibited the highest affinities for M1 and M3 receptors, and selectivity for M3 over M2 receptor. Compared to oxybutynin, YM-46303 showed approximately ten times higher inhibitory activity on bladder pressure in reflexly-evoked rhythmic contraction, and about 5-fold greater selectivity for urinary bladder contraction against salivary secretion in rats. Moreover, selective antagonistic activity was also observed in vitro. Further evaluation of antimuscarinic effects on bradycardia and pressor in pithed rats, and on tremor in mice, showed that YM-46303 can be useful for the treatment of urinary urge incontinence as a bladder-selective M3 antagonist with potent activities and fewer side effects.
Role of Alkali Halides in the Synthesis of Nitrogen Containing Heterocycles by Reductive Carbonylation of Aromatic Nitro-Derivatives Catalysed by Ru3(CO)12
Pizzotti, Maddalena,Cenini, Sergio,Quici, Silvio,Tollari, Stefano
, p. 913 - 918 (2007/10/02)
The presence of alkali halides as co-catalysts in the reductive carbonylation of o-nitrobiphenyl 1 catalysed by Ru3(CO)12 strongly increases the rate of reactions and slectivity towards heterocyclization products .With sodium halides, depending on the anion, the selectivity for carbazole is in the order Cl- > Br- ca.F- I-; whereas the selectivity for 5H-phenanthridin-6-one is the reverse I- > Br- ca.F- > Cl-.The influence of the cation can be explained with the polarization of a CO ligand of the ruthenium cluster, due to the interaction of the alkali cation with the oxygen lone pair.In fact high yields (>80percent) of heterocyclization products are obtained when the alkali cation is free to coordinate the CO.When this interaction is reduced, by sequestering the cation with crown-ethers, or better with cryptands, the yield of heterocyclic products is 14percent and 0percent respectively.The role of the anion and cation in the catalytic mechanism are discussed.The attempted extension of this reaction to other nitro-derivatives for the potential synthesis of aromatic heterocycles with larger rings are also reported.
