- Isocyanate stabilizer and preparation method thereof
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The invention relates to an isocyanate stabilizer and a preparation method. thereof, wherein the isocyanate stabilizer structure is (I) as shown in the general formula. , Preparation method can be obtained by one-step reaction synthesis, through separatio
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Paragraph 0065-0069
(2020/03/17)
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- Evaluation of the analgesic effect of 4-anilidopiperidine scaffold containing ureas and carbamates
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Fentanyl is a powerful opiate analgesic typically used for the treatment of severe and chronic pain, but its prescription is strongly limited by the well-documented side-effects. Different approaches have been applied to develop strong analgesic drugs with reduced pharmacologic side-effects. One of the most promising is the design of multitarget drugs. In this paper we report the synthesis, characterization and biological evaluation of twelve new 4-anilidopiperidine (fentanyl analogues). In vivo hot-Plate test, shows a moderate antinociceptive activity for compounds OMDM585 and OMDM586, despite the weak binding affinity on both μ and δ-opioid receptors. A strong inverse agonist activity in the GTP-binding assay was revealed suggesting the involvement of alternative systems in the brain. Fatty acid amide hydrolase inhibition was evaluated, together with binding assays of cannabinoid receptors. We can conclude that compounds OMDM585 and 586 are capable to elicit antinociception due to their multitarget activity on different systems involved in pain modulation.
- Monti, Ludovica,Stefanucci, Azzurra,Pieretti, Stefano,Marzoli, Francesca,Fidanza, Lorenzo,Mollica, Adriano,Mirzaie, Sako,Carradori, Simone,De Petrocellis, Luciano,Schiano Moriello, Aniello,Benyhe, Sándor,Zádor, Ferenc,Sz?cs, Edina,?tv?s, Ferenc,Erdei, Anna I.,Samavati, Reza,Dvorácskó, Szabolcs,T?mb?ly, Csaba,Novellino, Ettore
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p. 1638 - 1647
(2016/10/09)
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- Isatin N-phenylsemicarbazone: Effect of substituents and concentration on anion sensing selectivity and sensitivity
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The effect of substituent and concentration on anion sensing selectivity and sensitivity of nine new easily synthesized isatin N-phenylsemicarbazone E-isomer sensors IIIa-XIa was investigated. The substantial difference between the association constants for IIIa-XIa interaction with strongly and weakly basic anions allows detection of F- or CH3COO- anions even at high weakly basic anion excess. Substitution in position 5- of the isatin ring and para-substitution on the phenyl ring in the phenylsemicarbazide chain influence sensor:anion complex stoichiometry and thus also sensor sensitivity. Detection limits of 3-4 × 10-7 mol dm-3 for F- and CH3COO- anions by sensors IVa and Va bearing electron-withdrawing substituents are among the lowest published detection limits for these anions in organic solvents. The high selectivity and sensitivity of sensor VIa allows confident F- detection at tolerated fluoride drinking-water level. The solution dilution leads to a dramatic change in sensor selectivity. Consequently, one E-isomer can be used to sense both strongly and weakly basic anions. On the other side, higher sensor solution concentrations increase the F- and CH3COO- anion detection range, similar to the additional Z-isomer utilization. This journal is
- Cig, Marek,Jakusov, Klaudia,Donovalov, Jana,Sz?cs, Vojtech,Gplovsk, Anton
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p. 54072 - 54079
(2015/01/09)
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