3878-55-5Relevant articles and documents
Synthesis of alaremycin
Wang, Yong-Gang,Wachi, Masaaki,Kobayashi, Yuichi
, p. 481 - 483 (2006)
Methyl 5-azido-4-oxohexanoate was synthesized from 5-hexenoic acid in six steps and converted to the title compound by NaReO4- and CF 3SO3H-catalyzed reaction in Ac2CVCCl4 followed by hydrolysis of the methyl ester moiety. Georg Thieme Verlag Stuttgart.
Complex Formation of Calcium Ions and Monosubstituted Succinic Acid Derivatives in Aqueous Solutions
Mitrofanova
, p. 17 - 19 (2003)
Complex formation of calcium ions with succinic acid monoamide and methyl hydrogen succinate at 25°C and ionic strength I = 0.3 (KC1) was studied by pH-potentiometric titration. The stability constants of the complexes were determined.
New compounds for a good old class: Synthesis of two Β-lactam bearing cephalosporins and their evaluation with a multidisciplinary approach
Vigliotta, Giovanni,Giordano, Deborah,Verdino, Anna,Caputo, Ivana,Martucciello, Stefania,Soriente, Annunziata,Marabotti, Anna,De Rosa, Margherita
supporting information, (2020/01/22)
Antimicrobial resistance is spreading massively in the world and is becoming one of the main health threats of the 21st century. One of the possible strategies to overcome this problem is to modify the known classes of antibiotics in a rational way, with the aim of tuning their efficacy. In this paper, we present the synthesis and the evaluation of the biological activity of a series of two β-lactam bearing cephalosporin derivatives, in which an additional isolated azetidinone ring, bearing different substituents, is joined to the classical cephalosporanic nucleus by a chain of variable length. A computational approach has been also applied in order to predict the molecular interactions between some representative derivatives and selected penicillin-binding proteins, the natural targets of β-lactam antibiotics. All these derivatives are active against Gram-positive bacteria, with MIC100 comparable or even better than that of the reference antibiotic ceftriaxone, and show no or very low cytotoxic activity on different cell lines. Overall, these molecules appear to be able to exert their activity in particular against microorganisms belonging to some of the species more involved in the development of multidrug resistance.
Synthesis, characterization, lipophilicity and cytotoxic properties of novel bis(carboxylato)oxalatobis(1-propylamine)platinum(IV) complexes
Hizal, Selin,Hejl, Michaela,Jakupec, Michael A.,Galanski, Markus,Keppler, Bernhard K.
, p. 76 - 83 (2019/04/05)
A series of novel bis(carboxylato)oxalatobis(1-propylamine)platinum(IV) complexes as well as an ethylamine analog were synthesized. The compounds are either symmetrical with both axial ligands consisting of monoesters of succinic acid, or unsymmetrical, with one axial ligand being acetate. The compounds were characterized in detail by elemental analysis, mass spectrometry and multinuclear (1H, 13C, 15N, 195Pt) NMR spectroscopy. The reduction behavior was followed by NMR spectroscopy, while lipophilicity was determined by analytical reversed-phase HPLC measurements. The capacity of inhibiting proliferation of the human cancer cell lines A549 (non-small cell lung cancer), CH1(PA-1) (ovarian teratocarcinoma) and SW480 (colon carcinoma) was evaluated by the MTT assay. In the most sensitive cell line CH1(PA-1), all compounds exhibited IC50 values in the lower μM range. In general, the IC50 values decreased with increasing lipophilicity within the two compound series. Nevertheless, replacing one of the succinic ester ligands with acetate has a rather marginal impact on antiproliferative activity and is hardly disadvantageous.
