4136-97-4Relevant articles and documents
FePd alloy nanoparticles assembled on reduced graphene oxide as a catalyst for selective transfer hydrogenation of nitroarenes to anilines using ammonia borane as a hydrogen source
Metin, ?nder,Mendoza-Garcia, Adriana,Dalmizrak, Di?dem,Gültekin, Mehmet Serdar,Sun, Shouheng
, p. 6137 - 6143 (2016)
Addressed herein is a facile protocol for the synthesis and assembly of FePd alloy nanoparticles (NPs) on reduced graphene oxide (rGO) to catalyze transfer hydrogenation of nitroarenes to anilines under ambient conditions. 3.5 nm FePd NPs were synthesized by using a surfactant-assisted co-reduction method that allowed NP composition control. FePd NPs were then assembled on rGO via a liquid-phase self-assembly method and studied as catalysts to promote hydrogen transfer from ammonia borane (AB) to numerous nitroarenes in aqueous methanol solutions at room temperature. Among three different rGO-FePd, the commercial C-Pd and rGO-Pd catalysts tested, rGO-Fe48Pd52 showed the highest efficiency in converting nitroarenes to anilines, achieving >90% yields within 10-20 min of reactions. Our work demonstrates an efficient and selective approach to transfer hydrogenation of nitroarenes to anilines.
Synthesis, colon-targeted studies and pharmacological evaluation of an anti-ulcerative colitis drug 4-Aminosalicylic acid-β-O-glucoside
Li, Feifei,Wu, Guoli,Zheng, Huixia,Wang, Li,Zhao, Zhengbao
, p. 486 - 494 (2016)
A glycoside prodrug of 4-aminosalicylic acid (4-ASA) with d-glucose was synthesized for targeted drug delivery to inflammatory bowel. The in vitro assessment of 4-aminosalicylic acid-β-O-glucoside (4-ASA-Glu) as a colon-specific prodrug was studied using colitis rat with the healthy one as control. The stability studies in aqueous buffers (pH 1.2, 6.8 and 7.4) indicated that 4-ASA-Glu was stable over a period of 12 h. The incubation of 4-ASA-Glu with cecal or colonic contents of healthy rats at 37 °C released 4-ASA in 77 or 80% of the dose in 12 h, respectively. The amount of 4-ASA liberated from the incubation of 4-ASA-Glu in cecal or colonic contents of colitis rats at 37 °C was 69 or 79% in 12 h respectively, while less than 9% 4-ASA was detected from the incubation of 4-ASA-Glu with the homogenates of stomach or small intestine. The curative effect of 4-ASA-Glu was evaluated in 2, 4, 6-trinitrobenzenesulfonic acid (TNBS) induced experimental colitis model in male Sprague-Dawley (SD) rats. It was found that 4-ASA-Glu possess significantly ameliorate effect than sulfasalazine, oral 4- and 5-aminosalicylic acid.
New dual ATP-competitive inhibitors of bacterial DNA gyrase and topoisomerase IV active against ESKAPE pathogens
Durcik, Martina,Nyerges, ákos,Skok, ?iga,Skledar, Darja Gramec,Trontelj, Jurij,Zidar, Nace,Ila?, Janez,Zega, Anamarija,Cruz, Cristina D.,Tammela, P?ivi,Welin, Martin,Kimbung, Yengo R.,Focht, Dorota,Benek, Ond?ej,Révész, Tamás,Draskovits, Gábor,Szili, Petra éva,Daruka, Lejla,Pál, Csaba,Kikelj, Danijel,Ma?i?, Lucija Peterlin,Toma?i?, Tihomir
, (2021/02/01)
The rise in multidrug-resistant bacteria defines the need for identification of new antibacterial agents that are less prone to resistance acquisition. Compounds that simultaneously inhibit multiple bacterial targets are more likely to suppress the evolution of target-based resistance than monotargeting compounds. The structurally similar ATP binding sites of DNA gyrase and topoisomerase Ⅳ offer an opportunity to accomplish this goal. Here we present the design and structure-activity relationship analysis of balanced, low nanomolar inhibitors of bacterial DNA gyrase and topoisomerase IV that show potent antibacterial activities against the ESKAPE pathogens. For inhibitor 31c, a crystal structure in complex with Staphylococcus aureus DNA gyrase B was obtained that confirms the mode of action of these compounds. The best inhibitor, 31h, does not show any in vitro cytotoxicity and has excellent potency against Gram-positive (MICs: range, 0.0078–0.0625 μg/mL) and Gram-negative pathogens (MICs: range, 1–2 μg/mL). Furthermore, 31h inhibits GyrB mutants that can develop resistance to other drugs. Based on these data, we expect that structural derivatives of 31h will represent a step toward clinically efficacious multitargeting antimicrobials that are not impacted by existing antimicrobial resistance.
Fluoroquinolone derivative of p-aminosalicylic acid as well as intermediate, preparation method and application of fluoroquinolone derivative
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Paragraph 0051-0054, (2021/01/24)
The invention discloses a fluoroquinolone derivative of p-aminosalicylic acid as well as an intermediate, a preparation method and application of the fluoroquinolone derivative, and belongs to the technical field of drug synthesis. The structural formula of the fluoroquinolone derivative of p-aminosalicylic acid is shown in the specification. An in-vitro antibacterial activity determination resultshows that the target compound has good inhibition activity on bacteria as a whole; most compounds have good antibacterial activity on pichia pastoris, and some compounds have activity even strongerthan that of positive control drugs; the inhibitory activity of the two intermediates on mycobacterium smegmatis is higher than that of most positive control drugs; part of the target compounds have inhibitory activity on citrus germs. The fluoroquinolone derivative of p-aminosalicylic acid and the intermediate have potential application prospects in the fields of bacterium resistance, fungus resistance, tuberculosis resistance and citrus pathogen resistance.
