51771-32-5Relevant articles and documents
Antimicrobial Activity of N-(3-Chloro-2-aryl-4-oxoazetidin-1-yl)-4-nitro benzamide Derivatives
Alghamdi, Saad,Almehmadi, Mazen M.,Asif, Mohammad
, p. 91 - 95 (2022/03/27)
A series of N-(3-chloro-2-aryl-4-oxoazetidin-1-yl)-4-nitro benzamide derivatives (4a-g) were synthesized by reacting various N’-arylidene-4-nitro benzo hydrazide (3a-g) with chloro acetyl chloride in the presence of triethylamine and dioxane. Infrared (IR), proton nuclear magnetic resonance (1HNMR), and mass (MS) spectrometric techniques were used to describe the structure of synthesized compounds, which were further tested for in vitro antibacterial activity, and benzylpenicillin was used as a reference drug. Compounds (4b) and (4e) were showed high antibacterial action, whereas the remaining compounds (4a, 4c, 4d, 4f, and 4g) were showed moderate activity. Finally, this research demonstrates the design and development of novel antibacterial agents.
Structure-Based Rational Design of Novel Inhibitors Against Fructose-1,6-Bisphosphate Aldolase from Candida albicans
Han, Xinya,Zhu, Xiuyun,Hong, Zongqin,Wei, Lin,Ren, Yanliang,Wan, Fen,Zhu, Shuaihua,Peng, Hao,Guo, Li,Rao, Li,Feng, Lingling,Wan, Jian
, p. 1426 - 1438 (2017/07/03)
Class II fructose-1,6-bisphosphate aldolases (FBA-II) are attractive new targets for the discovery of drugs to combat invasive fungal infection, because they are absent in animals and higher plants. Although several FBA-II inhibitors have been reported, none of these inhibitors exhibit antifungal effect so far. In this study, several novel inhibitors of FBA-II from C. albicans (Ca-FBA-II) with potent antifungal effects were rationally designed by jointly using a specific protocols of molecular docking-based virtual screening, accurate binding-conformation evaluation strategy, synthesis and enzymatic assays. The enzymatic assays reveal that the compounds 3c, 3e-g, 3j and 3k exhibit high inhibitory activity against Ca-FBA-II (IC50 50 value of 2.7 μM. Importantly, the compounds 3f, 3g, and 3l possess not only high inhibitions against Ca-FBA-II, but also moderate antifungal activities against C. glabrata (MIC80 = 4-64 μg/mL). The compounds 3g, 3l, and 3k in combination with fluconazole (8 μg/mL) displayed significantly synergistic antifungal activities (MIC80 0.0625 μg/mL) against resistant Candida strains, which are resistant to azoles drugs. The probable binding modes between 3g and the active site of Ca-FBA-II have been proposed by using the DOX (docking, ONIOM, and XO) strategy. To our knowledge, no FBA-II inhibitors with antifungal activities against wild type and resistant strains from Candida were reported previously. The positive results suggest that the strategy adopted in this study are a promising method for the discovery of novel drugs against azole-resistant fungal pathogens in the future.
Synthesis of some novel pharmacologically active schiff bases using microwave method and their derivatives formazans by conventional method
Desai, Krunal G.,Desai
, p. 2097 - 2101 (2007/10/03)
Condensation of p-nitrobenzoylhydrazide 1 with substituted aromatic aldehydes 2 under microwave irradiation and by conventional method provide Schiff bases 3a-j. Schiff bases 3a-j on condensation with diazonium salt of 6-methoxy-2-aminobenzothiazole give formazans 4a-j. This reaction is carried out only by conventional method.