39115-96-3Relevant articles and documents
Synthesis, characterization and antimicrobial screening of novel hydrazide ligand & It’s transition metal complexes
Bhale,Yadav,Tekale,Nawale,Marathe,Kendrekar,Pawar
, p. 938 - 942 (2019)
Different transition metal complexes were synthesized from novel 3-bromo-2-[1-(4-hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)ethylidene]hydrazide ligand (H2L) and characterized by spectral techniques. The synthesized ligand was found to act mono as well as di deprotonated (OH, NH) manner and stoichiometry of the ligand to metal ions was confirmed to be 1:1 in case of complex using metal chloride salts, whereas 1:2 in case of metal(II) complexes using metal acetate(II) salt. Structures of metal complexes were confirmed by IR,1H NMR, TGA, XRD, elemental analysis and UV technique which revealed that Mn(II), Co(II), Ni(II), Cu(II) complexes were octahedral geometry and those of Cu(II), Zn(II) showed square planner and tetrahedral geometry around metal ion respectively. Furthermore H2L and its metal complexes were screened for antimicrobial activity which showed that ligand enhanced its biological activity after coordination with metal ions. In particular, Cd(II) and Mn(II) complexes exhibited excellent antifungal activity.
Oxazole ring-containing honokiol thioether derivative and preparation method and application thereof
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Paragraph 0042; 0045-0046, (2021/08/11)
The invention discloses an oxazole ring-containing honokiol thioether derivative, a preparation method thereof and application of the oxazole ring-containing honokiol thioether derivative as an alpha-glucosidase inhibitor, the chemical structure of the oxazole ring-containing honokiol thioether derivative is shown as a general formula (I), and R is selected from non-substituted or substituted phenyl. Compared with the prior art, the invention provides the novel honokiol thioether derivative containing the oxazole ring, and the honokiol thioether derivative containing the oxazole ring has good inhibitory activity on alpha-glucosidase, provides more possibilities for treating diabetes, and is expected to be used for preparing novel candidate drug molecules for treating diabetes. In addition, the preparation process is simple, the cost is low, and the yield is high.
Design, synthesis, in vitro and in vivo evaluation against MRSA and molecular docking studies of novel pleuromutilin derivatives bearing 1, 3, 4-oxadiazole linker
Liu, Jie,Zhang, Guang-Yu,Zhang, Zhe,Li, Bo,Chai, Fei,Wang, Qi,Zhou, Zi-Dan,Xu, Ling-Ling,Wang, Shou-Kai,Jin, Zhen,Tang, You-Zhi
, (2021/05/17)
A class of pleuromutilin derivatives containing 1, 3, 4-oxadiazole were designed and synthesized as potential antibacterial agents against Methicillin-resistant staphylococcus aureus (MRSA). The ultrasound-assisted reaction was proposed as a green chemistry method to synthesize 1, 3, 4-oxadiazole derivatives (intermediates 85–110). Among these pleuromutilin derivatives, compound 133 was found to be the strongest antibacterial derivative against MRSA (MIC = 0.125 μg/mL). Furthermore, the result of the time-kill curves displayed that compound 133 could inhibit the growth of MRSA in vitro quickly (- 4.36 log10 CFU/mL reduction). Then, compound 133 (- 1.82 log10 CFU/mL) displayed superior in vivo antibacterial efficacy than tiamulin (- 0.82 log10 CFU/mL) in reducing MRSA load in mice thigh model. Besides, compound 133 exhibited low cytotoxicity to RAW 264.7 cells. Molecular docking studies revealed that compound 133 was successfully localized in the binding pocket of 50S ribosomal subunit (ΔGb = -10.50 kcal/mol). The results indicated that these pleuromutilin derivatives containing 1, 3, 4-oxadiazole might be further developed into novel antibiotics against MRSA.
