75853-95-1Relevant articles and documents
Design, synthesis and biological evaluation of pleuromutilin-Schiff base hybrids as potent anti-MRSA agents in vitro and in vivo
Li, Bo,Zhang, Zhe,Zhang, Jian-Feng,Liu, Jie,Zuo, Xiang-Yi,Chen, Fang,Zhang, Guang-Yu,Fang, Han-Qing,Jin, Zhen,Tang, You-Zhi
, (2021/06/22)
A series of pleuromutilin derivatives with 1,2,4-triazole-3-substituted Schiff base structure were designed and synthesized under mild conditions. The in vitro antibacterial activities of the synthesized derivatives against 4 strains of Staphylococcus aureus (MRSA ATCC 43300, S.aureus ATCC 29213, S.aureus 144 and S.aureus AD3) and 1 strain of E. coli (ATCC 25922) were evaluated by the broth dilution method. Among these derivatives, compound 60 exhibited superior in vitro antibacterial effect against MRSA (MIC = 0.25 μg/mL) than tiamulin (MIC = 0.5 μg/mL), and compound 60 (?2.28 log10 CFU/mL) also displayed superior in vivo antibacterial efficacy than tiamulin (?1.40 log10 CFU/mL) in reducing MRSA load in the mouse thigh infection model. The time-kill study and the post-antibiotic effect study indicated that compound 60 showed a faster bactericidal kinetic and longer PAE time (exposure to 2 × MIC and 4 × MIC for 2 h, the PAE was 4.06 and 4.27 h) against MRSA compared with tiamulin (exposure to 2 × MIC and 4 × MIC for 2 h, the PAE was 1.72 and 2.14 h). Meanwhile, most of these compounds had no significant inhibitory effect on RAW 264.7 cells and HepG2 cells at the concentration of 4 μg/mL. Additionally, the development of resistance study showed that MRSA did not easily develop resistance against compound 60 compared with tiamulin after induction for 8 passages.
A containing sulfide [...] myricetin derivatives, their preparation and use
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Paragraph 0031; 0037; 0038, (2019/04/09)
The invention discloses a containing sulfide [...] myricetin derivatives, their preparation and use, its general structure is as follows [A] shown: wherein R is phenyl, substituted phenyl, aryl heterocyclic; n is the number of the carbon in the carbon chain are 3, 4, 5. The invention of tobacco mosaic virus, citrus ulcer bacteria and rice the dried bean curd is dry bacteria there are better control effect.
triazole Greece ioof alkali compound, preparation method thereof, and use thereof
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Paragraph 0030; 0032, (2016/10/08)
The invention relates to the field of thrombotic disease related drugs, belongs to triazole Schiff base compounds with brand new structures and derivatives of the triazole Schiff base compounds and particularly relates to PAR (Protease Activated Receptor)-1 antagonists with triazole Schiff base structures, preparation methods of the PAR-1 antagonists, pharmaceutical compositions containing the PAR-1 antagonists and applications of the PAR-1 antagonists to preparation of drugs for treating thrombotic diseases. The compounds have the structures as shown in the specification, wherein all the substituent groups are defined as the specification.