219611-84-4

Upstream product

• 100-10-7 4-dimethylamino-benzaldehyde 
• 20939-15-5 3-methyl-4-amino-5-mercapto-1,2,4-triazole 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of pleuromutilin-Schiff base hybrids as potent anti-MRSA agents in vitro and in vivo

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.

Pleuromutilin derivative with 1,2,4-triazole Schiff base as well as preparation and application of pleuromutilin derivative

The invention belongs to the field of medicinal chemistry, and particularly relates to a pleuromutilin derivative with 1,2,4-triazole Schiff base as well as preparation and application of the pleuromutilin derivative. The pleuromutilin derivative with 1,2,4-triazole Schiff base is a compound represented by a formula 2 or a pharmaceutically acceptable salt thereof, and a solvate, an enantiomer, a diastereoisomer, a tautomer or a mixture of the solvate, the enantiomer, the diastereoisomer and the tautomer of the compound of formula 2 or the pharmaceutically acceptable salt thereof, the compoundnot only has good in-vitro antibacterial activity, but also has the advantage of low preparation cost compared with valnemulin and retapamulin, so that the compound is particularly suitable for beingused as a novel antibacterial drug for preventing and treating human or animal bacterial infectious diseases, particularly infectious diseases caused by drug-resistant staphylococcus aureus.

Microwave-enhanced reactions of 4-amino-5-merecapto-1,2,4-triazoles with benzoyl chloride and aromatic aldehydes

The microwave-enhanced reactions of 4-amino-5-mercapto-3-substituent-1,2,4- triazoles with benzoyl chloride or arylaldehydes under solvent-free conditions without catalyst were studied. 3-Substituded-6-phenyl-1,2,4-triazolo[3,4-b]-1,3, 4-thiadiazoles were