Design, synthesis, in vitro and in vivo evaluation against MRSA and molecular docking studies of novel pleuromutilin derivatives bearing 1, 3, 4-oxadiazole linker was written by 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. And the article was included in Bioorganic Chemistry in 2021.Safety of Ethyl pyrazine-2-carboxylate This article mentions the following:
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 chem. method to synthesize 1,3,4-oxadiazole derivatives Among these pleuromutilin derivatives, compound 133 (I) was found to be the strongest antibacterial derivative against MRSA (MIC = 0.125μg/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. Mol. 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. In the experiment, the researchers used many compounds, for example, Ethyl pyrazine-2-carboxylate (cas: 6924-68-1Safety of Ethyl pyrazine-2-carboxylate).
Ethyl pyrazine-2-carboxylate (cas: 6924-68-1) belongs to pyrazine derivatives. Pyrazines are volatile compounds that are used in the cosmetic, food, flavor, and fragrance industries. Pyrazine heterocycles and their benzo derivatives possess many interesting properties, including chemical reactivity profiles, and have diverse applications in total synthesis, medicine, chemical biology, materials, dyes, and imaging.Safety of Ethyl pyrazine-2-carboxylate