Quantum-chemical study of organic reaction mechanisms. XI.*1 Biologically active 4-substituted 1,2,4-triazoles from diformylhydrazine and aminophenols

Chirkina, E. A.; Ларина, Л. И.

doi:10.1007/s11224-022-01969-1

Cited by 2 publications

(1 citation statement)

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“…According to the previous research (Chirkina & Larina, 2022), we propose the possible reaction mechanism of this reaction, which was shown in Figure 2. The key points of the mechanism for the formation of triazole is the nucleophilic attack of the amino nitrogen to the carbonyl carbon.…”

Section: Chemistrymentioning

confidence: 95%

Design, synthesis, and biological evaluation of pleuromutilin derivatives containing 1,2,4‐triazole linker

Zhou

Wang

et al. 2023

Drug Development Research

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A series of thioether pleuromutilin derivatives containing 1,2,4‐triazole on the side chain of C14 were designed and synthesized. The in vitro antibacterial activities experiments of the synthesized derivatives showed that compounds 72 and 73 displayed superior in vitro antibacterial effect against MRSA minimal inhibitory concentration (MIC = 0.0625 μg/mL) than tiamulin (MIC = 0.5 μg/mL). The results of time‐kill study and postantibiotic effect study indicated that compound 72 could inhibit the growth of MRSA quickly (−2.16 log10 CFU/mL) and showed certain postantibiotic effect (PAE) time (exposure to 2 × MIC and 4 × MIC for 2 h, the PAE was 1.30 and 1.35 h) against MRSA. Furthermore, the binding mode between compound 72 and 50S ribosome of MRSA was explored by molecular docking and five hydrogen bonds were formed between compound 72 and 50S ribosome.

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Section: Chemistrymentioning

confidence: 95%