Synthesis and antibacterial activity evaluation of N(7)-position-modified balofloxacins was written by Hong, Ge;Li, Weitian;Mao, Lina;Wang, Jiawen;Liu, Tianjun. And the article was included in Frontiers in Chemistry (Lausanne, Switzerland) in 2022.Recommanded Product: Tetrahydrofuran-2-carboxylic acid This article mentions the following:
A series of small-mol. fluoroquinolones, I [R = COMe, cyclopropylcarbonyl, pyridin-3-ylcarbonyl, etc.], II [R2 = COMe, 1,2,4-triazol-y-ylacetyl], and III, were synthesized, characterized by HRMS and NMR spectroscopy, and screened for their antibacterial activity against MRSA, P. aeruginosa, and E. coli as model G+/G– pathogens. Compounds I [R = Me, Et, n-Pr] were more potent than the reference drug balofloxacin against MRSA and P. aeruginosa (MIC values of 0.0195 and 0.039μg/mL for I [R = Me] (IV), 0.039 and 0.078μg/mL for each of I [R = Et, n-Pr], resp.). Anal. of the time-dependent antibacterial effect of compound IV toward MRSA showed that in the early logarithmic growth phase, bactericidal effects occurred, while in the late logarithmic growth phase, bacterial inhibition occurred because of concentration effects and possibly the development of drug resistance. Compound IV exhibited low toxicity toward normal mammalian cell lines 3T3 and L-02 and tumor cell lines A549, H520, BEL-7402 and MCF-7. The compound was not hemolytic. Atomic force microscopy (AFM) revealed that IV could effectively destroy the membrane and wall of MRSA cells, resulting in the outflow of the cellular contents. Docking studies indicated the good binding profile of these compounds toward DNA gyrase and topoisomerase IV. ADMET’s prediction showed that most of the synthesized compounds followed Lipinski’s “rule of five” and possessed good drug-like properties. Our data suggested that compound IV exhibited potent anti-MRSA activity and is worthy of further investigation. In the experiment, the researchers used many compounds, for example, Tetrahydrofuran-2-carboxylic acid (cas: 16874-33-2Recommanded Product: Tetrahydrofuran-2-carboxylic acid).
Tetrahydrofuran-2-carboxylic acid (cas: 16874-33-2) belongs to tetrahydrofuran derivatives. Solid acid catalysis, and the advantages often associated with their use, have been proved equally efficient for the synthesis of tetrahydrofurans or furans. Tetrahydrofuran reaction with hydrogen sulfide: In the presence of a solid acid catalyst, tetrahydrofuran reacts with hydrogen sulfide to give tetrahydrothiophene.Recommanded Product: Tetrahydrofuran-2-carboxylic acid
Referemce:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem