Design, synthesis and antimicrobial activities evaluation of Schiff base derived from secnidazole derivatives as potential FabH inhibitors

Researches and applications of nitroimidazole heterocycles in medicinal chemistry

“…含有脂肪胺乙基结构的卟啉衍生物43 用途广泛的合成药物中受欢迎且可靠的官能团之 一 [102,103] . 在脂肪胺乙基上引入羰基形成的酰胺类衍生 物44和45 (图5)对大肠杆菌的抑制浓度分别为MIC= 3.13 µg/mL, IC 50 =4.60 µM, 二者的抗菌活性均与广谱 抗生素卡那霉素(Kanamycin)相当, 其中酰胺键通过与 大肠杆菌的氨基酸残基进行氢键结合, 阻碍其生物合 成, 具有潜在的蛋白合成酶抑制活性 [104,105] .…”

PENHASCOS DE ATIVIDADE BIOLÓGICA COMO FERRAMENTA NA ANÁLISE DA RELAÇÃO ESTRUTURA ATIVIDADE EM UMA SÉRIE DE INIBIDORES DA ENZIMA Β-Cetoacil-Acp SINTASEIII

“…Após realizar uma análise preliminar na literatura, foram escolhidas 233 moléculas de 16 artigos ((LI et al, 2009;LI et al, 2010;LI et al, 2012;LI et al, 2013;LI et al, 2014;ALHAMADSHEH et al, 2007;ALHAMADSHEH et al, 2008;LV et al, 2010;YANG et al,2012;SONG et al, 2014;WANG et al, 2012;LI et al, 2014;MCKINNEY et al, 2016;CHENG et al, 2009;CHENG et al, 2010;CHENG et al, 2013;ZHANG et al, 2011) para compor o grupo de moléculas para estudo dos AC. Cada uma das 233 moléculas foi desenhada com o software livre MarvinSketch versão 15.9 (ChemAxon, 2017).…”

Design, synthesis, and antibacterial evaluation of new Schiff’s base derivatives bearing nitroimidazole and pyrazole nuclei as potent E. coli FabH inhibitors

“…Encouraged by potential clinical applications of Schiff's base derivatives and our previous investigations on FabH inhibitory activity of nitroimidazole derivatives [19], and another literature survey on pyrazole having the same activity [20], we report here the synthesis and structure-activity relationship of a new series of Schiff's base derivatives having nitroimidazole and pyrazole nuclei in a single scaffold and their antibacterial activities against Escherichia coli, Pseudomonas aeruginosa (P. aeruginosa), Bacillus subtilis (B. subtilis), and Staphylococcus aureus (S. aureus), as well as inhibitory activities against E. coli FabH.…”