Chemical synthesis, molecular docking and MepA efflux pump inhibitory effect by 1,8-naphthyridines sulfonamides was written by Oliveira-Tintino, Cicera Datiane de Morais;Tintino, Saulo Relison;Muniz, Debora Feitosa;Rodrigues dos Santos Barbosa, Cristina;Pereira, Raimundo Luiz Silva;Begnini, Ieda Maria;Rebelo, Ricardo Andrade;da Silva, Luiz Everson;Mireski, Sandro Lucio;Nasato, Michele Caroline;Krautler, Maria Isabel Lacowicz;Pereira, Pedro Silvino;Balbino, Tereza Cristina Leal;da Costa, Jose Galberto Martins;Rodrigues, Fabiola Fernandes Galvao;Teixeira, Alexandre Magno Rodrigues;Barreto, Humberto Medeiros;de Menezes, Irwin Rose Alencar;Coutinho, Henrique Douglas Melo;da Silva, Teresinha Goncalves. And the article was included in European Journal of Pharmaceutical Sciences in 2021.Safety of N-(6-Aminopyridin-2-yl)acetamide This article mentions the following:
To evaluate the antibacterial activity and to verify, in silico and in vitro, the inhibition of efflux mechanisms using a series of synthesized 1,8-naphthyridines sulfonamides I [R = 4-Me, 2,5-(Cl)2, 3-CF3, etc.] against Staphylococcus aureus strains carrying MepA efflux pumps were reported. The chem. synthesis occurred through the thermolysis of the Meldrums acid adduct. The sulfonamide derivatives I were obtained by the sulfonylation of 2-amino-5-chloro-1,8-naphthyridine with com. benzenesulfonyl chloride. Antibacterial activity was assessed by the broth microdilution test. Efflux pump inhibitory capacity was evaluated in silico by mol. docking and in vitro by analyzing synergistic effects on ciprofloxacin and ethidium bromide (EtBr) and by EtBr fluorescence emission assays. The following 1,8-naphthyridines were synthesized: I [R = 4-Me, 2,5-(Cl)2, 4-F, 2,3,4-(F)3, 3-CF3, 2,5-(F)2,4-Br]. The 1,8-naphthyridines derivatives I associated with sulfonamides did not showed antibacterial activity. However, they showed a favorable pharmacokinetic profile with possible MepA efflux pump inhibitory action, demonstrated in mol. docking. In addition to the promising results in reducing the concentration of intracellular EtBr. 1,8-naphthyridines I acted as putative agents in the inhibitory action of the MepA efflux pump. In the experiment, the researchers used many compounds, for example, N-(6-Aminopyridin-2-yl)acetamide (cas: 1075-62-3Safety of N-(6-Aminopyridin-2-yl)acetamide).
N-(6-Aminopyridin-2-yl)acetamide (cas: 1075-62-3) belongs to pyridine derivatives. Pyridine’s the lone pair does not contribute to the aromatic system but importantly influences the chemical properties of pyridine, as it easily supports bond formation via an electrophilic attack. Pyridine groups exist in countless molecules, and their applications include catalysis, drug design, molecular recognition, and natural product synthesis.Safety of N-(6-Aminopyridin-2-yl)acetamide