In 2011,Xin, Qi-Sheng; Fan, Hou-Xing; Guo, Bin; He, Hui-Li; Gao, Suo; Wang, Hui; Huang, Yan-Qin; Yang, Yu-She published 《Design, Synthesis, and Structure-Activity Relationship Studies of Highly Potent Novel Benzoxazinyl-Oxazolidinone Antibacterial Agents》.Journal of Medicinal Chemistry published the findings.Reference of 6-Bromopyridin-3-amine The information in the text is summarized as follows:
A series of novel benzoxazinyl-oxazolidinones bearing nonaromatic heterocycle or aryl groups were designed and synthesized. Their in vitro and in vivo antibacterial activities were investigated. Most of the (3S, 3aS) biaryl benzoxazinyl-oxazolidinones exhibited potent activity against Gram-pos. pathogens. SAR trends were observed; a pyridyl C ring was preferable to other 5- or 6-member aryl C rings, while fluorine substitution on the B ring generated derivatives with reduced activity. Various substituent group positions on the pyridyl ring were also evaluated. The resulting compounds displayed excellent activity against linezolid-resistant strains. Compound I exhibited excellent in vitro activity, with a MIC value of 0.25-0.5 μg/mL against MRSA and an activity against linezolid-resistant strains of 8-16-fold higher potency than linezolid. In a MRSA systemic infection model, compound 45 displayed an ED50 < 5.0 mg/kg, a potency that is nearly 3-fold better than that of linezolid. This compound also showed excellent pharmacokinetic profiles, with a half-life of more than 5 h as well as an oral bioavailability of 81% in rats. In the experiment, the researchers used many compounds, for example, 6-Bromopyridin-3-amine(cas: 13534-97-9Reference of 6-Bromopyridin-3-amine)
6-Bromopyridin-3-amine(cas: 13534-97-9) belongs to anime. Left-handed and right-handed forms (mirror-image configurations, known as optical isomers or enantiomers) are possible when all the substituents on the central nitrogen atom are different (i.e., the nitrogen is chiral). With amines, there is extremely rapid inversion in which the two configurations are interconverted.Reference of 6-Bromopyridin-3-amine