CAS: 443956-08-9; 6-Bromo-2-Nitropyridin-3-Ol

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3-羟基-2-硝基吡啶置于sodium Methylate体系中,用 甲醇 作为反应溶剂,化学反应 0.5H,反应生成 6-溴-2-硝基吡啶-3-醇
参考文献:氧杂双环辛烷连接的新型细菌拓扑异构酶抑制剂作为广谱抗菌剂.
标题:氧杂双环辛烷连接的新型细菌拓扑异构酶抑制剂作为广谱抗菌剂.
摘要:细菌耐药性正在侵蚀现有抗生素的临床实用性,因此有必要发现新的药物.ii型细菌拓扑异构酶是经过临床验证,高效且经过验证的药物靶标.该靶标易于被具有与喹诺酮抗生素具有替代和不同结合位点的各种抑制剂的抑制作用,从而使得能够开发出对喹诺酮类缺乏交叉耐药性的药物.在此描述的是新型细菌拓扑异构酶抑制剂(nbti),它是一类新型的回旋酶和topo Iv抑制剂,由三个不同的结构部分组成.接头部分的取代导致发现有效的广谱nbti,其脱靶活性降低(herg Ic50> 18μm),并改善了物理性能.am8191具有杀菌作用,并选择性抑制dna合成和金黄色葡萄球菌促旋酶(ic50 = 1.02μm)和topo Iv(ic50 = 10.4μm).在金黄色葡萄球菌鼠感染模型中,Am8191在小于2.5 Mg / Kg剂量下显示出肠胃外和口服功效(ed50).与金黄色葡萄球菌dna旋涡酶结合的am8191的共晶体结
DOI:10.1021/ml500069W

专利信息

专利号:US-11401277-B2
优先权日:2017-11-29
标 题 :Anti-bacterial heterocyclic compounds and their synthesis
发明人：PEER MOHAMED SHAHUL HAMEED; BHARATHAM NAGAKUMAR; KATAGIHALLIMATH NAINESH; SHARMA SREEVALLI; NANDISHAIAH RADHA; RAMACHANDRAN VASANTHI
权利人:BUGWORKS RES INC
摘要:The invention relates to compounds of Formula I and Formula (B) along with their stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms, and pharmaceutically active derivatives thereof. These compounds are useful for killing or inhibiting the growth of a microorganism selected from the group consisting of bacteria, virus, fungi, and protozoa.

专利号:US-10711011-B2
优先权日:2016-05-20
标题 :Substituted oxazolidines as anti-bacterial agents
发明人：PEER MOHAMED SHAHUL HAMEED; BHARATHAM NAGAKUMAR; KATAGIHALLIMATH NAINESH; SHARMA SREEVALLI; NANDISHAIAH RADHA
权利人:BUGWORKS RES INC
摘要:The present disclosure relates to compounds of Formula I, its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms thereof and pharmaceutical compositions containing them as the active ingredient which can be used as medicaments. The aforementioned substances can also be used in the manufacture of medicaments for treatment, prevention or suppression of diseases, and conditions mediated by microbes. The present disclosure also relates to the synthesis and characterization of aforementioned substances.