Effects of protonation and deprotonation on the reactivity of quinolone:A theoretical study

来源 :Chinese Science Bulletin | 被引量 : 0次 | 上传用户:myloft9h
下载到本地 , 更方便阅读
声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架
论文部分内容阅读
Quinolones are the subject of much research as antibacterial compounds and as a new class of antitumor agents.The protonation(P) and deprotonation(D) sites and conformations of quinolone were investigated.The proton affinity(PA) on each of the possible sites in 4-oxo-1,4-dihydroquinoline has been calculated by the restricted Hartree-Fock(HF) and density functional theory(DFT) methods with the basis set 6-311G**.The O-site of protonation was found to be strongly favored over the N-site for the studied compound in the gas phase.Deprotonation takes place in quinolone by detachment of the N-H and COOH protons.The PA of the simple quinolone molecule was used to characterize quinolone reactivity with DNA binding sites.The relative stabilities of the syn and anti conformations were investigated at the B3LYP/6-311G** level of theory;the syn form was shown to be slightly more stable.Its conformation seems to be intrastabilized by hydrogen-bonds consisting of a hydroxyl proton with the O10 atom as the acceptor.We computed and discussed the charge-density distribution and electrostatic potential to explain the reactivity of quinolone. Quinolones are the subject of much research as antibacterial compounds and as a new class of antitumor agents. Protonation (P) and deprotonation (D) sites and conformations of quinolone were investigated. Proton affinity (PA) on each of the possible sites in 4-oxo-1,4-dihydroquinoline has been calculated by the restricted Hartree-Fock (HF) and density functional theory (DFT) methods with the basis set 6-311G **. The O-site of protonation was found to be strongly favored over the N-site for the studied compound in the gas phase. Depotonation takes place in quinolone by detachment of the NH and COOH protons. The PA of the simple quinolone molecule was used to characterize quinolone reactivity with DNA binding sites. The relative ability of the syn and anti conformations were investigated at the B3LYP / 6-311G ** level of theory; the syn form was shown to be slightly more stable. It conformation seems to be intrastabilized by hydrogen-bonds consisting of a hydroxyl proton with the O10 atom as the acceptor. We computed and discussed the charge-density distribution and electrostatic potential to explain the reactivity of quinolone.
其他文献
<正> 苏联共产党中央委员会九月全体会议"关于进一步发展农业的办法"的决议对全苏人民为建设社会主义而进行的斗争具有极重要的意义。苏联共产党中央委员会九月全体会议在进一步发展农业方面制订了最重要的措施,指出了农业各部门迅速高涨及农产品急据增加的途径。
在高原低氧下呼吸的自主控制[俄文]/MalkinVB,GoraEP.//Fiziol.zh.Im.I.M.Sechenova.1993Nov,79(11).86~92.在低氧条件下自主呼吸(高通气或屏气)对心血管系统和神经系统的影响证实了在6000m... Autonomous Control of Breathing at High Altitude Hypoxia
少量浓鱼肝油滴剂致维生素A急性中毒1例瑞昌市人民医院(332200)汪先达1临床资料患儿,女,4个月,因烦躁、纳差、恶心呕吐3天入院。无咳嗽、发热、腹泻及抽搐。3天前一天内口服浓鱼肝油滴剂3次,每次
建立数据库,实现图书资料的计算机化管理是各图书馆的中心工作,建库属复杂的系统工程。通过讨论建库工作中人力、物力、和时间的合理安排与使用,以及工作中出现的问题和处理
通过提温操作解决了三聚氰胺生产中载气压缩机运行时间短的技术难题。 The technical problems of short running time of the carrier gas compressor in melamine product
赛庚定和甲氰咪胍联合治疗氨苄青霉素副作用76例观察550002贵州省人民医院张良君,王小农氨卡青霉素最常见的副作用为出现皮疹,皮疹发生率为7%左右。我们所遇到的多为迟缓反应,多为用药后5~10天
045用双能X线吸光测定计测量甲亢患者骨矿物质密度[英]/WakasugiM…//ClinEndocrinol.-1993,38(3).-283~286与甲状腺机能亢进(甲亢)有关的骨质疏松特征为皮质骨破骨细胞和成骨细胞活性的增高,然而骨矿物质密度(... 045 Bone mineral de
请下载后查看,本文暂不支持在线获取查看简介。 Please download to view, this article does not support online access to view profile.
对高促性腺激素组(高Gn)32例,低促性腺激素组(低Gn)27例,分别测定血液流变学及性激素.结果:两组全血低切粘度(ηb40~(s-1))、血浆粘度(ηp)、还原粘度(ηr)、k值、体外血栓长
美国发展高新技术产业策略孙元霞(黑龙江省科技情报研究所)美国的高新技术产业领域几乎影响到美国社会经济的各个方面,美国在发展高新技术及产业的有些思路和做法,值得我们在制定