方案摘要
方案下载应用领域 | |
检测样本 | |
检测项目 | |
参考标准 |
Out of the prominent global ailments, tuberculosis (TB) is still one of the leading causes of death worldwide due to infectious disease. Development of new drugs that shorten the current tuberculosis treatment time and have activity against drug resistant strains is of utmost importance. Towards these goals we have focused our efforts on developing novel anti-TB compounds with the general structure of 1-adamantyl-3-phenyl urea. This series is active against Mycobacteria and previous lead compounds were found to inhibit the membrane transporter MmpL3, the protein responsible for mycolic acid transport across the plasma membrane. However, these compounds suffered from poor in vitro pharmacokinetic (PK) profiles and they have a similar structure/SAR to inhibitors of human soluble epoxide hydrolase (sEH) enzymes. Therefore, in this study the further optimization of this compound class was driven by three factors: (1) to increase selectivity for anti-TB activity over human sEH activity, (2) to optimize PK profiles including solubility and (3) to maintain target inhibition. A new series of 1-adamantyl-3-heteroaryl ureas was designed and synthesized replacing the phenyl substituent of the original series with pyridines, pyrimidines, triazines, oxazoles, isoxazoles, oxadiazoles and pyrazoles. This study produced lead isoxazole, oxadiazole and pyrazole substituted adamantyl ureas with improved in vitro PK profiles, increased selectivity and good anti-TB potencies with sub lg/mL minimum inhibitory concentrations.
优选 KNAUER(德国诺尔)IJM 冲击射流混合系统Customized NanoProducers
型号:Customized NanoProducers优选 KNAUER(德国诺尔)IJM 冲击射流混合系统SingleCore NanoProducer
型号: IJM SingleCore NanoProducer优选 KNAUER(德国诺尔)IJM 冲击射流混合系统 IJM NanoScaler
型号:IJM NanoScaler优选 KNAUER(德国诺尔)IJM 冲击射流混合系统IJM DuoCore NanoProducer
型号:IJM DuoCore NanoProducer耐士科技:使用Biotage Isolera快速纯化液相制备色谱从库拉索芦荟叶皮提取天然的磷酸二酯酶抑制剂by耐士科技
耐士科技:通过Biotage Isolera快速纯化液相制备色谱帮助进行人体尿液中合成大麻素及其代谢产物的定量半定量测定by耐士科技
耐士科技:通过Biotage Isolera快速纯化液相制备色谱帮助进行人体尿液中合成烷基羟基代谢物的定量半定量测定by耐士科技
相关产品
KNAUER(德国诺尔)IJM 冲击射流混合系统Customized NanoProducers
KNAUER(德国诺尔)IJM 冲击射流混合系统IJM DuoCore NanoProducer
KNAUER(德国诺尔)IJM 冲击射流混合系统SingleCore NanoProducer
KNAUER(德国诺尔)IJM 冲击射流混合系统 IJM NanoScaler
KNAUER(德国诺尔) 高压制备液相色谱
KNAUER(德国诺尔)中压制备色谱
KNAUER(德国诺尔)Bio蛋白质层析纯化系统
KNAUER(德国诺尔) SMB模拟移动床色谱
KNAUER(德国诺尔)K-7400S冰点渗透压仪
NMN|β-烟酰胺单核苷酸 |CAS:1094-61-7
KNAUER(德国诺尔)制备柱
关注
拨打电话
留言咨询