189333-49-1Relevant articles and documents
Identification of Better Pharmacokinetic Benzothiazinone Derivatives as New Antitubercular Agents
Lv, Kai,You, Xuefu,Wang, Bin,Wei, Zengquan,Chai, Yun,Wang, Bo,Wang, Apeng,Huang, Guocheng,Liu, Mingliang,Lu, Yu
, p. 636 - 641 (2017)
A series of new 8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one(BTZ) derivatives containing a C-2 nitrogen spiro-heterocycle moiety based on the structures of BTZ candidates BTZ043 and PBTZ169 were designed and synthesized as new antitubercular agents. Many of them were found to have excellent in vitro activity (MIC 0.15 μM) against the drug susceptive Mycobacterium tuberculosis H37Rv strain and two clinically isolated multidrug-resistant strains. Compounds 11l and 11m display acceptable safety, greater aqueous solubility, and better pharmacokinetic profiles than PBTZ169, suggesting their promising potential to be lead compounds for future antitubercular drug discovery.
Preparation method of 3-alkyl-3, 9-diazaspiro [5, 5] undecane
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, (2020/08/29)
The invention relates to a preparation method of 3-alkyl-3, 9-diazaspiro [5, 5] undecane. The preparation method comprises the following steps: a. reacting a compound I with cyanoacetate under the action of ammonia water and a catalyst to obtain a compoun
Preparation method, intermediate and crystal form of spironolamine arylphosphine oxide
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, (2017/08/30)
The invention discloses a preparation method and a crystal form of high-purity spironolamine arylphosphine oxide. The invention further discloses a method for preparing a compound shown as a formula (I) and an intermediate compound.