- PROCESS FOR THE PREPARATION OF BEDAQUILINE FUMARATE
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The present disclosure relates to an improved process for the preparation of bedaquiline fumarate, comprising a step of preparing bedaquiline by reaction of 3-benzyl-6-bromo-2-methoxyquinoline 5 with 3-(dimethylamino)-l-(naphthalen-l-yl)propan-l-one 4 in the presence of lithium pyrrolidide.
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Page/Page column 9
(2020/08/22)
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- New 1-(2-chloroquinolin-3-yl)-4-dimethylamino-2-(naphthalen-1-yl)-1-phenylbutan-2-ols with antituberculosis activity
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New 4-dimethylamino-2-(naphthalen-1-yl)-1-phenyl-1-(quinolin-3-yl)butan-2-ols with antituberculosis activity were synthesized. (1R*,2S*)-1-(6-Bromo-2-chloroquinolin-3-yl)-4-dimethylamino-2-(naphthalen-1-yl)-1-phenylbutan-2-ol hydrocitrate exhibiting high
- Omel’kov,Fedorov,Stepanov
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p. 1908 - 1918
(2019/10/22)
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- Synthesis and anti-tubercular activity of conformationally-constrained and bisquinoline analogs of TMC207
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One of the most significant breakthroughs in the battle against tuberculosis is the recent approval of the quinoline compound, TMC207, for the treatment of drug-resistant tuberculosis. To gain insight into the molecular determinants of the activity of TMC207 and to evaluate the scope of quinoline compounds as anti-tubercular agents, we synthesized a series of TMC207 derivatives and evaluated their anti-tubercular activity. Making the lateral chain of the drug rigid by linking it to an adjacent phenyl substituent resulted in a decrease in activity. In contrast, replacing a phenyl substituent of TMC207 with a quinoline moiety gave bisquinolines that demonstrated potent anti-tubercular activity in in vitro experiments, in ex vivo mouse bone marrow macrophage assays, and also in the in vivo mouse model of the disease. These results provide new guiding principles for modifying the TMC207 scaffold to develop efficacious anti-tubercular drugs and set the stage for the development of bisquinolines as a promising new class of anti-tubercular agents.
- Kalia, Dimpy,Anil Kumar,Meena, Gajanand,Sethi, Kashmir Prasad,Sharma, Rohit,Trivedi, Priyanka,Khan, Shaheb Raj,Verma, Ajay Singh,Singh, Shyam,Sharma, Sandeep,Roy, Kuldeep K.,Kant, Ruchir,Krishnan, Manju Yasodha,Singh, Bhupendra N.,Sinha, Sudhir,Chaturvedi, Vinita,Saxena, Anil K.,Dikshit, Dinesh K.
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p. 1554 - 1563
(2015/08/24)
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- A novel antifungal agent with broad spectrum: 1-(4-Biphenylyl)-3-(1H- imidazol-1-yl)-1-propanone
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A series of (1-substituted aryl)-3-(1H-imidazol-1-yl)-1-propanones was synthesized through the N-alkylation of imidazole with 3-dimethylamino-1- (substituted aryl)-1-propanone hydrochlorides (ketonic Mannich bases). A second series of N1-substituted imidazoles was obtained by the reduction of the carbonyl function of the imidazole-ketones in the previous series by means of NaBH4. All of the compounds were evaluated for antifungal activity against 16 strains of Candida, and 3-(1H-imidazol-1-yl)-1-(4-biphenylyl)-1- propanone emerged as a broad-spectrum antifungal agent. Several 3-(1H-imidazol-1-yl)-1-(2′-(substituted benzyl)oxyphenyl)-1-propanones were also active towards Candida kefyr. Copyright
- Roman, Gheorghe,Mare?, Mihai,Nǎstasǎ, Valentin
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p. 110 - 118
(2013/04/10)
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- DIHYDROIMIDAZOTHIAZOLE DERIVATIVES
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Compounds of formula (I): or pharmaceutically acceptable salts thereof, exhibit 5-HT1A agonism in addition to noradrenaline reuptake inhibition and optionally also 5-HT reuptake inhibition are useful for the treatment of obesity.
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Page/Page column 38
(2008/06/13)
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