170017-74-0Relevant articles and documents
Synthesis and structure-activity relationships of new 2-phenoxybenzamides with antiplasmodial activity
Dolensky, Johanna,Hermann, Theresa,Hochegger, Patrick,Kaiser, Marcel,M?ser, Pascal,Pferschy-Wenzig, Eva-Maria,Saf, Robert,Seebacher, Werner,Weis, Robert
, (2021/11/08)
The 2-phenoxybenzamide 1 from the Medicines for Malaria Venture Malaria Box Project has shown promising multi-stage activity against different strains of P. falciparum. It was successfully synthesized via a retrosynthetic approach. Subsequently, twenty-one new derivatives were prepared and tested for their in vitro activity against blood stages of the NF54 strain of P. falciparum. Several insights into structure-activity relationships were revealed. The antiplasmodial activity and cytotoxicity of compounds strongly depended on the substitution pattern of the anilino partial structure as well as on the size of substituents. The diaryl ether partial structure had further impacts on the activity. Additionally, several physicochemical and pharmacokinetic parameters were calculated (log P, log D7.4 and ligand efficiency) or determined experimentally (passive permeability and CYP3A4 inhibition). The tert-butyl-4-{4-[2-(4-fluorophenoxy)-3-(trifluoromethyl)benzamido]phenyl}piperazine-1-carboxylate possesses high antiplasmodial activity against P. falciparum NF54 (PfNF54 IC50 = 0.2690 μM) and very low cytotoxicity (L-6 cells IC50 = 124.0 μM) resulting in an excellent selectivity index of 460. Compared to the lead structure 1 the antiplasmodial activity was improved as well as the physicochemical and some pharmacokinetic parameters.
PYRROLE mTORC INHIBITORS AND USES THEREOF
-
, (2020/01/12)
The present invention provides compounds, compositions thereof, and methods of using the same.
PYRROLE mTORC INHIBITORS AND USES THEREOF
-
, (2018/05/27)
The present invention provides compounds, compositions thereof, and methods of using the same.
COMPOUND SUITABLE FOR DETECTION OF VESICULAR ACETYLCHOLINE TRANSPORTER
-
, (2018/09/27)
PROBLEM TO BE SOLVED: To provide a compound suitable for detection of vesicular acetylcholine transporter which can be also used as a compound labeled in PET method. SOLUTION: The present invention provides a compound represented by formula (I), where Rs
NEW VORTIOXETINE INTERMEDIATE AND SYNTHESIS PROCESS THEREOF
-
, (2017/04/12)
The present invention provides a new intermediate II and a method for synthesizing the same. The method comprises: (a) firstly diazotizing a compound of formula I as a raw material, and then halogenating to obtain an intermediate II; and (b) reacting the
Suitable for vesicle acetylecholine translocator detection compound (by machine translation)
-
, (2016/10/07)
The present invention provides a compound represented by formula (I), wherein in formula (I), R 1 represents CH 3 , F, (CH 2 ) n -F, NH-(CH 2 ) n -F, O-(CH 2 ) n -F or S-(CH 2 ) n -F, and n represents an integer of 1 to 3.
SYNTHESIS OF VORTIOXETINE VIA (2-(PIPERAZINE-1 -YL)PHENYL)ANILINE INTERMEDIATES
-
, (2015/08/03)
The present invention provides a new synthetic process for the production of 1-(2-((2,4- dimethylphenyl)thio)phenyl)piperazine (vortioxetine), a drug for the treatment of depression and anxiety, which is conducted via (2-(piperazine-1-yl)phenyl)aniline intermediates.
Synthesis of vortioxetine via (2-(piperazine-1-yl)phenyl)aniline intermediates
-
, (2015/07/22)
The present invention provides a new synthetic process for the production of 1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine (vortioxetine), a drug for the treatment of depression and anxiety, which is conducted via (2-(piperazine-1-yl)phenyl)aniline intermediates.
PYRAZOL-3-ONES THAT ACTIVATE PRO-APOPTOTIC BAX
-
Page/Page column 40, (2013/04/25)
This application features pyrazol-3-one compounds that activate pro-apoptotic BAX. Also featured are methods of using such compounds, e.g., for the treatment or prevention of diseases, disorders, and conditions associated with deregulated apoptosis of cells (e.g., insufficient apoptosis of diseased or damaged cells or essentially the absence of apoptosis of diseased or damaged cells).
PIM KINASE INHIBITORS AND METHODS OF THEIR USE
-
Page/Page column 65, (2008/12/07)
New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase- mediated disorder, such as cancer.