13480-37-0Relevant articles and documents
Asymmetric pyrene derivatives comprising aryl amine group and organic light-emitting diode including the same
-
Paragraph 0252; 0268-0272, (2020/12/18)
The present invention relates to asymmetric pyrene derivatives represented by chemical formula A or chemical formula B and to an organic light-emitting device including the same, wherein substituents of Ar1, Ar2, Ar3, Ar4, Z and m are as defined in the detailed description of the present invention.
Bisphosphonate inhibition of the exopolyphosphatase activity of the Trypanosoma brucei soluble vacuolar pyrophosphatase
Kotsikorou, Evangelia,Song, Yongcheng,Chan, Julian M. W.,Faelens, Stephanie,Tovian, Zev,Broderick, Erin,Bakalara, Norbert,Docampo, Roberta,Oldfield, Eric
, p. 6128 - 6139 (2007/10/03)
Trypanosoma brucei, the causative agent of African trypanosomiasis, contains a soluble, vacuolar pyrophosphatase, TbVSP1, not present in humans, which is essential for the growth of bloodstream forms in their mammalian host. Here, we report the inhibition of a recombinant TbVSP1 expressed in Escherichia coli by a panel of 81 bisphosphonates. The IC50 values were found to vary from ～2 to 850 μM. We then used 3D QSAR (comparative molecular field and comparative molecular similarity index; CoMFA and CoMSIA) methods to analyze the enzyme inhibition results. The R2 values for the experimental versus the QSAR-predicted activities were 0.78 or 0.61 for CoMFA and 0.79 or 0.68 for CoMSIA, for two different alignments. The root-mean-square (rms) pIC50 error for the best CoMFA model was 0.41 for five test sets of five activity predictions, which translates to a factor of ～2.6 error in IC50 prediction. For CoMSIA, the rms pIC50 error and error factors were 0.35 and 2.2, respectively. In general, the most active compounds contained both a single aromatic ring and a hydrogen bond donor feature. Thirteen of the more potent compounds were then tested in vivo in a mouse model of T. brucei infection. The most active compound in vivo provided a 40% protection from death with no apparent side effects, suggesting that further development of such compounds may be of interest.
Novel thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions
-
, (2008/06/13)
Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4 and R7 are defined in the specification, Z is SO or SO2, and Ar is an aromatic or heteroaromatic group as defined herein.
NOVEL THIOPHENE AMIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATING COMPLEMENT-MEDIATED DISEASES AND CONDITIONS
-
Page 153, (2010/02/05)
Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula (I) or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4 and R7 are defined in the specification, Z is SO or SO2, and Ar is an aromatic or heteroaromatic group as defined herein.
Reaction of n-aminophthalimide derivatives with aluminum chloride in benzene
Ohwada, Atsushi,Li, Hao,Sakamoto, Takeshi,Kikugawa, Yasuo
, p. 225 - 233 (2007/10/03)
The reaction of N-aminophthalimide derivatives with AlCl3 in benzene has been investigated. From N-amino- and N-benzamidophthalimide (1a and 1b), N-amino- and N-benzamido3,3-diaryl-2,3-dihydroisoindol-1-ones (2) are obtained in high yield by initial attack of benzene on the imide carbonyl, assisted by the neighboring nitrogen atom. From N-arylaminophthalimide derivatives (4), the N-N bond is cleaved heterolytically to give an arylnitrenium ion and canonical forms involving the arene which are trapped by benzene to give aminobiaryls and N-arylanilines.
A TRIFLUOROMETHANESULFONIC ACID-CATALYZED REACTION OF ARYLHYDRAZINES WITH BENZENE
Ohta, Toshiharu,Miyake, Shinji,Shudo, Koichi
, p. 5811 - 5814 (2007/10/02)
Arylhydrazines reacted with benzene in the presence of trifluoromethanesulfonic acid (TFSA) to give aminobiphenyls.This is a general method for the synthesis of aminobiphenyls.
Acid-Catalyzed Reactions of N-Arylhydroxylamines and Related Compounds with Benzene. Iminium-Benzenium Ions
Shudo, Koichi,Ohta, Toshiharu,Okamoto, Toshihiko
, p. 645 - 653 (2007/10/02)
N-Arylhydroxylamines react with benzene in the presence of trifluoroacetic acid (TFA) at room temperature to give diphenylamines.When TFA was replaced by a strong acid, trifluoromethanesulfonic acid (TFSA), the major products were aminobiphenyls.The nature of the reaction was explored by reactions of 4-substituted phenylhydroxylamines and dialkylaniline N-oxides with benzene.Thus, it was demonstrated that the reactive intermediates are onium-benzenium dications which are trapped by benzene to give aminobiphenyls by a mechanism similar to the Friedel-Krafts alkylation.Further evidence for the proposed reaction mechanism was the observation that nitrosobenzene and azoxybenzene reacted with benzene to give analogous products in the presence of the stronger acid.
