446-34-4Relevant academic research and scientific papers
Selective small molecules blocking HIV-1 tat and coactivator PCAF association
Zeng, Lei,Li, Jiaming,Muller, Michaela,Yan, Sherry,Mujtaba, Shiraz,Pan, Chongfeng,Wang, Zhiyong,Zhou, Ming-Ming
, p. 2376 - 2377 (2007/10/03)
Development of drug resistance from mutations in the targeted viral proteins leads to continuation of viral production by chronically infected cells, contributing to HIV-mediated immune dysfunction. Targeting a host cell protein essential for viral reproduction, rather than a viral protein, may minimize the viral drug resistance problem as observed with HIV protease inhibitors. We report here the development of a novel class of N1-aryl-propane-1,3-diamine compounds using a structure-based approach that selectively inhibit the activity of the bromodomain of the human transcriptional co-activator PCAF, of which association with the HIV trans-activator Tat is essential for transcription and replication of the integrated HIV provirus. Copyright
A novel method for the nitration of simple aromatic compounds
Smith, Keith,Musson, Adam,DeBoos, Gareth A.
, p. 8448 - 8454 (2007/10/03)
Simple aromatic compounds such as benzene, alkylbenzenes, halogenobenzenes, and some disubstituted benzenes are nitrated in excellent yields with high regioselectivity under mild conditions using zeolite β as a catalyst and a stoichiometric quantity of nitric acid and acetic anhydride. The zeolite can be recycled, and the only byproduct is acetic acid, which can be separated easily from the nitration product by distillation; the process is inexpensive and represents an attractive method for the clean synthesis of a range of nitroaromatic compounds. For example, nitration of toluene gives a quantitative yield of mononitrotoluenes, of which 79% is 4-nitrotoluene; fluorobenzene gives a quantitative yield of mononitro compounds, of which 94% is 4-nitrofluorobenzene; and 2-fluorotoluene gives a 96% yield of mononitro products, of which 90% is the 5-nitro isomer and 10% is the 4-nitro isomer.
2-NITROARYL AND 2-CYANOARYL COMPOUNDS AS REGULATORS OF NITRIC OXIDE SYNTHASE
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, (2008/06/13)
2-Nitroaryl or 2-cyanoaryl compounds of the formula pharmaceutical compositions thereof, intermediates useful in the preparation of these compounds, and methods for treating disorders of vascular smooth muscles or diseases of the cartilage, macrophages, neurons, platelets, bronchial smooth muscles, optic muscles and gastrointestinal smooth muscles, in addition to sickle cell anemia, diabetes, synovitis, chondroarthritis and osteoarthritis by employing these compounds.
Thieno[3,2-b]-[1,5]benzodiazepines
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, (2008/06/13)
Thieno[1,5]benzodiazepines having useful CNS activity containing the novel tricyclic ring system: STR1 the 10-position being substituted by an amino, preferably a piperazino, group.
