5296-38-8Relevant academic research and scientific papers
Synthesis and structure-activity relationship studies of 1,3-disubstituted 2-propanols as BACE-1 inhibitors
Kumar, Arun Babu,Anderson, Jordan Micheal,Melendez, Anthony Lester,Manetsch, Roman
supporting information; experimental part, p. 4740 - 4744 (2012/08/07)
A library of 1,3-disubstituted 2-propanols was synthesized and evaluated as low molecular weight probes for β-secretase inhibition. By screening a library of 121 1,3-disubstituted 2-propanol derivatives, we identified few compounds inhibiting the enzyme at low micromolar concentrations. The initial hits were optimized to yield a potent BACE-1 inhibitor exhibiting an IC 50 constant in the nanomolar range. Exploration of the pharmacological properties revealed that these small molecular inhibitors possessed a high selectivity over cathepsin D and desirable physicochemical properties beneficial to cross the blood-brain barrier.
'Click synthesis' of some novel o-substituted oximes containing 1,2,3-triazole-1,4-diyl residues as new analogs of β-adrenoceptor antagonists
Rad, Mohammad Navid Soltani,Behrouz, Somayeh,Karimitabar, Fatemeh,Khalafi-Nezhad, Ali
experimental part, p. 491 - 501 (2012/05/04)
The 'click synthesis' of some novel O-substituted oximes, 7a-7t, which contain 1,2,3-triazolediyl residues, as new analogs of β-adrenoceptor antagonists is described (Schemes 1-4). The synthesis of these compounds was achieved in four to five steps. The formation of oximes of 9H-fluoren-9-one and benzophenone, i.e., 9a and 9b, respectively, followed by their reaction with propargyl bromide, afforded O-propargyl oximes 10a and 10b, respectively, which by a subsequent CuI-catalyzed Huisgen cycloaddition with prepared β-azido alcohols 11a-11j (Schemes 2 and 3), led to the target compounds 7a-7t in good yields. Copyright
Synthesis and plant growth retardant activity of bis-quaternary salts of ammonia from phenols
Sharma,Bala, Madhu
, p. 975 - 977 (2007/10/03)
Trialkylamines 3-(2-benzylphenoxy)-l-N,N-diethylaminpropan-2-ol (4a), 3-(4-benzylphenoxy)-l-N,N-diethylaminpropan-2-ol (4b), 3-(5-n-hutoxyphcnoxy)-l- N,N-diethylaminpropan-2-ol (4c) and 4,4'-bis(3-N,N-diethylamin-2- hydroxypropanoxy)biphenyl (9) were prepared from respective phenols and converted into corresponding bis-quaternary salts by reacting (4a-c) with malonyl chloride and (9) with ethyl bromide. These salts were tested for biological activity on germination, seedling growth and adventitious root formation on hypocotyl cuttings of Vigina radiata (SML-668). The results of biological studies of different compounds show that these salts do not inhibit seed germination and rather promotory in increasing shoot elongation if used from 10-50 μg/ml. However, all those compounds showed inhibitory action at higher concentration i.e. 100 μg/ml.
