1262052-41-4Relevant academic research and scientific papers
Synthesis, in vitro antimycobacterial and antibacterial evaluation of IMB-070593 derivatives containing a substituted benzyloxime moiety
Wei, Zengquan,Wang, Jian,Liu, Mingliang,Li, Sujie,Sun, Lanying,Guo, Huiyuan,Wang, Bin,Lu, Yu
, p. 3872 - 3893 (2013/06/05)
A series of novel IMB-070593 derivatives containing a substituted benzyloxime moiety and displaying a remarkable improvement in lipophilicity were synthesized and evaluated for their in vitro antimycobacterial and antibacterial activity. Our results reveal that the target compounds 19a-m have considerable Gram-positive activity (MIC: 0.008-32 μg/mL), although they are generally less active than the reference drugs against the Gram-negative strains. In particular, compounds 19h, 19j, 19k and 19m show good activity (MICs: 0.008-4 μg/mL) against all of the tested Gram-positive strains, including ciprofloxacin (CPFX)- and/or levofloxacin (LVFX)-resistant MSSA, MRSA and MSSE. Moreover, compound 19l (MIC: 0.125 μg/mL) is found to be 2-4 fold more active than the parent IMB070593, CPFX and LVFX against M. tuberculosis H37Rv ATCC 27294.
2-[(arylmethoxy)imino]imidazolidines with potential biological activities
Saczewski, Jaroslaw,Hudson, Alan L.,Rybczynska, Apolonia
experimental part, p. 671 - 680 (2010/07/04)
A series of 2-[(arylmethoxy)imino]imidazolidines was synthesized by reacting 2-chloro-4,5-dihydroimidazole with corresponding O- arylmethylhydroxylamines and evaluated for their α1-, α2-adrenergic and imidazoline I1, I2 receptor binding affinities. The most potent 2-[(naphthalen-1-ylmethoxy)imino] imidazolidine showed a high selectivity and good affinity for the [ 3H]prazosin-labeled α1-adrenoceptors (Ki = 107 nM). Representative compounds of this series were also tested in vivo for possible circulatory effects in rats after intravenous administration.
