COMPOUNDS, COMPOSITIONS, AND METHODS FOR MODULATING CFTR
The present disclosure is directed to disclosed compounds that modulate, e.g., address underlying defects in cellular processing of CFTR activity.
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Paragraph 0168
(2017/08/01)
THERAPEUTIC AGENTS, AND METHODS OF MAKING AND USING THE SAME
In part, the present invention is directed towards compounds with FabI inhibiting properties. Such compounds may also inhibit other enzymes, including those similar to FabI either structurally or functionally, for example, Fab K. Kits and compositions that include the disclosed compounds are also provided. Methods of treating a subject with a bacterial illness is also disclosed.
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Page/Page column 63; 130
(2008/06/13)
Enantioseparation of propafenone-type modulators of multidrug resistnace on cyclodextrin based chiral stationary phases
Enantioseparation of propafenone-type MDR-modulators on a rac-hydroxypropyl modified β-cyclodextrin CSP (CYCLOBOND I RSP) and a (S)-naphthylethylcarbamate modified column (CYCLOBOND I SN) is investigated. Best result could be achieved using the multimodal CYCLOBOND I SN column in the polar organic mode. Generally, the conformationally restricted benzofuranylethanolamines 2a and 2b showed remarkable higher α values than the corresponding propafenone derivatives 1a-e.
Ecker,Mohr,Geyer,Fleischhacker
p. 1 - 11
(2007/10/03)
Structure-activity relationship studies on benzofuran analogs of propafenone-type modulators of tumor cell multidrug resistance
A series of benzofurylethanolamine analogs of propafenone (1a) have been prepared and evaluated for multidrug resistance-reversing activity in two in vitro assay systems. As for propafenones, an excellent correlation of biological data with calculated lipophilicity values was found for benzofurans, whereby the latter generally had lower activity/lipophilicity ratios. Almost identical slopes of the regression lines were obtained for both propafenones and benzofurans. Multiple linear regression analysis of the complete data set yielded an equation with excellent predictive power (r2(cross-valid) = 0.968). Interaction measurements with artificial membranes indicated that the differences in activity between these two series of compounds are not due to differences in the interaction pattern with biological membranes.