|
[摘要]:With the rise of multidrug-resistant pathogens and the need for novel antibiotics, it is crit. to understand as much as possible from prior efforts and to apply learned lessons to the discovery of future antibiotics. One important parameter in particular has previously been mentioned but, in the view, not sufficiently analyzed: the physicochem. property space of antibacterial drugs. The authors selected 147 antibacterially active compds. that encompass both currently used drugs and compds. that are still under clin. investigation (see Methods for details). Where available, other property values were extd. from the literature, including protein binding and oral bioavailability in humans. This anal. suggests that natural products should be increasingly investigated again to identify novel antibacterial hits. Besides their high level of structural diversity, they are likely to better cover the required physicochem. property space for antibacterial compds. compared to synthetic mols. because of an increased d. of polar functionalities. |
|