In the constant search for new pharmacological compounds, molecular hybridisation is a well-known technique whereby two or more known pharmacophoric subunits are combined to create a new "hybrid" compound. This hybrid is expected to maintain the characteristics of the original compounds whilst demonstrating improvements to their pharmacological action. Accordingly, we report here a series of molecular hybrid compounds based upon eugenol and chloramphenicol pharmacophores. The hybrid compounds were screened for their in vitro antimicrobial potential against Gram-negative and Gram-positive bacteria and also rapidly growing mycobacteria (RGM). The results highlight that the antimicrobial profiles of the hybrid compounds improve in a very clear fashion when moving through the series. The most prominent results were found when comparing the activity of the hybrid compounds against some of the multidrug-resistant clinical isolates of Pseudomonas aeruginosa, methicillin-resistant clinical isolates of Staphylococcus aureus (MRSA) and clinical isolates of rapidly growing mycobacteria.
- MeSH
- antibakteriální látky terapeutické užití MeSH
- antiinfekční látky * farmakologie MeSH
- chloramfenikol farmakologie MeSH
- eugenol farmakologie MeSH
- farmakofor MeSH
- methicilin rezistentní Staphylococcus aureus * MeSH
- mikrobiální testy citlivosti MeSH
- Staphylococcus aureus MeSH
- Publikační typ
- časopisecké články MeSH
Development of information technologies in recent decades has facilitated also a great progress in the development of new drugs. Methods of Computer-Aided Drug Design allow us to explore the spatial interaction between the receptor and a potential drug. The review deals with a brief summary of these computational methods and is mainly focused on pharmacophore modelling, one of the modern approaches in drug design that has proved to be a useful tool.
