628325-60-0Relevant articles and documents
Ruthenium catalyzed β-C(sp3)-H functionalization on the 'privileged' piperazine nucleus
Murugesh,Bruneau, Christian,Achard, Mathieu,Sahoo, Apurba Ranjan,Sharma, Gangavaram V. M.,Suresh, Surisetti
supporting information, p. 10448 - 10451 (2017/09/25)
β-C(sp3)-H functionalization on the 'privileged' piperazine nucleus has been disclosed using ruthenium catalysis. The ruthenium catalyzed synthesis of a variety of piperazine fused indoles from ortho-piperazinyl (hetero)aryl aldehydes is presented. This transformation takes place via the dehydrogenation of piperazine followed by an intramolecular nucleophilic addition of the transient enamine moiety onto the carbonyl group and aromatization cascade.
Cationic chalcone antibiotics. Design, synthesis, and mechanism of action
Nielsen, Simon F.,Larsen, Mogens,Boesen, Thomas,Sch?nning, Kristian,Kromann, Hasse
, p. 2667 - 2677 (2007/10/03)
This paper describes how the introduction of "cationic" aliphatic amino groups in the chalcone scaffold results in potent antibacterial compounds. It is shown that the most favorable position for the aliphatic amino group is the 2-position of the B-ring, in particular in combination with a lipophilic substituent in the 5-position of the B-ring. We demonstrate that the compounds act by unselective disruption of cell membranes. Introduction of an additional aliphatic amino group in the á-ring results in compounds that are selective for bacterial membranes combined with a high antibacterial activity against both Gram-positive and -negative pathogens. The most potent compound in this study (78) has an MIC value of 2 μM against methicillin resistant Staphylococus aureus.
