116849-53-7Relevant academic research and scientific papers
QUINOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS
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Page/Page column 41, (2010/11/25)
Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N-oxide form thereof, wherein R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2, 3 or 4; R2 is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula ; R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is 1, 2 or 3; R4 and R5 are hydrogen, alkyl or benzyl; or R4 and R5 together and including the N to which they are attached may form a ring; R6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl ; or two vicinal R6 radicals may be taken together to form a bivalent radical of formula - CH=CH-CH=CH-; r is 1, 2, 3, 4 or 5; R7 is hydrogen, alkyl, Ar or Het; R8 is hydrogen or alkyl; R9 is oxo ; or R8 and R9 together form the radical -CH=CH-N=.
Aminoketone Enolisation: Influence of Increasing Chain Length on Intramolecular Catalysis
Cox, Brian G.,Maria, Paolo De,Guerzoni, Lorenza
, p. 163 - 168 (2007/10/02)
Kinetic results are reported on the rates of ionisation of piperidino- and morpholino-phenones of varying chain length in buffer and dilute hydroxide solution, as measured by their rates of halogenation.For both series of aminoketones two important factors are responsible for a high reactivity relative to acetophenone: the positive charge on the protonated (and N-methylated) derivatives, which has a strong influence in the α-(n=1) and β-(n=2) position, and intramolecular general base catalysis by the neutral amino group, which has a maximum effect for the δ-(n=4) derivative.Results for the more acidic protonated morpholinoketones are almost identical to those of corresponding piperidinoketones and show no evidence of intramolecular general acid catalysis.The reduced basicity of the morpholino group is reflected in lower rate constants for the intramolecular general base-catalysed reaction.
