415913-05-2Relevant academic research and scientific papers
EP1 RECEPTOR LIGANDS
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, (2013/03/28)
The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
Ionization constants of all seven positional isomers of quinolinesulfonamides and quinoline-N,N-dimethylsulfonamides
Ma?lankiewicz, Maria J.,Marciniec, Krzysztof,Ma?lankiewicz, Andrzej,Jaworska, Maria
, p. 284 - 288 (2013/02/23)
The pKa values of isomeric sulfamoylquinolines 2a-8a and N,N-dimethylsulfamoylquinolines 2b-8b were determined by means of a UV-VIS spectroscopic method that uses absorbance diagrams, at constant ionic strength (0.15 M). For sulfamoylquinolines 2a-8a two pKa values - for basic function (Nring: -0.31 to 3.36) and for acid function (SO 2NH2 group: 8.89-10.34) but only one in the case of N,N-dimethylsulfamoylquinolines 2b-8b (-0.05 to 3.07) - were obtained. The full geometry optimization in the 6-311 + G(d) basis set and the NBO population analysis were performed. Correlation between the experimentally determined and theoretically calculated (Sparc program) of pKa values as well as the differences between the calculated NBO population values for neutral and ionic forms were found for compounds 2a-7a and 2b-8b.
From haloquinolines and halopyridines to quinoline- and pyridinesulfonyl chlorides and sulfonamides
Maslankiewicz, Andrzej,Marciniec, Krzysztof,Pawlowski, Maciej,Zajdel, Pawel
, p. 1975 - 1990 (2008/09/16)
The action of sodium methanethiolate (in boiling DMF) towards haloazines (i.e. chloro- or bromo-pyridines and quinolines) (1) (with halogen substituent in non-aza-activated position) causes sequentially halogen ipso-substitution to methylthioazines (2) and then S-demethylation to azinethiolates (3A), which were: i) subjected to S-methylation, ii) oxidized to diazinyl disulfides (4) and iii) oxidatively chlorinated to azinesulfonyl chlorides (5). α- and γ-pyridine- and quinolinesulfonyl chlorides (5a, 5c, 5d and 5f) were prepared by oxidative chlorination of respective disulfides (4) performed in conc. hydrochloric acid and characterized by 1H and 13C NMR spectra. All azinesulfonyl chlorides (5) were effectively converted to corresponding azinesulfonamides (6).
