79421-39-9Relevant academic research and scientific papers
ANTI-INFECTIVE COMPOUNDS
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Page/Page column 30, (2015/02/25)
The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.
Structure-activity relationships of new cyanothiophene inhibitors of the essential peptidoglycan biosynthesis enzyme MurF
Hrast, Martina,Turk, Samo,Sosi?, Izidor,Knez, Damijan,Randall, Christopher P.,Barreteau, Hélène,Contreras-Martel, Carlos,Dessen, Andréa,O'Neill, Alex J.,Mengin-Lecreulx, Dominique,Blanot, Didier,Gobec, Stanislav
, p. 32 - 45 (2013/10/01)
Peptidoglycan is an essential component of the bacterial cell wall, and enzymes involved in its biosynthesis represent validated targets for antibacterial drug discovery. MurF catalyzes the final intracellular peptidoglycan biosynthesis step: the addition of D-Ala-D-Ala to the nucleotide precursor UDP-MurNAc-L-Ala-γ-D-Glu-meso-DAP (or L-Lys). As MurF has no human counterpart, it represents an attractive target for the development of new antibacterial drugs. Using recently published cyanothiophene inhibitors of MurF from Streptococcus pneumoniae as a starting point, we designed and synthesized a series of structurally related derivatives and investigated their inhibition of MurF enzymes from different bacterial species. Systematic structural modifications of the parent compounds resulted in a series of nanomolar inhibitors of MurF from S. pneumoniae and micromolar inhibitors of MurF from Escherichia coli and Staphylococcus aureus. Some of the inhibitors also show antibacterial activity against S. pneumoniae R6. These findings, together with two new co-crystal structures, represent an excellent starting point for further optimization toward effective novel antibacterials.
An improved synthesis of N-aryl and N-heteroaryl substituted piperidones
Sch?n, Uwe,Messinger, Josef,Buckendahl,Prabhu,Konda
, p. 2519 - 2525 (2008/02/02)
An efficient Pd(0)-catalyzed protocol for the rapid and efficient preparation of N-aryl and N-heteroaryl substituted piperidones is described. The two step syntheses proceed with an overall yield of 50-70% using X-Phos as optimal ligand for the Pd(0)-cata
SUBSTITUTED (AMINOIMINOMETHYL OR AMINOMETHYL) BENZOHETEROARYL COMPOUNDS
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, (2008/06/13)
This invention is directed to an (aminoiminomethyl or aminomethyl) benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.
Two-directional photoinduced electron transfer in a trichromophoric system
Depaemelaere, Sigrid,De Schryver, Frans C.,Verhoeven, Jan W.
, p. 2109 - 2116 (2007/10/03)
Competition bewtween electron transfer via a through σ-bond and a through π-bond mechanism has been studied in 1-(4-cyanophenyl)-4-(cyanomethylene)piperidine. In this trichromophoric system designed in a configuration acceptor-donor-acceptor, where the do
Cyclic urea derivatives, pharmaceutical compositions containing these compounds and methods of using the same
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, (2008/06/13)
The invention relates to cyclic urea derivatives of general formula STR1 wherein Ra, Rb, X and Y are as defined herein, pharmaceutical compositions containing the derivatives and processes for preparing them.
Pyrazolo(4,3-c)quinolines
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, (2008/06/13)
There are disclosed compounds of the formula STR1 wherein the various substituents are defined hereinbelow, and, by virtue of their ability to inhibit interleukin 1, their use as antiinflammatory agents and in treatment of disease states involving enzymat
