79421-46-8Relevant academic research and scientific papers
Anti-Inflammation Compounds
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Paragraph 0179; 0180, (2014/06/23)
The present invention refers to: a compound having the general formula (I), wherein n is 0, 1, 2 or; m is 0, 1, 2 or 3; o is 0, 1, 2 or 3; W, X, Y and Z are independently selected from CH, N or N-oxide; A is NR4, C═O, C═S, OP(O)(O), P═O, CH2, or a heteroarly selected from the group consisting of (a), (b), (c), (d), (e), (f), (g); V is C═O, O, S, CH2, or NR5; as well as its use in treating inflammatory diseases such as asthma, COPD, inflammation post infection, arthritis, atherosclerosis, pain and dermatitis.
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.
ANTI-INFECTIVE COMPOUNDS
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Page/Page column 29-30, (2011/10/10)
The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.
N-sulfonylcarboximidamide apoptosis promoters
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Page/Page column 13, (2008/06/13)
Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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.
Trypanocidal activity of conformationally restricted pentamidine congeners
Donkor, Isaac O.,Huang, Tien L.,Tao, Bin,Rattendi, Donna,Lane, Schennella,Vargas, Marc,Goldberg, Burt,Bacchi, Cyrus
, p. 1041 - 1048 (2007/10/03)
A series of conformationally restricted congeners of pentamidine in which the flexible pentyl bridge of pentamidine was replaced by trans-1,2-bismethylenecyclopropyl, phenyl, pyridinyl, piperazinyl, homopiperazinyl, and piperidinyl groups were synthesized
Alpha 1a adrenergic receptor antagonists
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, (2008/06/13)
This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
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 processes for preparing them
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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.
Synthesis and anti-Pneumocystis carinii activity of piperidine-linked aromatic diimidazolines
Huang, Tien L.,Zhang, Qian,White, Angele T.,Queener, Sherry F.,Bartlett, Marilyn S.,Smith, James W.,Donkor, Isaac O.
, p. 2087 - 2090 (2007/10/03)
A series of novel piperidine-linked aromatic diimidazolines (3-7) have been synthesized as conformationally restricted congeners of the anti-Pneumocystis carinii drug, Pentamidine. These compounds significantly inhibited the growth of Pneumocystis carinii in culture at 1 μg/mL.
