6002-15-9Relevant academic research and scientific papers
Optimization of diarylpentadienones as chemotherapeutics for prostate cancer
Patanapongpibul, Manee,Zhang, Changde,Chen, Guanglin,Guo, Shanchun,Zhang, Qiang,Zheng, Shilong,Wang, Guangdi,Chen, Qiao-Hong
, p. 4751 - 4760 (2018/08/21)
Our earlier studies indicate that (1E,4E)-1,5-bis(1-alkyl-1H-imidazol-2-yl)penta-1,4-diene-3-ones and (1E,4E)-1,5-bis(1-alkyl-1H-benzo[d]imidazol-2-yl)penta-1,4-diene-3-ones exhibit up to 121-fold greater antiproliferative potency than curcumin in human p
Direct and Regioselective Introduction of Acetals into Imidazoles at the 2-Position by an Iridium-Catalyzed Reaction with Formates in the Presence of Hydrosilanes
Fukumoto, Yoshiya,Iyori, Yasuaki,Chatani, Naoto
, p. 1662 - 1665 (2017/04/06)
The iridium-catalyzed reaction of imidazoles with formates in the presence of hydrosilanes as coreactants led to the production of 2-[(alkoxy)(siloxy)methyl]imidazoles. Dimethyl acetylenedicarboxylate was the additive of choice for the reaction in terms of reaction efficiency. No reaction was observed in the absence of the hydrosilanes. Whereas substituents at the 1- and 5-positions on the imidazole ring did not affect the reaction, substituents at the 4-position greatly retarded the reaction. The regioselective reaction of 1-methyl-1,2,4-triazole occurred at the carbon atom between the sp3 and sp2 nitrogen atoms of the ring but not between two sp2 nitrogen atoms. The products were converted into imidazole 2-carbaldehydes by hydrolysis under acidic conditions.
Synthesis and antimicrobial profile of N-substituted imidazolium oximes and their monoquaternary salts against multidrug resistant bacteria
Od?ak, Renata,Sko?ibu?i?, Mirjana,Maravi?, Ana
, p. 7499 - 7506 (2013/11/19)
Two different series of N-substituted imidazolium oximes and their monoquaternary salts were synthesized and biologically tested with respect to their ability to inhibit growth a diverse panel of antibiotic susceptible Gram-positive and antibiotic resistant Gram-negative bacteria as well fungal strains. The newly synthesized compounds were analyzed by spectral studies to confirm their structure. The preliminary results showed that all compounds tested possess promising antimicrobial potential against both susceptible Gram-positive and antibiotic resistant Gram-negative isolates, exhibiting a wide range of MIC values from 0.14 to 100.0 μg/mL. The structure-activity relationship demonstrates that the p-methylphenyl and p-fluorophenyl groups in monoquaternary salts 6 and 7 attached directly to the imidazolium ring could be essential for observed remarkable inhibitory profiles against clinically important pathogens Pseudomonas aeruginosa (MIC = 0.14 μg/mL) and Klebsiella pneumoniae (MIC = 1.56 μg/mL). Furthermore, the broth microdilution assay was then used to investigate the antiresistance efficacy of compound 7 against fourteen extended-spectrum β-lactamase (ESBL)-producing strains in comparison to eight clinically relevant antibiotics. Compound 7 exhibited a remarkable antiresistance profiles ranging between 0.39 and 12.50 μg/mL against all of ESBL-producing strains, which leads to the suggestion that may be interesting candidate for development of new antimicrobials to combat multidrug resistant Gram-negative bacteria.
Preparation of aza-polycyclic aromatic compounds via superelectrophilic cyclizations
Li, Ang,Gilbert, Thomas M.,Klumpp, Douglas A.
, p. 3654 - 3657 (2008/09/20)
(Chemical Equation Presented) Alkenyl-substituted N-heterocycles react in superacidic CF3SO3H (triflic acid) to produce dicationic intermediates. These superelectrophiles undergo cyclizations to give varied aza-polycyclic aromatic compounds in generally good yields (27-99%, 16 examples). Theoretical calculations indicate a preference for charge-separated dicationic intermediates.
Substituted heterocyclylisoquinolinium salts and compositions and method of use thereof
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, (2008/06/13)
Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
6-beta(substituted)-(S)-hydroxymethylpenicillanic acids and derivatives thereof
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, (2008/06/13)
Antibacterial penicillins of the formula STR1 or a pharmaceutically acceptable salt thereof wherein R1 is a heterocyclic group and R is hydrogen, the residue of certian carboxy protecting groups or the residue of an ester group readily hydrolyzable in vivo having activity against resistant organisms.
