40644-16-4Relevant academic research and scientific papers
Synthesis and evaluation of the oil removal potential of 3-bromo-benzimidazolone polymer grafted silica gel
Izevbekhai, Oisaemi Uduagele,Gitari, Wilson Mugera,Tavengwa, Nikita Tawanda,Ayinde, Wasiu Babatunde,Mudzielwana, Rabelani
, p. 11356 - 11363 (2021)
This work reports the synthesis of 3-bromo-benzimidazolone using melt condensation, its polymerization and functionalization on silica which was extracted from diatomaceous earth in our previous work. The synthesized compounds were characterized using FTIR, NMR, SEM-EDS and TEM. The FTIR and NMR spectra of the synthesized benzimidazolones showed the compounds to have several functional groups: A band due to Si-O-C at 1085.41 cm?1, a broad band at 3380 cm?1and chemical shifts: positive distortionless enhancement by polarization transfer (DEPT)13C peaks (indicating lack of CH2and CH3groups),1H NMR - 11.053 ppm (N-H), 7.086 ppm (Ar-H);13C NMR - 155.34 ppm (CO), 101.04 ppm (C-Br) characteristic of benzimidazolones. SEM-EDS of the functionalized silica showed a rough irregular morphology with Si and O as the major elements. Carbon was also present indicating that silica was successfully functionalized with 3-bromo-benzimidazolone and TEM showed interconnected smear-like particles arranged irregularly. The functionalized silica was then applied in the treatment of oily wastewater and factors like initial oil concentration, adsorption dosage and time were optimized using the central composite design of response surface methodology in the design expert software. The amount of oil adsorbed was obtained by quantifying the total organic carbon using TOC test kits. Results showed that the optimum conditions for oil removal were 6650 mg L?1oil concentration, with adsorbent dosage of 0.004 g and a contact time of 16 h. Under these conditions, the percentage adsorption was 97.9% with a desirability of 0.99. The materials were therefore seen to be applicable to field wastewaters.
Design, synthesis and biological evaluation of arylpyridin-2-yl guanidine derivatives and cyclic mimetics as novel msk1 inhibitors. An application in an asthma model
Bihel, Frédéric,Bollenbach, Maud,Bourguignon, Jean-Jacques,Camelin, Guillaume,Daubeuf, Fran?ois,Frossard, Nelly,Nemska, Simona,Obrecht, Adeline,Rognan, Didier,Schmitt, Martine,Villa, Pascal,Wagner, Patrick
supporting information, (2021/06/21)
Mitogen-and Stress-Activated Kinase 1 (MSK1) is a nuclear kinase, taking part in the activation pathway of the pro-inflammatory transcription factor NF-kB and is demonstrating a therapeutic target potential in inflammatory diseases such as asthma, psoriasis and atherosclerosis. To date, few MSK1 inhibitors were reported. In order to identify new MSK1 inhibitors, a screening of a library of low molecular weight compounds was performed, and the results highlighted the 6-phenylpyridin-2-yl guanidine (compound 1a, IC50~18 μM) as a starting hit for structure-activity relationship study. Derivatives, homologues and rigid mimetics of 1a were designed, and all synthesized compounds were evaluated for their inhibitory activity towards MSK1. Among them, the non-cytotoxic 2-aminobenzimidazole 49d was the most potent at inhibiting significantly: (i) MSK1 activity, (ii) the release of IL-6 in inflammatory conditions in vitro (IC50~2 μM) and (iii) the inflammatory cell recruitment to the airways in a mouse model of asthma.
LACTAM-CONTAINING COMPOUNDS FOR THE TREATMENT OF PAIN
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Page/Page column 23; 30, (2021/02/12)
Provided herein are compounds that are useful in the treatment of pain in a subject. Also provided herein is a pharmaceutical composition comprising compounds or pharmaceutically acceptable salts thereof, and a pharmaceutically acceptable carrier and meth
Design and synthesis of a novel series of (1′S,2R,4′S)-3H-4′-azaspiro[benzo[4,5]imidazo[2,1-b]oxazole-2,2′-bicyclo[2.2.2]octanes] with high affinity for the α7 neuronal nicotinic receptor
Cook, James,Zusi, F. Christopher,Hill, Matthew D.,Fang, Haiquan,Pearce, Bradley,Park, Hyunsoo,Gallagher, Lizbeth,McDonald, Ivar M.,Bristow, Linda,Macor, John E.,Olson, Richard E.
, p. 5002 - 5005 (2017/10/23)
We describe an efficient and convergent synthesis of a series of (1′S,2R,4′S)-3H-4′-azaspiro[benzo[4,5]imidazo[2,1-b]oxazole-2,2′-bicyclo[2.2.2]octanes] displaying potency for the α7 nicotinic acetylcholine receptor (nAChR) and good selectivity vs. the re
QUINUCLIDINE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
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, (2016/06/01)
There are disclosed a series of quinuclidines having the Formula (I). which bind to the nicotinic α7 receptor and may be useful for the treatment of disorders of the central nervous system.
PHENYLSULFONAMIDE-SUBSTITUTED, PYRAZOLO[1, 5-A]PYRIMIDINES, METHODS FOR PREPARATION AND USES THEREOF
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Page/Page column 32-33, (2009/10/22)
Phenylsulfonamide substituted, pyrazolo[1,5-a]pyrimidines are described. The compounds of the invention selectively inhibit Raf kinase activity and are useful for treating disorders associated with Raf kinases. Formula (I)
BRIDGED, BICYCLIC HETEROCYCLIC OR SPIRO BICYCLIC HETEROCYCLIC DERIVATIVES OF PYRAZOLO[1,5-A]PYRIMIDINES, METHODS FOR PREPARATION AND USES THEREOF
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Page/Page column 96, (2009/10/21)
Compounds of formula A: Formula (1) pharmaceutically acceptable salts thereof are described, which selectively inhibit Raf kinase activity and are useful for treating disorders mediated by Raf kinases.
