- Structural Modifications of Benzimidazoles via Multi-Step Synthesis and Their Impact on Sirtuin-Inhibitory Activity
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Benzimidazole derivatives have been shown to possess sirtuin-inhibitory activity. In the continuous search for potent sirtuin inhibitors, systematic changes on the terminal benzene ring were performed on previously identified benzimidazole-based sirtuin i
- Yoon, Yeong Keng,Choon, Tan Soo
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- Metal catalyst-free amination of 2-chloro-5-nitrobenzoic acid in superheated water
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A series of N-arylanthranilic acid derivatives were synthesised by amination of 2-chloro-5-nitrobenzoic acid with various arylamine in superheated water with potassium carbonate as base. Good yields were achieved within 2-3 h at 150-190 °C. The results indicated that this metal catalyst-free method is a simple, environmentally-friendly and efficient synthesis of N-phenylanthranilic acid derivatives. Furthermore, it will work with an alkylamine and phenol.
- Lan, Cong,Xia, Zhi-Ning,Li, Zheng-Hua,Liang, Rong-Hui
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p. 726 - 728
(2013/02/23)
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- AGENT FOR TREATMENT OR PREVENTION OF DISEASES ASSOCIATED WITH ACTIVITY OF NEUROTROPHIC FACTORS
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A compound depicted by the formula below, or a pharmaceutically acceptable salt or solvate thereof. wherein, R1 represents (1) a C3-6 alkyl group,(2) a C1-6 alkyl group substituted with one or more substituent group(s) sel
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Page/Page column 43
(2012/04/17)
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- Synthesis of 1-heterocyclic aminomethyl-3-(4'-anilino-3'-nitrobenzoyl hydrazono)- 2-indolinones as antifilarial and CNS active agents
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A series of 1-heterocyclic aminomethyl-3-(4'-anilino-3'-nitrobenzoyl hydrazono)-2-indolinones (VIa-VIl) have been synthesized and tested for their antifilarial and CNS activity. The compounds VIa, VId, VIg have exhibited 75.8, 78.2 and 70.5 % microfilaricidal activity respectively.
- Beg,Gupta
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p. 1569 - 1572
(2012/01/06)
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- 3-Nitro-4-amino benzoic acids and 6-amino nicotinic acids are highly selective agonists of GPR109b
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A series of 3-nitro-4-substituted-aminobenzoic acids were prepared and found to act as potent and highly selective agonists of the orphan human GPCR GPR109b, a low affinity receptor for niacin. No activity was observed at the closely homologous high affinity niacin receptor, GPR109a. A second series, comprising 6-amino-substituted nicotinic acids was, also prepared and several analogues showed comparable activity to the nitroaryl series.
- Skinner, Philip J.,Cherrier, Martin C.,Webb, Peter J.,Sage, Carleton R.,Dang, Huong T.,Pride, Cameron C.,Chen, Ruoping,Tamura, Susan Y.,Richman, Jeremy G.,Connolly, Daniel T.,Semple, Graeme
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p. 6619 - 6622
(2008/04/02)
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- Structure-activity relationships for 1-phenylbenzimidazoles as selective ATP site inhibitors of the platelet-derived growth factor receptor
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1-Phenylbenzimidazoles are shown to be a new class of ATP-site inhibitors of the platelet-derived growth factor receptor (PDGFR). Structure- activity relationships (SARs) are narrow, with closely related heterocycles being inactive. A systematic study of
- Palmer, Brian D.
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p. 5457 - 5465
(2007/10/03)
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- 1-Aminomethyl-3-(4'-arylamino-3'-nitrobenzoylhydrazono)-2-indolinones as DEC analogs and their anifilarial activity
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Acid catalysed condensation of 4-arylamino-3-nitrobenzoylhydrazines (IVa-d) with indoline-2,3-dione followed by aminomethylation using N-methylpiperazine, morpholine and piperidine as the amino components furnishes the title compounds (VIa-l) in good yiel
- Varma, Rajendra S.,Shukla, Amita,Fatma, Nigar,Chatterjee, R. K.
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p. 347 - 351
(2007/10/02)
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- Micellar Catalysis of Organic Reactions. 29. SNAr Reactions with Neutral Nucleophiles
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The reaction of a number of nitroactivated halobenzoates (1-4) with some primary and tertiary amines has been studied in the presence of micelles of cetyltrimethylammonium bromide (CTAB) and in water.With primary amines aminodehalogenation was observed, and it was found that if the reaction center of the aromatic substrate was located at the micelle water interface (compounds 1 and 2) the reaction was catalyzed by CTAB, but if the reaction center was more deeply buried into the micelle interior the reaction with aniline was inhibited by micelles of CTAB (compounds 3 and 4), while CTAB had little effecton the reaction of n-propylamine with compound 4.With the more sterically bulky tertiary amines, hydroxydehalogenation was observed rather than aminodehalogenation, and the reactions were all catalyzed by CTAB, but for the substrate with a more deeply buried reaction center (compound 4), the catalysis was stronger than for that with a reaction center at or near the interface (compound 2).The mechanism of hydroxydehalogenation was found to be specific base catalysis by the tertiary amine.Thus, the observation of micellar catalysis or inhibition of these reactions depends on the orientation of the organic substrate within the micellar aggreagate and the reaction product, amine or phenol, depends on the streric bulk of the amine at least for the compounds investigated here which contain two substituents ortho to the reaction center.
- Broxton, Trevor J.,Marcou, Victor
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p. 1041 - 1044
(2007/10/02)
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