72470-43-0Relevant articles and documents
An efficient synthesis, characterization and biological activity of novel Schiff bases of 2-aryl-1H-benzo[d]imidazole-4-carbohydrazide derivatives
Gupta, Premlata,Jat, Kamal,Solanki, Vijendra Singh,Shrivastava, Ruchi
, p. 173 - 179 (2020/06/29)
A series of N′-aryllidene-2-aryl-1H-benzo[d]imidazole-4-carbohydrazide (Schiff bases) 3a1-3d4 were synthesized by condensation reaction of 2-aryl-1H-benzo[d]imidazole-4-carbohydrazide (2a-2d) with substituted aromatic aldehyde. The c
Discovery of TD-8954, a clinical stage 5-HT4 receptor agonist with gastrointestinal prokinetic properties
McKinnell, R. Murray,Armstrong, Scott R.,Beattie, David T.,Fatheree, Paul R.,Long, Daniel D.,Marquess, Daniel G.,Shaw, Jeng-Pyng,Vickery, Ross G.
, p. 4210 - 4215 (2013/07/25)
The discovery of a series of 5-HT4 receptor agonists based on a novel 2-alkylbenzimidazole aromatic core is described. Optimization of the 2-substituent of the benzimidazole ring led to a series of agonists with subnanomolar binding affinity and moderate-to-high intrinsic activity relative to that of 5-HT. Consistent with our previously described multivalent design approach to this target, subsequent optimization of the linker and secondary binding group regions of the series afforded compound 18 (TD-8954), a potent and selective 5-HT4 receptor agonist in vitro with demonstrated prokinetic activity in multiple species.
AROMATIC AMINO ACID DERIVATIVES AND MEDICINAL COMPOSITIONS
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Page 28, (2010/02/09)
An aromatic amino acid derivative represented by the formula ( I ) or its pharmacologically acceptable salt: wherein,R1 is a hydrogen atom or an amino-protecting group,R2 is a halogen atom or an alkyl, aralkyl or aryl group,R3 is 1○ a hydrogen atom, 2○ an aroylamino group, 3○ a phenyl group substituted with lower alkyl, phenyl, phenoxy, etc. 4○ a naphthyl or tetrahydronaphthyl group optionally substituted with hydroxy, lower alkoxy or di(lower)alkylamino, 5○ an unsaturated mono-cyclic heterocyclic group containing N, O and/or S substituted with lower alkyl, phenyl, naphthyl or tetrahydroquinolyl, 6○ an unsaturated or partially saturated condensed heterocyclic group containing N, O and/or S, optionally substituted with oxo, carboxy, amino, lower alkyl, etc.; X is a halogen atom, an alkyl group or an alkoxy group; Y is oxygen atom or nitrogen atom; 1 is 0 or 1; m is 0, 1 or 2; n is an integer of 0-5. This compound can inhibit a transporter (LAT1) of essential amino acid which is one of main nutrition for cancer cells and accordingly cause drain of the essential amino acid on the cancer cells and finally can prohibit the multiplication of cancer cells.