4654-08-4Relevant academic research and scientific papers
Ion-transport activity of phenylpentanoic acids occurring in the roots of Athyrium yokoscense
Hiraga, Yoshikazu,Kurokawa, Masashi,Guo, Jian-Ru,Suga, Takayuki
, p. 958 - 960 (1999)
5-(3′-Hydroxyphenyl)pentanoic add (1) and 5-(3′-methoxyphenyl)pentanoic acid (2) occurring in the roots of Athyrium yokoscense showed transport activity to alkaline and alkaline earth metal ions and heavy divalent metal ions.
Racemic total synthesis of dactyloidin and demethyldactyloidin through the dl-proline-catalyzed Knoevenagel condensation/[4 + 2] cycloaddition cascade
Tan, Haibo,Liu, Hongxin,Chen, Xinzheng,Chen, Huiyu,Qiu, Shengxiang
, p. 9977 - 9983 (2015/10/12)
An efficient approach towards the first racemic total synthesis of dactyloidin (2) and demethyldactyloidin (3) is described. Their oxygen-bridged tricyclic ketal systems were rapidly constructed by using a remarkable biomimetic Knoevenagel condensation/[4 + 2] cycloaddition cascade as the critical strategy and the 1,5-dicarbonyl segment was assembled by Grignard addition.
RE12 derivatives displaying Vaccinia H1-related phosphatase (VHR) inhibition in the presence of detergent and their anti-proliferative activity against HeLa cells
Thuaud, Frederic,Kojima, Shuntaro,Hirai, Go,Oonuma, Kana,Tsuchiya, Ayako,Uchida, Takako,Tsuchimoto, Teruhisa,Sodeoka, Mikiko
, p. 2771 - 2782 (2014/05/06)
New derivatives of Vaccinia H1-related phosphatase (VHR) inhibitor RE12 (5) were designed by replacing the long straight alkyl chain with other hydrophobic functionalities containing two aromatic rings, with the aim of obtaining potent, cell-active inhibitors. We established a direct coupling reaction between tetronic acid derivative and thioimidate to prepare the RE derivatives 6a-6i efficiently. These compounds all showed VHR-inhibitory activity in the presence of 0.001% NP-40, whereas RE12 (5) was inactive under this condition, even at 100 μM. Further structure-activity studies focused on terminal substitution afforded trifluoromethyl derivative 6k (RE176) and nitro derivative 6l (RE177). The IC50 value of 6l in the presence of NP-40 was almost equivalent to that of RE12 (5) in its absence. Compound 6k (RE176) potently inhibited proliferation of HeLa cells.
G-PROTEIN-CONJUGATED RECEPTOR AGONIST
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Page/Page column 34, (2010/03/02)
Disclosed is a novel aralkyl carboxylic acid compound which has an agonistic activity on GPR-120 and/or GPR-40, particularly GPR-120, and is therefore useful as an appetite regulator, an anti-obesity agent, a therapeutic agent for diabetes, a pancreatic beta differentiating cell growth enhancer, a therapeutic agent for metabolic syndrome, a therapeutic agent for a gastrointestinal disease, a therapeutic agent for a neuropathy, a therapeutic agent for a mental disorder, a therapeutic agent for a pulmonary disease, a therapeutic agent for a pituitary hormone secretion disorder or a lipid flavoring/seasoning agent. The aralkyl carboxylic acid compound is represented by the general formula (I). (I) wherein the ring Q represents a pyridyl or the like; R1 represents a C1-6 alkyl group or the like; R2 represents a hydrogen atom, a C1-4 alkyl group or a C1-4 alkoxy group; m and n independently represent an integer of 1 to 5; and X represents an oxygen atom, a sulfur atom or - NR3- [wherein R3 represents a hydrogen atom or a C1-4 alkyl group].
Initial structure-activity relationship of a novel class of nonpeptidyl GnRH receptor antagonists: 2-arylindoles
Chu, Lin,Hutchins, Jennifer E.,Weber, Ann E.,Lo, Jane-Ling,Yang, Yi-Tien,Cheng, Kang,Smith, Roy G.,Fisher, Michael H.,Wyvratt, Matthew J.,Goulet, Mark T.
, p. 509 - 513 (2007/10/03)
A nonpeptidyl GnRH receptor antagonist (1), with a unique 2-arylindole core, was identified through the Merck in-house screening for binding affinity on the rat GnRH receptor. SAR studies directed toward the alkoxy-ethanolamine and 2-aryl groups resulted in a simpler lead structure with improved activity. This compound 50 exhibits a 60-fold improvement in binding activity over our initial lead 1.
Kinetics and Mechanism of the Alkaline Hydrolysis of Pentachlorophenyl ω-(p-Hydroxyphenyl)alkanoates
Cevasco, Giorgio,Thea, Sergio
, p. 269 - 272 (2007/10/03)
A kinetic study of the alkaline hydrolysis of pentachlorophenyl esters of ω-(p-hydroxyphenyl)alkanoic acids 3 shows that the dissociative route involving a spirodienone intermediate is not a feasible alternative to the normal associative BAC2 pathway.
Materials Chemistry of Chiral Macromolecules. 1. Synthesis and Phase Transitions
Moore, J. S.,Stupp, S. I.
, p. 3429 - 3441 (2007/10/02)
This paper describes work on synthesis of chiral macromolecules as part of a materials chemistry study which seeks to establish links in these systems among molecular structure, three-dimensional molecular organization, and properties.The basic materials
