926294-00-0Relevant articles and documents
Synthesis of resveratrol derivatives as new analgesic drugs through desensitization of the TRPA1 receptor
Nakao, Syuhei,Mabuchi, Miyuki,Wang, Shenglan,Kogure, Yoko,Shimizu, Tadashi,Noguchi, Koichi,Tanaka, Akito,Dai, Yi
supporting information, p. 3167 - 3172 (2017/06/13)
A series of 31 resveratrol derivatives was designed, synthesized and evaluated for activation and inhibition of the TRPA1 channel. Most acted as activators and desensitizers of TRPA1 channels like resveratrol or allyl isothiocyanate (AITC). Compound 4z (HUHS029) exhibited higher inhibitory activity than resveratrol with an IC50 value of 16.1?μM. The activity of 4z on TRPA1 was confirmed in TRPA1-expressing HEK293 cells, as well as in rat dorsal root ganglia neurons by a whole cell patch clamp recording. Furthermore, pretreatment with 4z exhibited an analgesic effect on AITC-evoked TRPA1-related pain behavior in vivo.
The application of template selectophores for the preparation of molecularly imprinted polymers
Danylec, Basil,Schwarz, Lachlan J.,Harris, Simon J.,Boysen, Reinhard I.,Hearn, Milton T. W.
supporting information, p. 17601 - 17613 (2015/10/12)
Molecularly imprinted polymers are versatile materials with wide application scope for the detection, capture and separation of specific compounds present in complex feed stocks. A major challenge associated with their preparation has been the need to sacrifice one mole equivalent of the template molecule to generate the complementary polymer cavities that selectively bind the target molecule. Moreover, template molecules can often be difficult to synthesise, expensive or lack stability. In this study, we describe a new approach, directed at the use of synthetic selectophores, chosen as readily prepared and low cost structural analogues with recognition groups in similar three-dimensional arrangements as found in the target molecule. To validate the approach, a comparative study of selectophores related to the polyphenolic compound (E)-resveratrol has been undertaken using traditional and green chemical synthetic approaches. These molecular mimic compounds were employed as polymer templates and also as binding analytes to interrogate the recognition sites associated with the molecularly imprinted polymers. Importantly, the study confirms that the use of selectophores has the potential to confer practical advantages, including access to more efficient methods for selection and preparation of suitable template molecules with a broader range of molecular diversity, as well as delivering imprinted polymers capable of recognizing the target compound and structurally related products.
Design, synthesis, biological and structural evaluation of functionalized resveratrol analogues as inhibitors of quinone reductase 2
St. John, Sarah E.,Jensen, Katherine C.,Kang, Soosung,Chen, Yafang,Calamini, Barbara,Mesecar, Andrew D.,Lipton, Mark A.
, p. 6022 - 6037 (2013/09/23)
Resveratrol (3,5,4′-trihydroxylstilbene) has been proposed to elicit a variety of positive health effects including protection against cancer and cardiovascular disease. The highest affinity target of resveratrol identified so far is the oxidoreductase enzyme quinone reductase 2 (QR2), which is believed to function in metabolic reduction and detoxification processes; however, evidence exists linking QR2 to the metabolic activation of quinones, which can lead to cell toxicity. Therefore, inhibition of QR2 by resveratrol may protect cells against reactive intermediates and eventually cancer. With the aim of identifying novel inhibitors of QR2, we designed, synthesized, and tested two generations of resveratrol analogue libraries for inhibition of QR2. In addition, X-ray crystal structures of six of the resveratrol analogues in the active site of QR2 were determined. Several novel inhibitors of QR2 were successfully identified as well as a compound that inhibits QR2 with a novel binding orientation.
N-Arylbenzamides: Extremely simple scaffolds for the development of novel estrogen receptor agonists
Caldarelli, Antonio,Minazzi, Paolo,Canonico, Pier Luigi,Genazzani, Armando A.,Giovenzana, Giovanni B.
, p. 148 - 152 (2013/04/23)
The research of estrogen receptor (ER) ligands has benefited in the last decade from the implementation of combinatorial chemistry. The general pharmacophore has been identified and subsequently a multitude of compounds have been synthesized. Surprisingly, up to now simple amides have not been taken into consideration. Here we show that amides resulting from the condensation of hydroxybenzoic acids with aminophenols result in compounds retaining the pharmacophore structure of an ER ligand with a clear estrogenic activity.
MOLECULARLY IMPRINTED POLYMERS
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, (2012/03/12)
The present invention provides methods of designing molecularly imprinted polymers (MIPs) which have applications in extracting bioactive compounds from a range of bioprocessing feedstocks and wastes. The present invention is further directed to MIPs designed by the methods of the present invention.
Hydroxybenzamide Derivatives, the Method For Preparing Thereof and the Cosmetic Composition Containing the Same
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Page/Page column 3, (2008/12/08)
Disclosed is a hydroxybenzamide derivative represented by the following Formula. A method for preparing the same and a cosmetic composition comprising the same are also disclosed. More particularly, the hydroxybenzamide derivative is obtained by reacting
HYDROXYBENZAMIDE DERIVATIVES, THE METHOD FOR PREPARING THEREOF AND THE COSMETIC COMPOSITION CONTAINING THE SAME
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Page/Page column 6-7; 9, (2010/11/26)
Disclosed is a hydroxybenzamide derivative represented by the following Formula (1). A method for preparing the same and a cosmetic composition comprising the same are also disclosed. More particularly, the hydroxybenzamide derivative is obtained by react
