41888-65-7Relevant academic research and scientific papers
Orthopalladation of GFP-Like Fluorophores Through C–H Bond Activation: Scope and Photophysical Properties
Collado, Sandra,Pueyo, Alejandro,Baudequin, Christine,Bischoff, Laurent,Jiménez, Ana Isabel,Cativiela, Carlos,Hoarau, Christophe,Urriolabeitia, Esteban P.
, p. 6158 - 6166 (2018/11/23)
The luminescence of oxazolones R1-C6H4CH=CC(O)O-CN(R2) (1a–1j) and imidazolones R1-C6H4CH=CC(O)NR3CN(R2) (1k–1q) has been examined. The new GFP-like imidazo
New compounds having skin whitening, antioxidant and PPAR activity, and medical use thereof
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Paragraph 0343; 0346; 0358, (2017/04/14)
PURPOSE: A novel compound with skin whitening, antioxidation, and PPAR activation effects, and a medical use thereof are provided to be used for a pharmaceutical composition or a cosmetic product. CONSTITUTION: A compound is denoted by chemical formula 1. A skin whitening composition contains the compound as an active ingredient. An antioxidative composition for preventing or treating oxidative diseases contains the compound of chemical formula 1 as an active ingredient. The oxidative diseases are selected among skin aging, pigmentation, wrinkling, psoriasis, or eczema. The composition prevents or treats diseases which are regulated by PPAR(peroxisome proliferator-activated receptor) activity. The PPAR includes PPAR alpha or PPAR gamma.
Resolving Electronic Transitions in Synthetic Fluorescent Protein Chromophores by Magnetic Circular Dichroism
Cowie, Thomas Y.,?afa?ík, Martin,?ebestík, Jaroslav,Pohl, Radek,Bou?, Petr,?těpánek, Petr
, p. 2348 - 2354 (2016/08/27)
The detailed electronic structures of fluorescent chromophores are important for their use in imaging of living cells. A series of green fluorescent protein chromophore derivatives is examined by magnetic circular dichroism (MCD) spectroscopy, which allows the resolution of more bands than plain absorption and fluorescence. Observed spectral patterns are rationalized with the aid of time-dependent density functional theory (TDDFT) computations and the sum-over-state (SOS) formalism, which also reveals a significant dependence of MCD intensities on chromophore conformation. The combination of organic and theoretical chemistry with spectroscopic techniques also appears useful in the rational design of fluorescence labels and understanding of the chromophore's properties. For example, the absorption threshold can be heavily affected by substitution on the phenyl ring but not much on the five-member ring, and methoxy groups can be used to further tune the electronic levels.
NOVEL COMPOUND HAVING SKIN-WHITENING, ANTI-OXIDIZING AND PPAR ACTIVITIES AND MEDICAL USE THEREFOR
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Paragraph 0234; 0236; 0242, (2014/02/16)
Provided are a novel compound having skin-whitening, anti-oxidizing and PPAR activities and a medical use thereof, and the compound has skin-whitening activities for the suppression of tyrosinase, and accordingly, is useful for use in skin-whitening pharmaceutical composition or cosmetic products; has anti-oxidant activities, and accordingly, is useful for the prevention and treatment of skin-aging; and has PPAR activities, and in particular, PPARα and PPARγ activities, and accordingly, is useful for use in pharmaceutical compositions or health foods which are effective for the prevention and treatment of obesity, metabolic disease, or cardiovascular disease.
Asymmetric synthesis of unnatural amino acids and tamsulosin chiral intermediate
Arava, Veera Reddy,Amasa, Srinivasulu Reddy,Goud Bhatthula, Bharat Kumar,Kompella, Laxmi Srinivas,Matta, Venkata Prasad,Subha
supporting information, p. 2892 - 2897 (2013/09/02)
An efficient and enantioselective hydrogenation of N-acetylamino phenyl acrylic acids was successfully developed by using ruthenium catalyst. This methodology is important in the field of pharmaceuticals and provides a new process for the preparation of unnatural amino acids and tamsulosin chiral intermediate.
Defining the mechanism of action and enzymatic selectivity of psammaplin A against its epigenetic targets
Baud, Matthias G. J.,Leiser, Thomas,Haus, Patricia,Samlal, Sharon,Wong, Ai Ching,Wood, Robert J.,Petrucci, Vanessa,Gunaratnam, Mekala,Hughes, Siobhan M.,Buluwela, Lakjaya,Turlais, Fabrice,Neidle, Stephen,Meyer-Almes, Franz-Josef,White, Andrew J. P.,Fuchter, Matthew J.
scheme or table, p. 1731 - 1750 (2012/04/23)
Psammaplin A (11c) is a marine metabolite previously reported to be a potent inhibitor of two classes of epigenetic enzymes: histone deacetylases and DNA methyltransferases. The design and synthesis of a focused library based on the psammaplin A core has been carried out to probe the molecular features of this molecule responsible for its activity. By direct in vitro assay of the free thiol generated upon reduction of the dimeric psammaplin scaffold, we have unambiguously demonstrated that 11c functions as a natural prodrug, with the reduced form being highly potent against HDAC1 in vitro (IC50 0.9 nM). Furthermore, we have shown it to have high isoform selectivity, being 360-fold selective for HDAC1 over HDAC6 and more than 1000-fold less potent against HDAC7 and HDAC8. SAR around our focused library revealed a number of features, most notably the oxime functionality to be important to this selectivity. Many of the compounds show significant cytotoxicity in A549, MCF7, and W138 cells, with the SAR of cytotoxicity correlating to HDAC inhibition. Furthermore, compound treatment causes upregulation of histone acetylation but little effect on tubulin acetylation. Finally, we have found no evidence for 11c functioning as a DNMT inhibitor.
Pseudo-peptides derived from isomannide: Inhibitors of serine proteases
Barros, Thalita G.,Pinheiro, Sergio,Williamson,Tanuri, Amilcar,Gomes Jr.,Pereira, Helena S.,Brindeiro,Neto, Jose B. A.,Antunes,Muri, Estela M. F.
scheme or table, p. 701 - 709 (2010/08/05)
In this paper, we describe the synthesis of a novel class of pseudo-peptides derived from isomannide and several oxazolones as potential inhibitors of serine proteases as well as preliminary pharmacological assays for hepatitis C. Hepatitis C, dengue and West Nile fever are among the most important flaviviruses that share one important serine protease enzyme. Serine proteases belong to the most studied class of proteolytic enzymes and are a primary target in the drug development field. Several pseudo-peptides were obtained in good yields from the reaction of isomannide and oxazolones, and their anti-HCV potential using the HCV replicon-based assay was shown.
The total synthesis of fukiic acid, an HIV-1 integrase inhibitor
Queffelec, Clemence,Bailly, Fabrice,Mbemba, Gladys,Mouscadet, Jean-Francois,Debyser, Zeger,Witvrouw, Myriam,Cotelle, Philippe
, p. 2268 - 2271 (2008/12/23)
A successful synthesis of fukiic acid is described in 7% overall yield (6 steps from veratraldehyde). rac-Fukiic acid was found to be a potent inhibitor of HIV-1 integrase but did not reveal any antiviral activity in the MT-4 cells assay.
Oxazolones: New tyrosinase inhibitors; synthesis and their structure-activity relationships
Khan, Khalid Mohammed,Mughal, Uzma Rasool,Khan, Mahmud Tareq Hassan,Zia-Ullah,Perveen, Shahnaz,Iqbal Choudhary, Muhammad
, p. 6027 - 6033 (2007/10/03)
The tyrosinase inhibitory potential of seventeen synthesized oxazolone derivatives has been evaluated and their structure-activity relationships developed in the present work. All the synthesized derivatives, 3-19, demonstrated excellent in vitro tyrosina
Electron transfer-initiated and highly selective photocyclization of N-acyl-α-dehydroarylalaninamides to 3,4-dihydroquinolinone derivatives
Maekawa, Kei,Fujita, Kunio,Iizuka, Katsuyuki,Igarashi, Tetsutaro,Sakurai, Tadamitsu
, p. 117 - 131 (2007/10/03)
The irradiation of (Z)-N-acyl-α-dehydroarylalaninamides [(Z)-1] in methanol containing 1,8-diazabicyclo[5.4.0]undec-7-ene gave substituted 3,4-dihydro-2-quinolinones (2) in high yields along with minor amounts of 2-quinolinone (3) and 4,5-dihydrooxazole (
