71198-74-8Relevant academic research and scientific papers
Concise Modular Synthesis of Thalassotalic Acids A-C
Schulz, Joseph M.,Lanovoi, Hunter T.,Ames, Amanda M.,McKegg, Phillip C.,Patrone, James D.
, p. 1045 - 1048 (2019/05/14)
The novel N-acyldehydrotyrosine analogues known as thalassotalic acids A-C were isolated from a marine bacterium by Deering et al. in 2016. These molecules were shown to have tyrosinase inhibition activity and thus are an attractive set of molecules for further study and optimization. To this end, a concise and modular synthesis has been devised and executed to produce thalassotalic acids A-C and two unnatural analogues. This synthesis has confirmed the identity and inhibitory data of thalassotalic acids A-C, more potent synthetic analogues (IC50 = 65 μM), and provides a route for further structure-activity relationship studies to optimize these molecules.
Stereoselective Intermolecular [2 + 2] Cycloadditions of Erlenmeyer-Pl?chl Azlactones Using Visible Light Photoredox Catalysis
Marra, Isabellar F. S.,De Almeida, Angelina M.,Silva, Larissa P.,De Castro, Pedro P.,Corrêa, Charlane C.,Amarante, Giovanni Wilson
, p. 15144 - 15154 (2018/12/14)
The first report of the preparation of symmetric and nonsymmetric diaminotruxinic derivatives through the photoredox [2 + 2] cycloadditions of Erlenmeyer azlactones is described, affording the desired compounds in high regio- and diastereocontrol (only head-to-head coupling). Mechanistic studies by DFT suggest that the reaction proceeds through a neutral photocatalytic pathway.
DUAL EMISSION FLUORESCENT COMPOUNDS
-
Page/Page column 44, (2017/09/19)
The invention relates to a dual emission fluorescent compound comprising a chromophore suitable for exhibiting an emission at a first wavelength from an excited state; wherein the compound further comprises one or more groups suitable for inducing a structural rearrangement in the molecule on formation of the excited state, wherein the structural rearrangement stabilises at least a second electromagnetic emission at a second wavelength, such that dual emission is observable at room temperature. Such dual emission allows for the super sensitive ratiometric quantification of analytes.
An efficient and concise method to synthesize locked GFP chromophore analogues
Chatterjee, Soumit,Karuso, Peter
, p. 5197 - 5200 (2016/11/13)
A series of GFP analogues, which are fluorescent in the solid state at room temperature, but weakly fluorescent in solution, have been synthesized via an oxazolone formation process that involves a condensation reaction in the presence of a Lewis acid following a Knoevenagel condensation. A ring opened intermediate is formed which cyclizes readily upon heating to produce the imidazolinone. This method is faster, simpler and produces higher yields than alternative methods. A few analogues represent locked GFP derivatives where the exocyclic single bond rotation has been stopped. Weak fluorescence, even after stopping single bond rotation, indicates that restriction of conformation is not effectively controlled and that the double bond rotation is solely responsible for the major non-radiative pathway.
New compounds having skin whitening, antioxidant and PPAR activity, and medical use thereof
-
Paragraph 0498-0499, (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.
NOVEL COMPOUND HAVING SKIN-WHITENING, ANTI-OXIDIZING AND PPAR ACTIVITIES AND MEDICAL USE THEREFOR
-
Paragraph 0312; 0313, (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.
Facile synthesis of 4-arylidene-5-imidazolinones as synthetic analogs of fluorescent protein chromophore
Lee, Cheng-Yu,Chen, Yun-Chung,Lin, Hao-Chun,Jhong, Yuandong,Chang, Chih-Wei,Tsai, Ching-Hua,Kao, Chai-Lin,Chien, Tun-Cheng
supporting information; experimental part, p. 5898 - 5907 (2012/09/07)
A facile and effective synthesis for a wide variety of 4-arylidene-5- imidazolinone derivatives was developed. 4-Arylidene-5-oxazolinones were prepared by Erlenmeyer azlactone synthesis from N-acylglycines and arylaldehydes. The ring-opening reactions of the 4-arylidene-5-oxazolinones with primary amines afforded 2-acylamino-3-arylacrylamides in excellent yields. A new dehydrative cyclization of the 2-acylamino-3-arylacrylamides in pyridine under reflux furnished the corresponding 4-arylidene-5-imidazolinones in good yields.
New methacrylic oxazolone and thiazolidinone containing polymers for nonlinear opticalApplications
Smokal, Vitaliy,Kolendo, Aleksey,Krupka, Oksana,Derkowska, Beata,Czaplicki, Robert,Sahraoui, Bouchta
experimental part, p. 263/[1011]-270/[1018] (2009/10/11)
Oxazalone and thiazolidinone derivatives were synthesized and their physicochemical properties are determined by absorption, HNMR spectroscopies. The third order nonlinear optical properties of oxazolone and thiazolidinone containing compounds were investigated in solutions using degenerate four wave mixing (DFWM) method at 532 nm.
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
Montmorillonite K-10 mediated Erlenmeyer synthesis of 4-arylmethylene-2- phenyl-5(4H)-oxazolones
Karade,Shirodkar,Dhoot,Waghmare
, p. 46 - 47 (2007/10/03)
Aromatic aldehydes and hippuric acid in acetic anhydride undergoes classical Erlenmeyer synthesis in the presence of a catalytic amount of Montmorillonite K-10 to afford the corresponding azlactones in excellent yields with high selectivity. The azlactone
