- Dynamic multicolor protein labeling in living cells
-
Yellow Fluorescence-Activating and absorption-Shifting Tag (Y-FAST, hereafter called FAST) is a 14 kDa protein tag giving a bright green-yellow fluorescent complex upon interaction with the fluorogenic dye 4-hydroxy-3-methylbenzylidene rhodanine (HMBR). H
- Li, Chenge,Plamont, Marie-Aude,Sladitschek, Hanna L.,Rodrigues, Vanessa,Aujard, Isabelle,Neveu, Pierre,Le Saux, Thomas,Jullien, Ludovic,Gautier, Arnaud
-
-
Read Online
- Design and microwave synthesis of new (5z) 5-arylidene-2-thioxo-1,3-thiazolinidin-4-one and (5z) 2-amino-5-arylidene-1,3-thiazol-4(5h)-one as new inhibitors of protein kinase dyrk1a
-
Here, we report on the synthesis of libraries of new 5-arylidene-2-thioxo-1,3-thiazolidin-4-ones 3 (twenty-two compounds) and new 2-amino-5-arylidene-1,3-thiazol-4(5H)-ones 5 (twenty-four compounds) with stereo controlled Z-geometry under microwave irradi
- Bazureau, Jean-Pierre,Bourahla, Khadidja,Carreaux, Fran?ois,Charlier, Thierry,Durieu, Emilie,Guihéneuf, Solène,Le Guével, Rémy,Limanton, Emmanuelle,Lozach, Olivier,Meijer, Laurent,Paquin, Ludovic,Rahmouni, Mustapha
-
supporting information
(2021/11/08)
-
- Environmentally friendly approach to knoevenagel condensation of rhodanine in choline chloride: Urea deep eutectic solvent and qsar studies on their antioxidant activity
-
A series of rhodanine derivatives was synthesized in the Knoevenagel condensation of rhodanine and different aldehydes using choline chloride:urea (1:2) deep eutectic solvent. This environmentally friendly and catalyst free approach was very effective in
- Molnar, Maja,Brahmbhatt, Harshad,Rastija, Vesna,Pavi?, Valentina,Komar, Mario,Karna?, Maja,Babi?, Jurislav
-
-
- Molecular modeling of drug-pathophysiological Mtb protein targets: Synthesis of some 2-thioxo-1, 3-thiazolidin-4-one derivatives as anti-tubercular agents
-
Twenty novel 2-thioxo-1, 3-thiazolidin-4-one derivatives (5a-5t) were synthesized and evaluated for their antitubercular activity. The structure of the compounds was confirmed by IR, NMR and Mass Spectroscopy methods. In addition, single-crystal X-ray diffraction was performed for compound 5a. All the synthesized compounds were screened for their in-vitro antimycobacterial activity against MTB (H37RV, ATCC No: 27294) by Alamar Blue assay method. Compounds 5r, 5k, 5t displayed most potent in-vitro activity with MICs of 0.05, 0.1, 0.2 μg/ml concentrations respectively which are comparatively potent than the standards. Molecular docking and dynamics simulations were performed to find out the plausible mechanism of the titled compounds.
- Noorulla,Suresh, Ayyadurai Jerad,Devaraji, Vinod,Mathew, Bijo,Umesh, Devi
-
p. 682 - 696
(2017/07/13)
-
- FLUOROGEN ACTIVATING AND SHIFTING TAG (FAST)
-
The present invention relates to a functional derivative of a Photoactive Yellow Protein (PYP), or a functional fragment thereof, for fluorescently labelling particles, e.g. proteins, or surfaces, which is capable of binding reversibly a fluorogenic chrom
- -
-
Page/Page column 48; 49
(2016/01/25)
-
- New compounds having skin whitening, antioxidant and PPAR activity, and medical use thereof
-
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.
- -
-
Paragraph 0280; 0287
(2017/04/14)
-
- Microwave-Assisted condensation reactions of acetophenone derivatives and activated methylene compounds with aldehydes catalyzed by boric acid under solvent-free conditions
-
We here disclosed a new protocol for the condensation of acetophenone derivatives and active methylene compounds with aldehydes in the presence of boric acid under microwave conditions. Implementation of the reaction is simple, healthy and environmentally
- Brun, Elodie,Safer, Abdelmounaim,Carreaux, Franois,Bourahla, Khadidja,L'Helgoua'ch, Jean-Martial,Bazureau, Jean-Pierre,Villalgordo, Jose Manuel
-
p. 11617 - 11631
(2015/08/06)
-
- NOVEL COMPOUND HAVING SKIN-WHITENING, ANTI-OXIDIZING AND PPAR ACTIVITIES AND MEDICAL USE THEREFOR
-
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.
- -
-
Paragraph 0203; 0207
(2014/02/16)
-
- Facile and convenient synthesis of 5-arylalkylidenerhodanines by electrocatalytic crossed aldol condensation
-
An electrochemically induced catalytic crossed Aldol condensation of one equivalent of rhodanine with various aromatic aldehydes and ketones in ethanol in an undivided cell in the presence of sodium bromide as an electrolyte results in the formation of th
- Veisi, Hojat,Vafajoo, Zahra,Maleki, Behrooz,Maghsoodlou, Malek Taher
-
p. 672 - 677
(2013/07/26)
-
- Privileged scaffolds or promiscuous binders: A comparative study on rhodanines and related heterocycles in medicinal chemistry
-
Rhodanines and related five-membered heterocycles with multiple heteroatoms have recently gained a reputation of being unselective compounds that appear as "frequent hitters" in screening campaigns and therefore have little value in drug discovery. However, this judgment appears to be based mostly on anecdotal evidence. Having identified various rhodanines and related compounds in screening campaigns, we decided to perform a systematic study on their promiscuity. An amount of 163 rhodanines, hydantoins, thiohydantoins, and thiazolidinediones were synthesized and tested against several targets. The compounds were also characterized with respect to aggregation and electrophilic reactivity, and the binding modes of rhodanines and related compounds in published X-ray cocrystal structures were analyzed. The results indicate that the exocyclic, double bonded sulfur atom in rhodanines and thiohydantoins, in addition to other structural features, offers a particularly high density of interaction sites for polar interactions and hydrogen bonds. This causes a promiscuous behavior at concentrations in the "screening range" but should not be regarded as a general knockout criterion that excludes such screening hits from further development. It is suggested that special criteria for target affinity and selectivity are applied to these classes of compounds and that their exceptional and potentially valuable biomolecular binding properties are consequently exploited in a useful way.
- Mendgen, Thomas,Steuer, Christian,Klein, Christian D.
-
supporting information; experimental part
p. 743 - 753
(2012/03/11)
-
- Evaluation of dihydropyrimidin-(2H)-one analogues and rhodanine derivatives as tyrosinase inhibitors
-
A series of dihydropyrimidin-(2H)-one analogues and rhodanine derivatives were synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were evaluated. The results showed that some of the synthesized compounds exhibited
- Liu, Jinbing,Wu, Fengyan,Chen, Lingjuan,Hu, Jianming,Zhao, Liangzhong,Chen, Changhong,Peng, Liwang
-
supporting information; experimental part
p. 2376 - 2379
(2011/05/15)
-
- Synthesis and characterization of (Z)-5-arylmethylidenerhodanines with photosynthesis-inhibiting properties
-
A series of rhodanine derivatives was prepared. The synthetic approach, analytical and spectroscopic data of all synthesized compounds are presented. Lipophilicity of all the discussed rhodanine derivatives was analyzed using the RP-HPLC method. The compo
- Opletalova, Veronika,Dolezel, Jan,Kralova, Katarina,Pesko, Matus,Kunes, Jiri,Jampilek, Josef
-
experimental part
p. 5207 - 5227
(2011/08/06)
-
- Solvent-free synthesis of 5-benzylidene-2-thioxothiazolidin-4-ones and thiazolidine-2,4-diones catalysed by glycine under microwave irradiation
-
A novel and clean synthesis of 5-benzylidene-2-thioxothiazolidin-4-ones and thiazolidine-2,4-diones has been achieved in good yields by condensation of aromatic aldehydes with rhodanine or thiazolidine-2,4-dione under microwave irradiation using glycine a
- Yang, Ben-Yong,Yang, De-Hong
-
experimental part
p. 238 - 239
(2011/07/09)
-
- Rhodanine derivatives as novel inhibitors of PDE4
-
The discovery, synthesis and in vitro activity of a novel series of rhodanine based phosphodiesterase-4 (PDE4) inhibitors is described. Structure-activity relationship studies directed toward improving potency led to the development of submicromolar inhibitors 2n and 3i (IC50 = 0.89 & 0.74 μM). The replacement of rhodanine with structurally related heterocycles was also investigated and led to the synthesis of pseudothiohydantoin 7 (IC50 = 0.31 μM).
- Irvine, Mark W.,Patrick, Graham L.,Kewney, Justin,Hastings, Stuart F.,MacKenzie, Simon J.
-
p. 2032 - 2037
(2008/12/21)
-
- A practical access to novel 2-amino-5-arylidene-1,3-thiazol-4(5H)-ones via sulfur/nitrogen displacement under solvent-free microwave irradiation
-
A new effective approach to the synthesis of a small library of 2-amino-5-arylidene-1,3-thiazol-4(5H)-ones was reported using solvent-free reaction conditions under microwave irradiation. In the first step, rhodanines were subjected to Knoevenagel condens
- Bourahla, Khadidja,Derdour, A?cha,Rahmouni, Mustapha,Carreaux, Fran?ois,Bazureau, Jean Pierre
-
p. 5785 - 5789
(2008/02/09)
-
- PHARMACEUTICAL COMPOSITIONS
-
Compounds for use in compositions and methods for modulating the activity of nuclear receptors are provided. In particular, compounds for use in compositions and methods for modulating the estrogen related receptors are provided. In one embodiment, the compounds provided herein are ERR modulators. In another embodiment, the compounds provided herein are agonists, partial agonists, antagonists. or inverse agonists of ERR or ERR?. In certain embodiments, the compounds of the invention, as described above in the Summary of the Invention, are compounds of formula (I).
- -
-
Page/Page column 60-61
(2008/06/13)
-
- Method for treating multiple sclerosis
-
Provided is a method of treating multiple sclerosis employing certain aryl-substituted rhodanines.
- -
-
-
- COMPOUNDS USEFUL AS HYPOGLYCEMIC AGENTS AND FOR TREATING ALZHEIMER'S DISEASE
-
Provided are methods for treating hyperglycemia and Alzheimer's disease utilizing certain rhodanine derivatives. Certain of the rhodanine derivatives utilized in the instant methods are novel and, accordingly, such compounds and pharmaceutical formulation
- -
-
-