52353-64-7Relevant academic research and scientific papers
Microwave-assisted synthesis of new 2-aryl and 2-alkylimidazolones and evaluation of their in vitro anticancer activity and their in vivo toxicity on zebrafish embryos
Bou Zeid, Samar,Hamade, Aline,Najjar, Fadia,Carreaux, Francois,Eid, Samar
, p. 2549 - 2560 (2021/02/05)
Herein we describe the synthesis of five new 2-aryl and 2-alkylimidazolone derivatives via an effective one-pot synthetic strategy assisted by microwave irradiations which allowed us to access the desired product in a reduced time reaction compared to the
Structure-fluorescence activation relationships of a large Stokes shift fluorogenic RNA aptamer
Bessi, Irene,H?bartner, Claudia,Lenz, Ann-Kathrin,Steinmetzger, Christian
, p. 11538 - 11550 (2020/05/01)
The Chili RNA aptamer is a 52 nt long fluorogen-activating RNA aptamer (FLAP) that confers fluorescence to structurally diverse derivatives of fluorescent protein chromophores. A key feature of Chili is the formation of highly stable complexes with different ligands, which exhibit bright, highly Stokes-shifted fluorescence emission. In this work, we have analyzed the interactions between the Chili RNA and a family of conditionally fluorescent ligands using a variety of spectroscopic, calorimetric and biochemical techniques to reveal key structure-fluorescence activation relationships (SFARs). The ligands under investigation form two categories with emission maxima of ～540 or ～590 nm, respectively, and bind with affinities in the nanomolar to low-micromolar range. Isothermal titration calorimetry was used to elucidate the enthalpic and entropic contributions to binding affinity for a cationic ligand that is unique to the Chili aptamer. In addition to fluorescence activation, ligand binding was also observed by NMR spectroscopy, revealing characteristic signals for the formation of a G-quadruplex only upon ligand binding. These data shed light on the molecular features required and responsible for the large Stokes shift and the strong fluorescence enhancement of red and green emitting RNA-chromophore complexes.
Copper(II)-Mediated Aerobic Oxidation of Benzylimidates: Synthesis of Primary α-Ketoamides
Kumar, Yogesh,Shaw, Mukta,Thakur, Rima,Kumar, Amit
, p. 6617 - 6625 (2016/08/16)
A simple and straightforward method for the synthesis of primary α-ketoamides has been discovered. The reaction represents the first example of benzylimidates directly converting to primary α-ketoamides by using sustainable molecular oxygen as an oxidant. This reaction proceeds in the presence of copper(II) salt via cleavage of benzylic C-H and C-O bonds of the benzylimidates with liberation of alcohols as the only byproduct. A wide substrate scope, operationally mild conditions, the use of single substrates, and a reaction scaled up to grams make this strategy very attractive and practical. Furthermore, mechanistic studies illustrate that the imidate group adjacent to the benzylic position plays crucial role in facilitating this chemical process.
PYRIDINONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF
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Page/Page column 130-131, (2011/07/09)
Pyridinone derivatives, process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially sex-hormone-related conditions in both men and women, as well as a mammal in general (also referred to herein as a "subject"). For example, such conditions include endometriosis, uterine fibroids, polycystic ovarian disease, heavy menstrual bleeding, particularly menorrahagia and dysmenorrehea, hirsutism, precocious puberty, gonadal steroid-dependent neoplasia such as cancers of the prostate, breast and ovary, gonadotrope pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hypertrophy, contraception and infertility (e.g., assisted reproductive therapy such as in vitro fertilization). The present application relates in particular to pyridinone derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists.
AMIDINE-CONTAINING COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS
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Page/Page column 18, (2009/07/17)
The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X′, X″, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic recep
The Preparation and Liquid Crystal Behaviour of Pyrimidines and Dioxans Incorporating a Dimethylene Linking Group
Andrews, B. M.,Gray, G. W.,Bradshaw, M. J.
, p. 257 - 270 (2007/10/02)
The preparation of 2-(4-cyanophenylethyl)-5-alkylpyrimidines and trans-2-(4-(cyanophenylethyl)-5-alkyl-1,3-dioxans, which incorporate a dimethylene linking group into phenylpyrimidine and phenyldioxan structures, is described.The pyrimidinyl compounds exhibit only virtual nematic-isotropic transitions and the dioxan compounds have monotropic nematic-isotropic transitions.Comparisons are made between the liquid crystal behaviour of these compounds and similar materials not incorporating the linking group.Comparisons are also made with related systems incorporating the bicyclo(2.2.2) octane ring and with systems in which the dimethylene group links two phenyl rings.The materials described have been found to exhibit interesting dielectric properties.The pyrimidine compounds, for example, have higher perpendicular and parallel permittivities than corresponding materials without the dimethylene linkage.
