108237-91-8Relevant academic research and scientific papers
A Small Molecule Mimetic of the Humanin Peptide as a Candidate for Modulating NMDA-Induced Neurotoxicity
Alam, Mohammad Parvez,Bilousova, Tina,Spilman, Patricia,Vadivel, Kanagasabai,Bai, Dongsheng,Elias, Chris J.,Evseenko, Denis,John, Varghese
, p. 462 - 468 (2018)
Humanin (HN), a 24-amino acid bioactive peptide, has been shown to increase cell survival of neurons after exposure to Aβ and NMDA-induced toxicity and thus could be beneficial in the treatment of Alzheimer's disease (AD). The neuroprotection by HN is rep
Highly efficient heterogeneous copper-catalysed coupling of oxime acetates with isothiocyanates leading to 2-aminothiazoles
Tuo, Yuxink,Yao, Fang,Liao, Yang,Cai, Mingzhong
, p. 225 - 229 (2017)
The heterogeneous coupling reaction of oxime acetates with isothiocyanates was achieved at 110°C in toluene in air in the presence of a bidentate nitrogen-functionalised MCM-41-immobilised copper(I) complex (MCM-41-2N-CuI) with Cs2CO3 as base to afford a variety of 2-aminothiazoles in good yields. The MCM-41-2N-CuI catalyst can be easily recovered by a simple filtration and reused at least eight times without significant loss of activity.
Aryliodoazide synthons: A different approach for diversified synthesis of 2-aminothiazole, 1,3-thiazole, and 1,3-selenazole scaffolds
Majnooni, Sahar,Duffield, Joseph,Price, Jessica,Khosropour, Ahmad Reza,Zali-Boeini, Hassan,Beyzavi, M. Hassan
supporting information, p. 516 - 521 (2019/08/01)
Several straightforward and practical processes have been established for the construction of 2-aminothiazoles, 1,3-thiazoles and 1,3-selenazoles from aryliodoazides. These strategies successfully proceed with a wide spectrum of substituted thioamides and its derivatives producing the resulting five-membered heterocycles obtained in satisfactory yields. The unique features of these protocols are operational simplicity and highly functional group tolerance, which make them convenient and practical routes for the preparation of various libraries of 2-aminothiazoles, 1,3-thiazoles, and 1,3-selenazoles.
Antibacterial synergist, preparation method and uses thereof
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, (2018/03/28)
The present invention relates to an antibacterial synergist, a preparation method and uses thereof, and specifically discloses a compound represented by a formula (I) and having antibacterial synergyactivity, or an optical isomer, a cis-trans isomer or a pharmaceutically acceptable salt thereof, and a preparation method thereof. The present invention further discloses a medical composition containing the compound, and uses thereof. According to the present invention, the compound can effectively enhance the antibacterial activity of polymyxin B against Acinetobacter baumannii and Klebsiella pneumoniae, and can be used for the antibacterial treatment of pathogenic bacteria insensitive to polymyxin or having low bacterial inhibition activity. The formula (I) is defined in the specification.
GP130 MODULATORS
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Paragraph 0321-0322, (2018/03/28)
There are provided, inter alia, compounds and methods useful for the treatment of neurological conditions, such as neurological disorders and neurodegenerative diseases, including Alzheimer's Disease.
Copper-Catalyzed Coupling of Oxime Acetates with Isothiocyanates: A Strategy for 2-Aminothiazoles
Tang, Xiaodong,Zhu, Zhongzhi,Qi, Chaorong,Wu, Wanqing,Jiang, Huanfeng
supporting information, p. 180 - 183 (2016/02/03)
A new strategy for 2-aminothiazoles is developed via the copper-catalyzed coupling of oxime acetates with isothiocyanates. Various 4-substituted and 4,5-disubstituted 2-aminothiazoles were formed smoothly under mild reaction conditions. This process involved copper-catalyzed N-O bond cleavage, activation of vinyl sp2 C-H bonds, and C-S/C-N bond formations. It is noteworthy that the oxime acetates were used not only as a substrate but also as a single oxidant.
Carbon tetrabromide mediated oxidative cyclocondensation of ketones and thioureas: An easy access to 2-aminothiazoles
Keshari, Twinkle,Kapoorr, Ritu,Yadav, Lal Dhar S.
supporting information, p. 5623 - 5627 (2015/09/21)
A simple, mild, and efficient one-pot method for the synthesis of substituted 2-aminothiazoles has been reported. The reaction involves the formation of sulfenyl bromide as an umpolung intermediate of nucleophilic sulfur, which is responsible for C-S bond formation leading to oxidative cyclization of ketones and thioureas to furnish the desired products. Carbon tetrabromide was used as a convenient and mild brominating reagent under basic condition at room temperature to give 2-aminothiazoles in good to excellent yields.
PHTHALAZINONES AND ISOQUINOLINONES AS ROCK INHIBITORS
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Paragraph 0329-0331, (2014/08/06)
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
NOVEL HETEROARYL-AMINO DERIVATIVES
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Page/Page column 38; 58, (2013/05/09)
Disclosed is a compound of formula (I), wherein R1, R2, L, Rm and Rn are as defined herein. The compound of formula (I) may be used in preventing and/or treating acyl CoA-diacylglycerol acyltransferase 1(DGAT-1) related diseases, such as obesity, coronary disease, hypertension, hyperlipidemia, arteriosclerosis, type II diabetes, stroke, hepatitis C, and the like.
Bromineless bromine as an efficient desulfurizing agent for the preparation of cyanamides and 2-aminothiazoles from dithiocarbamate salts
Yella, Ramesh,Kavala, Veerababurao,Patel, Bhisma K.
experimental part, p. 792 - 805 (2011/04/22)
In a one-pot procedure, bromineless brominating reagent 1,1'-(ethane-1,2-diyl)dipyridinium bistribromide (EDPBT) has been used as a desulfurizing agent in the preparation of organic cyanamides and substituted thiazoles starting from dithiocarbamic acid salts. In this approach, alkyl/aryl isothiocyantes were first obtained by the desulfurization of dithiocarbamic acid salts with EDPBT. The in situ-generated isothiocyanates reacts with an aqueous ammonia, forming alkyl or aryl thioureas, which on subsequent oxidative desulfurization with EDPBT led to the formation of corresponding cyanamides in good yields. Alternatively, an efficient one-pot synthesis of substituted thiazoles has been achieved by the condensation of the in situ-generated 1-aryl thioureas with the in situ-generated -bromoketones from ketones, again using EDPBT. The reagent EDPBT can be easily prepared from the readily available reagents. Desulfurizing ability dominates over its brominating ability for substrates amenable to bromination.
