43018-72-0Relevant articles and documents
Synthesis and fungicidal activity of N-2-(3-methoxy-4-propargyloxy) phenethyl amides. Part 3: Stretched and heterocyclic mandelamide oomyceticides
Lamberth, Clemens,Kempf, Hans-Joachim,Kriz, Miroslav
, p. 57 - 62 (2007)
Novel analogues of mandipropamid have been designed and prepared. The synthetic approach to these stretched and heterocyclic mandelamides is outlined. Biological data demonstrate their high efficacy against important plant diseases like tomato and potato
Catalyst-Free Decarbonylative Trifluoromethylthiolation Enabled by Electron Donor-Acceptor Complex Photoactivation
Lipp, Alexander,Badir, Shorouk O.,Dykstra, Ryan,Gutierrez, Osvaldo,Molander, Gary A.
supporting information, p. 3507 - 3520 (2021/06/11)
A catalyst- and additive-free decarbonylative trifluoromethylthiolation of aldehyde feedstocks has been developed. This operationally simple, scalable, and open-to-air transformation is driven by the selective photoexcitation of electron donor-acceptor (EDA) complexes, stemming from the association of 1,4-dihydropyridines (donor) with N-(trifluoromethylthio)phthalimide (acceptor), to trigger intermolecular single-electron transfer events under ambient- and visible light-promoted conditions. Extension to other electron acceptors enables the synthesis of thiocyanates and thioesters, as well as the difunctionalization of [1.1.1]propellane. The mechanistic intricacies of this photochemical paradigm are elucidated through a combination of experimental efforts and high-level quantum mechanical calculations [dispersion-corrected (U)DFT, DLPNO-CCSD(T), and TD-DFT]. This comprehensive study highlights the necessity for EDA complexation for efficient alkyl radical generation. Computation of subsequent ground state pathways reveals that SH2 addition of the alkyl radical to the intermediate radical EDA complex is extremely exergonic and results in a charge transfer event from the dihydropyridine donor to the N-(trifluoromethylthio)phthalimide acceptor of the EDA complex. Experimental and computational results further suggest that product formation also occurs via SH2 reaction of alkyl radicals with 1,2-bis(trifluoromethyl)disulfane, generated in-situ through combination of thiyl radicals. (Figure presented.).
CHEMICAL COMPOUNDS AS ATF4 PATHWAY INHIBITORS
-
Page/Page column 93-94, (2018/01/19)
The invention is directed to substituted piperidine derivatives. Specifically, the invention is directed to compounds according to Formula IIII: wherein A, B, X, Y, L1, L2, L3, R1, R2, R3, R4, R5, R6, R9, z2, z4, z5, and z6 are as defined herein, and salts thereof. The compounds of the invention are inhibitors of the ATF4 pathway and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, spinal cord injury, traumatic brain injury, ischemic stroke, stroke, diabetes, Parkinson disease, Huntington's disease, Creutzfeldt-Jakob Disease, and related prion diseases, progressive supranuclear palsy, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, inflammation, fibrosis, chronic and acute diseases of the liver, chronic and acute diseases of the lung, chronic and acute diseases of the kidney, chronic traumatic encephalopathy (CTE), neurodegeneration, dementia, cognitive impairment, atherosclerosis, ocular diseases, arrhythmias, in organ transplantation and in the transportation of organs for transplantation. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting the ATF4 pathway and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
ANTICANCER AGENT COMPRISING AMINOACETONITRILE COMPOUND AS ACTIVE INGREDIENT
-
Paragraph 0790, (2016/08/17)
The present invention relates to an anticancer agent having a high safety and a superior anticancer activity, and an anticancer agent containing, as an active ingredient, an aminoacetonitrile compound represented by the formula (I) wherein R1 i
ANTI CANCER AGENT COMPRISING AMINOACETONITRILE COMPOUND AS ACTIVE INGREDIENT
-
Paragraph 0110, (2016/12/12)
The present invention relates to an anticancer agent having a high safety and a superior anticancer activity, and anticancer agent containing, as an active ingredient, an aminoacetonitrile compound represented by the formula (I) wherein R1 is a
Thiosemicarbazones as Aedes aegypti larvicidal
Da Silva, Jo?o Bosco P.,Navarro, Daniela Maria Do A.F.,Da Silva, Aluizio G.,Santos, Geanne K.N.,Dutra, Kamilla A.,Moreira, Diogo Rodrigo,Ramos, Mozart N.,Espíndola, José Wanderlan P.,De Oliveira, Ana Daura T.,Brondani, Dalci José,Leite, Ana Cristina L.,Hernandes, Marcelo Zaldini,Pereira, Valéria R.A.,Da Rocha, Lucas F.,De Castro, Maria Carolina A.B.,De Oliveira, Beatriz C.,Lan, Que,Merz, Kenneth M.
, p. 162 - 175 (2015/06/22)
Abstract A set of aryl- and phenoxymethyl-(thio)semicarbazones were synthetized, characterized and biologically evaluated against the larvae of Aedes aegypti (A. egypti), the vector responsible for diseases like Dengue and Yellow Fever. (Q)SAR studies were useful for predicting the activities of the compounds not included to create the QSAR model as well as to predict the features of a new compound with improved activity. Docking studies corroborated experimental evidence of AeSCP-2 as a potential target able to explain the larvicidal properties of its compounds. The trend observed between the in silico Docking scores and the in vitro pLC50 (equals -log LC50, at molar concentration) data indicated that the highest larvicidal compounds, or the compounds with the highest values for pLC50, are usually those with the higher docking scores (i.e., greater in silico affinity for the AeSCP-2 target). Determination of cytotoxicity for these compounds in mammal cells demonstrated that the top larvicide compounds are non-toxic.
New class of bioluminogenic probe based on bioluminescent enzyme-induced electron transfer: BioLeT
Takakura, Hideo,Kojima, Ryosuke,Kamiya, Mako,Kobayashi, Eiji,Komatsu, Toru,Ueno, Tasuku,Terai, Takuya,Hanaoka, Kenjiro,Nagano, Tetsuo,Urano, Yasuteru
supporting information, p. 4010 - 4013 (2015/04/14)
Bioluminescence imaging (BLI) has advantages for investigating biological phenomena in deep tissues of living animals, but few design strategies are available for functional bioluminescent substrates. We propose a new design strategy (designated as bioluminescent enzyme-induced electron transfer: BioLeT) for luciferin-based bioluminescence probes. Luminescence measurements of a series of aminoluciferin derivatives confirmed that bioluminescence can be controlled by means of BioLeT. Based on this concept, we developed bioluminescence probes for nitric oxide that enabled quantitative and sensitive detection even in vivo. Our design strategy should be applicable to develop a wide range of practically useful bioluminogenic probes.
An efficient and green oxidation of vicinal diols to aldehydes using polymer-supported (diacetoxyiodo)benzene as the oxidant
Chen, Fen-Er,Xie, Bin,Zhang, Ping,Zhao, Jian-Feng,Wang, Hui,Zhao, Lei
, p. 619 - 622 (2007/10/03)
An operationally simple and clean oxidation of a variety of vicinal diols to aldehydes using polymer-supported (diacetoxyiodo)benzene (PSDIB) has been developed in high to excellent yields. Protecting groups such as OAc, OR, OBn, OBz and isopropylidene in the substrates were found to be stable under these reaction conditions. The regenerated PSDIB could be reused for the same reaction, affording oxidation products in high yield and purity. Georg Thieme Verlag Stuttgart.
Mild and selective hydrozirconation of amides to aldehydes using Cp 2Zr(H)Cl: Scope and mechanistic insight
Spletstoser, Jared T.,White, Jonathan M.,Tunoori, Ashok Rao,Georg, Gunda I.
, p. 3408 - 3419 (2007/10/03)
An investigation of the use of Cp2Zr(H)Cl (Schwartz's reagent) to reduce a variety of amides to the corresponding aldehydes under very mild reaction conditions and in high yields is reported. A range of tertiary amides, including Weinreb's amides, can be converted directly to the corresponding aldehydes with remarkable chemoselectivity. Primary and secondary amides proved to be viable substrates for reduction as well, although the yields were somewhat diminished as compared to the corresponding tertiary amides. Results from NMR experiments suggested the presence of a stable, 18-electron zirconacycle intermediate that presumably affords the aldehyde upon water or silica gel workup. A series of competition experiments revealed a preference of the reagent for substrates in which the lone pair of the nitrogen is electron releasing and thus more delocalized across the amide bond by resonance. This trend accounts for the observed excellent selectivity for tertiary amides versus esters. Experiments regarding the solvent dependence of the reaction suggested a kinetic profile similar to that postulated for the hydrozirconation of alkenes and alkynes. Addition of p-anisidine to the reaction intermediate resulted in the formation of the corresponding imine mimicking the addition of water that forms the aldehyde.
Aminoacetonitrile derivative agricultural and horticultural insecticide containing the same and use thereof
-
, (2008/06/13)
An aminoacetonitrile derivative of the formula (I): (wherein Ar1and Ar2represents phenyl group; substituted phenyl group having at least one subsituent selected from halogen atom, nitro group, cyano group, (halo) C1-C
