5520-79-6Relevant articles and documents
Arylaminopropanone derivatives as potential cholinesterase inhibitors: Synthesis, docking study and biological evaluation
Cs?llei, Jozef,Enriz, Daniel,Garro, Adriana D.,Gutierrez, Lucas J.,Hudcová, Anna,Kroutil, Ale?,Kubínová, Renata,Oravec, Michal
, (2020)
Neurodegenerative diseases in which the decrease of the acetylcholine is observed are growing worldwide. In the present study, a series of new arylaminopropanone derivatives with N-phenylcarbamate moiety (1-16) were prepared as potential acetylcholinesterase and butyrylcholinesterase inhibitors. In vitro enzyme assays were performed; the results are expressed as a percentage of inhibition and the IC50 values. The inhibitory activities were compared with reference drugs galantamine and rivastigmine showing piperidine derivatives (1-3) as the most potent. A possible mechanism of action for these compounds was determined from a molecular modelling study by using combined techniques of docking, molecular dynamics simulations and quantum mechanics calculations.
Novel urea linked ciprofloxacin-chalcone hybrids having antiproliferative topoisomerases I/II inhibitory activities and caspases-mediated apoptosis
Mohammed, Hamada H.H.,Abbas, Samar H.,Hayallah, Alaa M.,Abuo-Rahma, Gamal El-Din A.,Mostafa, Yaser A.
, (2021)
A novel series of urea-linked ciprofloxacin (CP)-chalcone hybrids 3a-j were synthesized and screened by NCI-60 cancer cell lines as potential cytotoxic agents. Interestingly, compounds 3c and 3j showed remarkable antiproliferative activities against both
Synthesis and in vitro antimycobacterial activity of novel n-arylpiperazines containing an ethane-1,2-diyl connecting chain
Gonec, Tomás,Malík, Ivan,Cs?llei, Jozef,Jampílek, Josef,Stolaríková, Jirina,Solovic, Ivan,Miku, Peter,Keltoová, Stanislava,Kollár, Peter,O'Mahony, Jim,Coffey, Aidan
, (2018/01/17)
Novel 1-(2-{3-/4-[(alkoxycarbonyl)amino]phenyl}-2-hydroxyethyl)-4-(2-fluorophenyl)-piperazin-1-ium chlorides (alkoxy = methoxy to butoxy; 8a-h) have been designed and synthesized through multistep reactions as a part of on-going research programme focused
Chemoselective synthesis of carbamates using CO2 as carbon source
Riemer, Daniel,Hirapara, Pradipbhai,Das, Shoubhik
, p. 1916 - 1920 (2018/08/17)
Synthesis of carbamates directly from amines using CO2 as the carbon source is a straightforward and sustainable approach. Herein, we describe a highly effective and chemoselective methodology for the synthesis of carbamates at room temperature and atmosp
SUBSTITUTED ANILINE DERIVATIVES
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Page 59, (2008/06/13)
The present invention relates to aniline derivatives of the general formula I or pharmaceutically acceptable salts thereof and their use.
Kinetics and mechanism of the reactions of anilines with ethyl S-aryl thiocarbonates
Castro, Enrique A.,Leandro, Leonardo,Millan, Pablo,Santos, Jose G.
, p. 1953 - 1957 (2007/10/03)
The reactions of anilines with ethyl S-(2,4-dinitrophenyl) thiocarbonate (DNPTC) and ethyl S-(2,4,6-trinitrophenyl) thiocarbonate (TNPTC) are subjected to a kinetic study in aqueous solution at 25.0 °C and ionic strength 0.2 (KCl). The reactions are studied by following spectrophotometrically (400 nm) the release of the corresponding substituted benzenethiolate anion. Under aniline excess, pseudo-first-order rate coefficients (k(obsd)) are found. Plots of k(obsd) VS [N] (N is the free substituted aniline) are linear and pH independent, with slope k(N). The Bronsted-type plots (log k(N) vs pK(a) of anilinium ions) are linear, with slopes β = 0.9 for DNPTC, in agreement with a stepwise mechanism where the breakdown of a tetrahedral addition intermediate (T(±)) is rate determining, and β = 0.54 for TNPTC, consistent with a concerted mechanism. Consideration of the results for aminolysis from the present work and those from previous studies leads to the following conclusions. (i) The tetrahedral intermediate possessing a 2,4-dinitrobenzenethio group is more stable than that including the 2,4,6-trinitrobenzenethio group. (ii) The tetrahedral intermediate possessing the 2,4,6-trinitrobenzenethio group has no existence beyond the limit of a vibration period (concerted mechanism). (iii) Tetrahedral intermediates possessing anilino groups are less stable than those derived from pyridines but are more stable than the tetrahedral intermediates derived from secondary alicyclic amines. (iv) Anilines are more reactive toward the carbonyl group of methyl 2,4-dinitrophenyl carbonate than toward the carbonyl of DNPTC.
Bisphosphonic acid derivatives as anti-arthritic agents
-
, (2008/06/13)
The bisphosphonates of formula (III) bicyclic bisphosphonates (V), and cyclic bisphosphonates (VII) are useful as anti-arthritic agents and do not have the side effects of anti-arthritic agents which are prostaglandin synthetase inhibitors.
A simple method for the synthesis of carbamates
Angeles,Santillan,Martinez,Ramirez,Moreno,Salmon,Martinez
, p. 2441 - 2447 (2007/10/02)
A new method for carbamate synthesis using aryl and alkylamines with sodium hydride and diethylcarbonate in dry benzene is described.
AROYLNITRENES WITH SINGLET GROUND STATES: PHOTOCHEMISTRY OF ACETYL-SUBSTITUTED AROYL AND ARYLOXYCARBONYL AZIDES
Sigman, Michael E.,Autrey, Tom,Schuster, Gary B.
, p. 4297 - 4305 (2007/10/02)
The photochemistry of 4-acetylbenzoyl azide (ABA), 4-acetyl-4'-biphenoyl azide (ADA), and 4-acetylphenoxycarbonyl azide (APA) shows unusual wavelength and structrural effects.Irradiation of ABA or ADA into their ?-?* bands with deep-UV light leads to formation of 4-acetylbenzoylnitrene (ABN) and 4-acetyl-4'-biphenylnitrene (ADN), respectively, in competition with photo-Curtis rearrangement to form isocyanates.Irradiation of these azides into their n-?* bands with near-UV light gives only the aroylnitrenes.The triplet excited states of the azides were detected chemically and by transient spectroscopic techniques.Nitrogen loss following near-UV irradiation occurs exclusively from the excited triplet azides.However, the chemical properties of ABN and ADN are consistent only with reactions originating from their singlet states.An ESR spectrum is observed at 8 K for ((4-acetylphenoxy)carbonyl)nitrene (APN) but not for 4-acetylbenzoylnitrene (ABN) of 4-acetyl-4'-biphenylcarbonylnitrene (ADN).The chemical properties of APN in tert-butyl alcohol show that its triplet is no more than 5 kcal/mol below its lowest single state.In contrast, the chemical properties of ABN and ADN indicate that these niterenes have singlet ground states.
