- Synthesis of Mixed Secondary and Tertiary Amines
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Abstract: A one-stage and facile method of synthesis of expensive methyl- and ethyl(allyl)amines, methyl- and ethyl(prop-2-ynyl)amines, and methyl- and ethyl(allyl)(3-phenylprop-2-ynyl)amines is developed. The synthesized amines present practical interest, because some (prop-2-ynyl)amines are used in the therapy cancer.
- Ayrapetyan, L. V.,Chukhajian, E. O.,Mkrtchyan, H. S.,Panosyan, H. A.
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p. 353 - 355
(2020/04/17)
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- Thiol activated prodrugs of sulfur dioxide (SO2) as MRSA inhibitors
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Drug resistant infections are becoming common worldwide and new strategies for drug development are necessary. Here, we report the synthesis and evaluation of 2,4-dinitrophenylsulfonamides, which are donors of sulfur dioxide (SO2), a reactive sulfur species, as methicillin-resistant Staphylococcus aureus (MRSA) inhibitors. N-(3-Methoxyphenyl)-2,4-dinitro-N-(prop-2-yn-1-yl)benzenesulfonamide (5e) was found to have excellent in vitro MRSA inhibitory potency. This compound is cell permeable and treatment of MRSA cells with 5e depleted intracellular thiols and enhanced oxidative species both results consistent with a mechanism involving thiol activation to produce SO2.
- Pardeshi, Kundansingh A.,Malwal, Satish R.,Banerjee, Ankita,Lahiri, Surobhi,Rangarajan, Radha,Chakrapani, Harinath
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p. 2694 - 2697
(2015/06/08)
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- Xanthine compounds having terminally animated alkynol side chains
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Compounds of the formula I, STR1 in which one of the radicals R1 and R3 is an alkynol residue of the formula Ia or Ib STR2 are suitable for producing pharmaceuticals having a neuroprotective effect.
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- Aliphatic propargylamines as cellular rescue agents
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The present invention relates to the use of a group of propargylamines of the general formula (I) STR1 wherein R1 is hydrogen or CH3 and R2 is (CH2)n CH3 and n is an integer from 0 to 16, and salts thereof, as cellular rescue agents in the treatment and prevention of diseases in which cell death occurs by apoptosis. Some of the compounds of formula I are novel. The invention is also directed to the use of these compounds in the treatment of these diseases, as well as to processes for the preparation of the compounds.
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- Thermal Oxidative Deamination of Aliphatic Amines to Aldehydes with Bis(diphenylphosphinyl) Peroxide
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Reaction of N-substituted alkylamines having pseudoacidic hydrogen at the 1-methylene group with bis(diphenylphosphinyl) peroxide yields the deaminated products by thermal elimination of diphenylphosphinic acid from the intermediate O-diphenylphosphinylhydroxylamines.
- Masse, Guy,Sturtz, Georges
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p. 907 - 910
(2007/10/02)
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