- 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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- NOVEL ARYLALKENE DERIVATIVES AND USE THEREOF AS SELECTIVE ESTROGEN RECEPTOR MODULATORS
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The invention provides novel ethylene derivatives represented by Formula I, which may be used as selective estrogen receptor modulators (SERMs) and useful in the prophylaxis and/or treatment of estrogen-dependent conditions or conditions.
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Paragraph 0207
(2013/07/19)
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- METHOD FOR TREATING CHRONIC PAIN USING MEK INHIBITORS
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The invention features a method for treating chronic pain using a compound selected from formulae (I), (II)A, (I)B and (I)C.
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- Infrared and Raman spectra, conformational stability, vibrational assignment, ab initio calculations and r0 structural parameters for N-methylpropargyl amine
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The infrared spectra (3200 to 50 cm-1) of gaseous and solid and Raman spectra (3200 to 10 cm-1) of the liquid and solid N-methylpropargyl amine (4-aza-1-pentyne), HC≡CCH2N(CH3)H, have been recorded. All three possible conformers, i.e., methyl group (Me-trans) hydrogen atom (H-trans), and lone pair (LP-trans) trans to the ethynyl group, have been identified in the fluid phase with only the conformer with the LP-trans remaining in the solid. Variable temperature (-105 to -150°C) studies of the infrared spectra of the sample dissolved in liquid krypton have been carried out. From these data the enthalpy difference has been determined to be 360 ± 72 cm-1 (4.31 ± 0.86 kJ mol-1), between the most stable LP-trans conformer and the second most stable Me-trans rotamer. An enthalpy difference of 100 ± 20 cm-1 is estimated between the Me-trans form and the least stable H-trans conformer. These results are in reasonable agreement with the ab initio predictions at all levels of calculations. It is estimated that there is only 8% of the H-trans form and 14% of the Me-trans conformer present at ambient temperature. A complete vibration assignment is proposed for the LP-trans conformer which is based on infrared band contours, infrared intensities, Raman activities, and group frequencies, which is supported by normal coordinate calculations utilizing the force constants from ab initio MP2/6-31G(d) and DFT(B3LYP) calculations. Proposed assignments are also made for several of the fundamentals of the other two conformers. The conformational stabilities, barriers to internal rotation, and fundamental vibrational frequencies which have been determined experimentally are compared to those obtained from ab initio calculations. Utilizing previously reported microwave rotational constants for two isotopomers of the LP-trans rotamer along with ab initio predicted structural values, r0 parameters have been obtained for this conformer. The results are discussed and compare to the corresponding properties of some similar molecules.
- Guirgis, Gamil A.,Bell, Stephen,Zheng, Chao,Durig, James R.
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p. 1438 - 1450
(2007/10/03)
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- Benzenesulfonamide derivatives and their use as MEK inhibitors
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Benzenesulfonamides of formula (I), in which W is OR1, NR2OR1, NRARB, NR2NRARB, or NR2(CH2)2-4NRARBand the other variables as defined in the claims, are inhibitors of MEK and are effective in the treatment of proliferative diseases, cancer, stroke, heart failure, xenograft rejection, arthritis, cystic fibrosis, hepatomegaly, cardiomegaly, Alzheimer's disease, complications of diabetes, septic shock, and viral infection.
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- Process for the preparation of 1,2,4-substituted imidazoles and related aminoalkylimidazole derivatives
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The invention provides a new and efficient process for preparing 2,4(5)-substituted or 1,2,4-substituted imidazole derivatives. The invention also provides a process for preparing substituted aminoalkylimidazole derivatives, useful for the treatment of mammals having a variety of disease states, including stroke, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism, and the like. The invention also relates to novel aminoalkylimidazole 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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