- Planarity of heteroaryldithiocarbazic acid derivatives showing tuberculostatic activity: Structure-activity relationships
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The search for new tuberculostatics is an important issue due to the increasing resistance of Mycobacterium tuberculosis to existing agents and the resulting spread of the pathogen. Heteroaryldithiocarbazic acid derivatives have shown potential tuberculos
- Szczesio, Ma?gorzata,Go?ka, Jolanta,Korona-G?owniak, Izabela,Orlewska, Czes?awa,Gobis, Katarzyna,Olczak, Andrzej
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Read Online
- Ligand-Controlled Regiodivergence in Nickel-Catalyzed Hydroarylation and Hydroalkenylation of Alkenyl Carboxylic Acids**
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A nickel-catalyzed regiodivergent hydroarylation and hydroalkenylation of unactivated alkenyl carboxylic acids is reported, whereby the ligand environment around the metal center dictates the regiochemical outcome. Markovnikov hydrofunctionalization products are obtained under mild ligand-free conditions, with up to 99 % yield and >20:1 selectivity. Alternatively, anti-Markovnikov products can be accessed with a novel 4,4-disubstituted Pyrox ligand in excellent yield and >20:1 selectivity. Both electronic and steric effects on the ligand contribute to the high yield and selectivity. Mechanistic studies suggest a change in the turnover-limiting and selectivity-determining step induced by the optimal ligand. DFT calculations reveal that in the anti-Markovnikov pathway, repulsion between the ligand and the alkyl group is minimized (by virtue of it being 1° versus 2°) in the rate- and regioselectivity-determining transmetalation transition state.
- Deng, Ruohan,Engle, Keary M.,Fu, Yue,Gao, Yang,Li, Zi-Qi,Liu, Peng,Tran, Van T.
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supporting information
p. 23306 - 23312
(2020/10/19)
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- 3-pyridyl-3-amino-2-cyanoacrylate compound, and preparation method and application thereof
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The invention discloses a 3-pyridyl-3-amino-2-cyanoacrylate compound, and a preparation method and application thereof. The structure of the compound is shown in a general formula (1). The preparationmethod of the compound comprises the following steps: taking a compound shown in a formula (II) as a raw material to carry out a reaction with a fatty alcohol in an organic solvent in the presence ofhydrogen chloride to obtain pyridyl imidate, and carrying out a reaction on the pyridyl imidate with cyanoacetate in an organic solvent under catalysis of a catalyst for condensation to prepare the 3-pyridyl-3-amino-2-cyanoacrylate compound. The compound has bactericidal activity and can be used for preventing and treating diseases.
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Paragraph 0058-0060; 0069-0070
(2019/07/10)
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- MODULATORS OF C3A RECEPTOR AND METHODS OF USE THEREOF
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Provided are compounds that are modulators of C3a receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, the compounds are pyridones. In certain embodiments, provided are methods for treatment or amelioration of diseases associated with modulation of C3a receptor activity.
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Page/Page column 163-164
(2008/12/07)
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- EPOTHILONE ANALOGUES MODIFIED AT POSITIONS C12-C13 AS ANTICANCER DRUGS
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The invention relates to analogues of epothilones of formulae (A), (B), (I) and (II), uses and methods of making the same.
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Page/Page column 38
(2008/12/06)
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- Total synthesis of the thiopeptide antibiotic amythiamicin D
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The thiopeptide (or thiostrepton) antibiotics are a class of sulfur containing highly modified cyclic peptides with interesting biological properties, including reported activity against MRSA and malaria. Described herein is the total synthesis of the thi
- Hughes, Rachael A.,Thompson, Stewart P.,Alcaraz, Lilian,Moody, Christopher J.
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p. 15644 - 15651
(2007/10/03)
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- Synthesis, structure and tuberculostatic activity of N′-(amino-pyridyl-methylene)-hydrazinecarbodithioic acid methyl esters
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The methods of preparation of the title esters from imidates or amidrazones are described, and structures of the compounds are elucidated on the basis of 1H, 13C-NMR, 2D-NMR spectra and X-ray diffraction method. Tuberculotic activity was also studied.
- Orlewska,Foks,Sowinski,Martynowski,Olczak,Glowka
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p. 1237 - 1245
(2007/10/03)
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- NEW BINUCLEAR HETEROCYCLIC LIGANDS SHARING AN α-DIIMINE MOIETY AND THEIR RUTHENIUM(II) TRIS-CHELATES
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A number of chelating heterocyclic ligands which include pyridine, pyrazine, 1,3-heteroazole, and/or 1,2,4-heterodiazole moieties, have been prepared and characterized in order to tune the excited state properties of the corresponding Ru(II) complexes.The detailed study on the binuclear heterocycles by using uv, 1H- and 13C-nmr spectroscopy, as well as mass spectrometry, is also provided.The synthesis and spectral data (uv, ir, 1H- and 13C-nmr) of the ruthenium(II) tris-chelates is also included.
- Orellana, Guillermo,Alvarez-Ibarra, Carlos,Quiroga, Maria Luz
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p. 731 - 742
(2007/10/02)
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