66232-41-5Relevant academic research and scientific papers
HETEROCYCLIC COMPOUND
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Paragraph 0306, (2020/06/23)
Provided is a heterocyclic compound that can have an antagonistic action on an NMDA receptor containing the NR2B subunit, and is expected to be useful as a prophylactic or therapeutic agent for major depression, bipolar disorder, migraine, pain, periphera
Ligand-Enabled γ-C(sp3)?H Olefination of Free Carboxylic Acids
Ghiringhelli, Francesca,Ghosh, Kiron Kumar,Mondal, Arup,Uttry, Alexander,Wedi, Philipp,van Gemmeren, Manuel
supporting information, p. 12848 - 12852 (2020/06/25)
We report the ligand-enabled C?H activation/olefination of free carboxylic acids in the γ-position. Through an intramolecular Michael addition, δ-lactones are obtained as products. Two distinct ligand classes are identified that enable the challenging palladium-catalyzed activation of free carboxylic acids in the γ-position. The developed protocol features a wide range of acid substrates and olefin reaction partners and is shown to be applicable on a preparatively useful scale. Insights into the underlying reaction mechanism obtained through kinetic studies are reported.
Synthesis and evaluation of quinazolines as inhibitors of the bacterial cell division protein FtsZ
Nepomuceno, Gabriella M.,Chan, Katie M.,Huynh, Valerie,Martin, Kevin S.,Moore, Jared T.,Obrien, Terrence E.,Pollo, Luiz A. E.,Sarabia, Francisco J.,Tadeus, Clarissa,Yao, Zi,Anderson, David E.,Ames, James B.,Shaw, Jared T.
supporting information, p. 308 - 312 (2015/03/30)
The bacterial cell division protein FtsZ is one of many potential targets for the development of novel antibiotics. Recently, zantrin Z3 was shown to be a cross-species inhibitor of FtsZ; however, its specific interactions with the protein are still unknown. Herein we report the synthesis of analogues that contain a more tractable core structure and an analogue with single-digit micromolar inhibition of FtsZs GTPase activity, which represents the most potent inhibitor of Escherichia coli FtsZ reported to date. In addition, the zantrin Z3 core has been converted to two potential photo-cross-linking reagents for proteomic studies that could shed light on the molecular interactions between FtsZ and molecules related to zantrin Z3.
Preparation of saccharincarboxylic acids and -carboxylic acid esters
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, (2008/06/13)
Saccharincarboxylic acids and -carboxylic acid esters of the formula I STR1 where the substituents have the following meanings: L and M are hydrogen, alkyl, alkoxy, alkylthio, chlorine, cyano, alkylsulfonyl, nitro or trifluoromethyl; Z is hydrogen, alkyl, cycloalkyl, alkyl, aryl or aralkyl; R is H or C1 -C6 -alkyl, are prepared by reacting corresponding bromo- or iodo-substituted saccharin derivatives of the formula II STR2 where L, M and Z have the abovementioned meanings, or if Z≠H, compounds of the formula III STR3 in the presence of a palladium, nickel, cobalt or rhodium transition metal catalyst and of a base with carbon monoxide and water or a C1 -C6 -alcohol under elevated pressure.
Saccharin derivatives
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, (2008/06/13)
Saccharin derivatives of the formula I STR1 where the substituents have the following meanings: L and M are hydrogen, C1 -C4 -alkyl, C1 -C4 -alkoxy, C1 -C4 -alkylthio, chlorine, cyano, methylsulfonyl, nitro or trifluoromethyl; Z is hydrogen, C1 -C4 -alkyl, C3 -C8 -cycloalkyl, C3 -C6 -alkenyl, C3 -C5 -alkynyl, C1 -C4 -acyl, benzyl or phenyl, the phenyl rings in each case being unsubstituted or substituted by halogen or C1 -C4 -alkyl; Q is a radical T-J, where T is a carbonyl radical CO or the radical --CHY, J is a 4-linked isoxazole ring of the formula II STR2 where R1 is hydrogen or C1 -C4 -alkyl and R2 is C1 -C4 -alkyl, cyclopropyl, 1-methylcyclopropyl or 1-methylthiocyclopropyl; Y is an OH group, a hydroxyl group which may be acylated by C2 -C4 -acyl or a chlorine atom; and agriculturally customary salts of the compounds I are described.
Saccharin derivatives
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, (2008/06/13)
Saccharin derivatives of the formula I STR1 where the substituents have the following meanings: L and M are hydrogen, C1 -C4 -alkyl, C1 -C4 -alkoxy, C1 -C4 -alkylthio, chlorine, cyano, meth
5-hydroxypyrazol-4-ylcarbonyl-substituted saccharin derivatives
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, (2008/06/13)
5-Hydroxypyrazol-4-ylcarbonyl-substituted saccharin derivatives of the formula I STR1 where the substituents have the following meanings: L and M are hydrogen, C1 -C4 -alkyl, C1 -C4 -alkoxy, C1 -Csub
Saccharin derivatives
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, (2008/06/13)
Saccharin derivatives of the formula I STR1 where the substituents have the following meanings: L and M are hydrogen, alkyl, alkoxy, alkylthio, chlorine, cyano, methylsulfonyl, nitro or trifluoromethyl; Z is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl,
HUMAN LEUKOCYTE ELASTASE (HLE) INHIBITORS, AND RELATED PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE
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, (2008/06/13)
Novel therapeutic agents useful as inhibitors of HLE are provided. The compounds have the structural formula (I) STR1 wherein R 1 through R 9, m, n and p are as defined herein. Methods of using the compounds of formula (I) to inhibit serine proteases and
