- Optimization of a urea-containing series of nicotinamide phosphoribosyltransferase (NAMPT) activators
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NAD+ is a crucial cellular factor that plays multifaceted roles in wide ranging biological processes. Low levels of NAD+ have been linked to numerous diseases including metabolic disorders, cardiovascular disease, neurodegeneration,
- Pinkerton, Anthony B.,Sessions, E. Hampton,Hershberger, Paul,Maloney, Patrick R.,Peddibhotla, Satyamaheshwar,Hopf, Meghan,Sergienko, Eduard,Ma, Chen-Ting,Smith, Layton H.,Jackson, Michael R.,Tanaka, Jun,Tsuji, Takashi,Akiu, Mayuko,Cohen, Steven E.,Nakamura, Tsuyoshi,Gardell, Stephen J.
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- Mesoionic Carbene-Iridium Complex Catalyzed Ortho-Selective Hydrogen Isotope Exchange of Anilines with High Functional Group Tolerance
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Mesoionic carbene-iridium complex 1a has been investigated in the hydrogen isotope exchange (HIE) reaction of anilines. By employing 1 mol % of 1a as catalyst, anilines were selectively deuterated at the ortho-position with high deuteration levels. High ortho-selectivity was observed for anilines with various competing directing groups, which is in contrast with catalytic results of Kerr's catalysts.
- Cao, Lei,Huang, Linwei,Huang, Shiqing,Liu, Wei,Yan, Xiaoyu,Zhang, Gang,Zhang, Zengyu,Zhao, Peng
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supporting information
(2020/03/13)
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- Optimization of norbornyl-based carbocyclic nucleoside analogs as cyclin-dependent kinase 2 inhibitors
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We report on the discovery of norbornyl moiety as a novel structural motif for cyclin-dependent kinase 2 (CDK2) inhibitors which was identified by screening a carbocyclic nucleoside analogue library. Three micromolar hits were expanded by the use of medic
- K?prülüo?lu, Cemal,Dejmek, Milan,?ála, Michal,Ajani, Haresh,H?ebabecky, Hubert,Fanfrlík, Jind?ich,Jorda, Radek,Dra?ínsky, Martin,Procházková, Eli?ka,?ácha, Pavel,Kry?tof, Vladimír,Hobza, Pavel,Lep?ík, Martin,Nencka, Radim
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- A simple synthesis of anilines by LiAlH4/TiCl4 reduction of aromatic nitro compounds
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A rapid and efficient single-step synthesis of substituted anilines has been developed. The aromatic nitro compounds were reduced by using reducing systems generated by the action of an excess of LiAlH4 on TiCl4. Anilines substituted with different functional groups were synthesized in high yields and purity starting from the corresponding nitro compounds. The developed procedure is applicable to nitroaromatics containing both electron withdrawing and electron donating substituents. Substrates with electron donor substituents require a larger excess of LiAlH4. The reducing power of the prepared reactant systems depends on the used molar ratio of LiAlH4 and TiCl4.
- Di Gioia, Maria Luisa,Leggio, Antonella,Guarino, Isabella Federica,Leotta, Vanessa,Romio, Emanuela,Liguori, Angelo
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supporting information
p. 5341 - 5344
(2015/09/01)
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- A selective, tin-free radical mediated synthesis of indoles based on a sulfonate template
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A synthesis of indoles based on a vinyl sulfonate template is described. The approach employs a sulfonate group which plays three discrete roles in the synthetic sequence. Firstly the highly electron-withdrawing sulfonate group behaves as an activating group for a 1,4-addition of an aniline to the unsaturated system. Secondly, the electron-withdrawing nature of the same group also allows it to behave as a radical stabilising group which facilitates radical cyclisation to an aromatic ring to yield a transient indoline. Finally, the pendant sulfonate group behaves as a leaving group to yield the indole.
- Gray, Vincent James,Wilden, Jonathan D.
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supporting information; experimental part
p. 41 - 44
(2012/01/05)
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- TRIAZOLE COMPOUNDS AS LIPOXYGENASE INHIBITORS
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There is provided compounds of formula (I) wherein W is an optionally substituted aryl or heteroaryl group, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a lipoxygenase (e.g. 15- lipoxygenase) is desired and/or required, and particularly in the treatment of inflammation.
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Page/Page column 40
(2008/06/13)
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- Neuropeptide Y antagonists
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The compound is a neuropeptide Y antagonist and is effective in treating feeding disorders, cardiovascular diseases and other physiological disorders.
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Page column 28
(2010/02/05)
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- Amide derivatives useful as Neuropeptide Y (NPY) antagonists
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The compound is a neuropeptide Y antagonist and is effective in treating feeding disorders, cardiovascular diseases and other physiological disorders.
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- Azo coupling of o- and p-(dialkylaminosulfonyl)benzene-diazonium salts with 7-acetylamino-4-hydroxynaphthalene-2-sulfonic acid in citrate-phosphate buffer solution
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Dependences of the partial rate constants for azo coupling of o-(dialkylaminosulfonyl)benzene-diazonium salts with 7-acetylamino-4-hydroxynaphthalene-2-sulfonic acid (N-Acetyl-I-acid) on the fraction of the dianionic form of the latter indicate considerable steric hindrances to the second stage of the reaction. Ionization of the hydroxy group of N-acetyl-I-acid gives rise to additional electrostatic repulsion at the stage of formation of the σ complex, which reduces the rate of azo coupling at the 3-position of orthanilic acid.
- Kornev,Zheltov
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p. 962 - 968
(2007/10/03)
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- 4-Sulfonamidoanilide tertiary carbinols: A novel series of potassium channel openers
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Sulfonamides are viable replacements for the phenylsulfonyl and benzoyl moieties initially described for the anilide tertiary carbinol series of K(ATP) potassium channel openers. The SAR of this new series and the synthetic chemistry employed to generate its members are described.
- Empfield,Mayhugh,Ohnmacht,Frank,Grant,Li
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p. 775 - 778
(2007/10/03)
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- Aminosulfonylphenyl compounds for treating urinary incontinence
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Compounds of formula I STR1 wherein R 1, R 2, R 3, R 4, R 5 and A-B have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinery incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
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