- Synthesis and biological properties of novel glucocorticoid androstene C-17 furoate esters
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A series of novel corticosteroid derivatives featuring C-17 furoate ester functionality have been synthesised. Profiling in vitro and in vivo has resulted in the identification of a compound with a longer duration of action and a lower oral side effect profile in rodents compared to budesonide.
- Sandham, David A.,Barker, Lucy,Beattie, David,Beer, David,Bidlake, Louise,Bentley, David,Butler, Keith D.,Craig, Sarah,Farr, David,Ffoulkes-Jones, Claire,Fozard, John R.,Haberthuer, Sandra,Howes, Colin,Hynx, Deborah,Jeffers, Sarah,Keller, Thomas H.,Kirkham, Paul A.,Maas, Janet C.,Mazzoni, Lazzaro,Nicholls, Andrew,Pilgrim, Gaynor E.,Schaebulin, Elisabeth,Spooner, Gillian M.,Stringer, Rowan,Tranter, Pamela,Turner, Katharine L.,Tweed, Morris F.,Walker, Christoph,Watson, Simon J.,Cuenoud, Bernard M.
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- Furan Carboxylic Acids Production with High Productivity by Cofactor-engineered Whole-cell Biocatalysts
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Furan carboxylic acids are useful chemicals in various industries. In this work, biocatalytic production of furan carboxylic acids was reported with high productivities by cofactor-engineered Escherichia coli cells. NADH oxidase (NOX) was introduced into E. coli harboring aldehyde dehydrogenases (ALDHs) to promote intracellular NAD+ regeneration, thus significantly enhancing ALDH-catalyzed oxidation. These engineered biocatalysts were capable of efficient aerobic oxidation of a variety of aromatic aldehydes. More importantly, they exhibited high substrate tolerance toward toxic furans. E. coli co-expressing vanillin dehydrogenase and NOX (E. coli_CtVDH1_NOX) enabled efficient oxidation of 250 mM of 5-hydroxymethylfurfural (HMF) to 5-hydroxymethyl-2-furancarboxylic acid (HMFCA), providing a productivity of 3.7 g/L h. With E. coli_CtVDH2_NOX as catalyst, up to 240 mM of furfural and 5-methoxymethylfurfural (MMF) could be smoothly oxidized. 2-Furoic acid (FCA, 227 mM) and 5-methoxymethyl-2-furancarboxylic acid (MMFCA, 287 mM) were produced in fed-batch synthesis, providing the productivities of 2.0 and 5.6 g/L h, respectively.
- Zhang, Xue-Ying,Wang, Xin,Li, Nan-Wei,Guo, Ze-Wang,Zong, Min-Hua,Li, Ning
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p. 3257 - 3264
(2020/05/25)
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- NICOTINIC ACETYLCHOLINE RECEPTORSUB-TYPE SELECTIVE AMIDES OF DIAZABICYCLOALKANES
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Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteoraryl carboxylic acids and certain diazabicycloalkanes. The
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Page/Page column 32
(2008/12/05)
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- INHIBITORS OF HIV REPLICATION
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The present invention relates to compounds of formula (I) wherein R1, R2, R3 and R4 are as defined herein, compositions and uses thereof for treating human immunodeficiency virus (HIV) infection. In particular,
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Page/Page column 36
(2008/12/06)
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- Phosphorylamides, their preparation and use
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A phosphorylamide derivative represented by the general formula (I): STR1 wherein R represents an amino group that may be substituted, or a salt thereof, possesses potent antibacterial activity against Helicobacter bacterium, especially Helicobacter pylori, and is useful for prevention or treatment of digestive diseases caused by Helicobacter bacterium, solely or in combination with an antacid or an acid secretion inhibitor.
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