- Comparative inhibition of tetrameric carbonyl reductase activity in pig heart cytosol by alkyl 4-pyridyl ketones
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Context and objective: The present study is to elucidate the comparative inhibition of tetrameric carbonyl reductase (TCBR) activity by alkyl 4-pyridyl ketones, and to characterize its substrate-binding domain. Materials and methods: The inhibitory effect
- Shimada, Hideaki,Tanigawa, Takahiro,Matayoshi, Kazunori,Katakura, Kazufumi,Babazono, Ken,Takayama, Hiroyuki,Murahashi, Tsuyoshi,Akita, Hiroyuki,Higuchi, Toshiyuki,Eto, Masashi,Imamura, Yorishige
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p. 397 - 400
(2014/06/09)
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- The anion of 3-methyl-2-pyridin-4-yl-1,3-oxazine
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n-Butyllithium at -78°C readily abstracts the methine proton from the title compound. The anion reacts efficiently with a range of electrophiles to provide 4-pyridyl ketones upon acid hydrolysis.
- Sheldrake, Peter,Tyrrell, Elizabeth,Mintias, Shirin,Shahid, Imran
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p. 2263 - 2268
(2007/10/03)
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- APPLICATIONS of ORGANOLITHIUM and RELATED REAGENTS in SYNTHESIS. Part V. Directed Metallation of Secondary Picolin- and Isonicotinamides. A Useful Method for the Synthesis of 2,3- and 3,4-Disubstituted Pyridines, Including Furopyridin-3(1H)-one and Furopyridine-1(3H)-one
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The metallation reaction of N-methyl-, N-benzyl- and N-phenyl-amides (1a-c) and (2a-c) derived from picolinic and isonicotinic acids by BunLi in THF leading to the corresponding bis(N- and 3-)lithiated amides (3a-c) and (4a-c), are described.The N-phenylamides (anilides) (1c) and (2c), in comparison with the other aliphatic derivatives, demonstrate greater abilities to direct ortho lithiation at the 3-position of the pyridine ring, and give with very good yields bis(N- and 3-)lithiated anilides (3c) and (4c), respectively.The N-benzylamides (1b) and (2b) are ortho metallated under kinetic control at -78 deg C to form the bis(N- and 3-)lithiated benzylamides (3b) and (4b), but the organometallic intermediates rearrange at room temperature to give the thermodynamically more stable bis(N- and α-)lithiated amides (3g) and (4g) (benzyl-type anions).The generated carbanions (3c), (4c), (3g) and (4g) were trapped by a variety of electrophiles (e.g. alkyl halides and aldehydes).The synthesis of furopyridin-3(1H)-one (18) and furopyridin-(3H)-one (19) is included.
- Epsztajn, Jan,Bieniek, Adam,Plotka, Mieczyslaw W.
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p. 442 - 474
(2007/10/02)
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- Ligand interaction of sustituted pyridines with cytochrome P-450.
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A series of pyridyl ketones and alkyl pyridines was evaluated as type II ligands for cytochrome P-450. Activity as type II ligands was evaluated in terms of the lipid solubility and the pKa values of the compounds.
- Born,Early
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p. 850 - 851
(2007/10/02)
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