- A chiral 2-D donor - Acceptor array of a bipyrazine N-oxide and tetracyanoethylene
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(equation presented) Hexamethylbipyrazine-N,N′,N″,N?-tetraoxide (1) is synthesized in racemic form and cocrystallized with tetracyanoethylene to give a donor-acceptor (DA) networked lattice. The resulting DA2 cocrystal contains homochiral 2-D DA arrays (layers) cohered by 2.7 ? NO?C=C DA bonds with periplanar O p-orbital/C=C orientations. Layer formation is stereoselective, while interlayer relations yield a racemic lattice.
- McGee, Byron J.,Sherwood, Lindsay J.,Greer, Melinda L.,Blackstock, Silas C.
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- Compound or pharmaceutically acceptable salt, isomer, prodrug, polymorph or solvate thereof
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The invention relates to the field of pharmacochemistry, in particular to a compound or pharmaceutically acceptable salt, isomer, prodrug, polymorphic substance or solvate thereof. The invention provides a compound or a pharmaceutically acceptable salt, isomer, prodrug, polymorph or solvate thereof. The chemical structural formula of the compound is shown as a formula I in the specification. Compared with similar compounds in the prior art, the compound provided by the invention has greater performance advantages, has better antioxidant, nerve cell protection and anti-platelet aggregation activity, is easy to pass through a blood-brain barrier, has good oral bioavailability, can greatly improve patient compliance and clinical convenience, and has good clinical application prospects. The compound can be developed into a medicine for treating and preventing oxidative stress related diseases such as cardiovascular and cerebrovascular diseases and neurodegenerative diseases, can also be used for treating thromboembolic diseases, and has a good industrialization prospect.
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- Pyrazole alcohol compound, pharmaceutical composition thereof and application thereof to drugs
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The invention discloses a 1-(3,5,6-trimethyl pyrazine-2-yl)-5-pyrazole alcohol compound, a tautomer thereof, a pharmaceutical composition thereof and application thereof to drugs. The 1-(3,5,6-trimethyl pyrazine-2-yl)-5-pyrazole alcohol compound has double effects of resisting platelet aggregation and protecting nerve cells, and comprises a compound as shown in the formula (I), a tautomer (Ia) thereof, or a stereoisomer, a geometrical isomer, a hydrate or a solvate thereof, or a pharmaceutically acceptable salt or prodrug as shown in the description. The 1-(3,5,6-trimethyl pyrazine-2-yl)-5-pyrazole alcohol compound and the pharmaceutical composition thereof provided by the invention can be used for preparing drugs for prevention and/or treatment and/or auxiliary treatment of cerebral apoplexy, cardiovascular and cerebrovascular diseases, senile dementia and complications thereof caused by thrombosis and excessive free radicals.
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- Discovery of tetrasubstituted pyrazines as semiochemicals in a sexually deceptive orchid
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Sexually deceptive orchids employ mimicry of insect sex pheromones to exploit a diverse group of pollinators. The chemical structures of five semiochemicals (1-3, 7, 8) produced by populations of the warty hammer orchid, Drakaea livida, pollinated by a thynnine wasp in the genus Catocheilus were elucidated. With the exception of (2,5-dimethylpyrazin-3-yl)methyl 3-methylbutanoate (7), all active compounds were tetrasubstituted pyrazines, including hydroxymethyl (1) and ester (2 and 3) trimethylpyrazine derivatives. Male Catocheilus wasps were responsive to all of these compounds in GC-EAD experiments.
- Bohman, Bjoern,Jeffares, Lynne,Barrow, Russell A.,Phillips, Ryan D.,Peakall, Rod,Flematti, Gavin,Dixon, Kingsley W.,Byrne, Lindsay T.,Skelton, Brian W.
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p. 1589 - 1594,6
(2020/09/09)
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- Pyrazine biosynthesis in corynebacterium glutamicum
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The volatile compounds released by Corynebacterium glutamicum were collected by use of the CLSA technique (closed-loop stripping apparatus) and analysed by GC-MS. The headspace extracts contained several acyloins and pyrazines that were identified by their synthesis or comparison to commercial standards. Feeding experiments with [2H7]acetoin resulted in the incorporation of labelling into trimethylpyrazine and tetramethylpyrazine. Several deletion mutants targeting genes of the primary metabolism, were constructed to elucidate the biosynthetic pathway to pyrazines in detail. A deletion mutant of the ketol-acid reductoisomerase was not able to convert the acetoin precursor (S)2-acetolactate into the pathway intermediate (R)-2,3-dihydroxy-3-methylbutanoate to the branched amino acids. This mutant requires valine, leucine, and isoleucine for growth and produces significantly higher amounts and more different compounds of the acyloin and pyrazine classes. Gene deletion of the acetolactate synthase (AS) resulted in a mutant that is not able to convert pyruvate into (5)-2-acetolactate. This mutant also requires branched amino acids and produces only very small amounts of pyrazines likely from valine via the valine biosynthetic pathway operating in reverse order. A ΔASΔKR double mutant was constructed that does not produce any pyrazines at all. These results open up a detailed biosynthetic model for the formation of alkylated pyrazines via acyloins.
- Dickschat, Jeroen S.,Wickel, Susanne,Bolten, Christoph J.,Nawrath, Thorben,Schulz, Stefan,Wittmann, Christoph
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supporting information; experimental part
p. 2687 - 2695
(2010/08/07)
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- AROMATIC NITROGEN-CONTAINING 6-MEMBERED RING COMPOUNDS AND THEIR USE
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The present invention provides aromatic nitrogen-containing 6-membered ring compounds having execellent PDE10 inhibitory activity. The present invention relates to an aromatic nitrogen-containing 6-membered ring compound represented by the following formula [I0] or a pharmaceutically acceptable salt thereof, a method for preparing the same, and use of said compounds for PDE10 inhibitors, and a pharmaceutical composition comprising said compounds as an active ingredient: Formula [I0] wherein: X1, X2 and X3 each independently are N or CH, and at least two of X1, X2 and X3 are N; A is *-CH=CH-, *-C(Alk)=CH-, *-CH2-CH2- or *-O-CH2- (* is a bond with R1); Alk is a lower alkyl group; Ring B is an optionally substituted nitrogen-containing aliphatic heterocyclic group; R1 is an optionally substituted nitrogen-containing heterocyclic group, a nitrogen-containing heterocyclic moiety of which is a moiety selected from the group consisting of quinoxalinyl, quinolyl, isoquinolyl, quinazolinyl, pyrazinyl, pyrimidinyl and a moiety thereof fused with a 5 to 6-membered aliphatic ring thereto; Y0 is a group selected from the group consisting of the following (1) to (5): (1) an optionally substituted phenyl or an optionally substituted aromatic monocyclic 5 to 6-membered heterocyclic group; (2) an optionally substituted aminocarbonyl; (3) an optionally substituted amino lower alkyl; (4) -O-R2 wherein R2 is hydrogen, an optionally substituted lower alkyl, lower cycloalkyl, aliphatic monocyclic 5 to 6-membered heterocyclic group, or Formula [AA]; (5) mono- or di-substituted amino; provided that, when Y0 is mono- or di-substituted amino, the nitrogen-containing heterocyclic moiety of R1 is not quinoxalinyl or quinolyl.
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Page/Page column 61
(2010/04/06)
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- Reactions of Halogenomethanes in the Vapor Phase. Part 4. The Reactions of Imidazoles with Chloroform at 550 deg C, and a Comparison with their Liquid-phase Reactions with Trichloroacetate Ion or Hexachloroacetone and Base
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1-Unsubstituted imidazoles and chloroform at 550 deg C in a flow system give mainly 5-chloropyrimidines, together with 4-chloropyrimidines and chloropyrazines.The effects of methyl substituents on the ratio of products is considered.The liquid-phase reactions of 2-methyl- and 2,4,5-trimethyl-imidazole under conditions in which dichlorocarbene is said to be formed in basic or neutral conditions were studied, and compared with the gas-phase reactions with chloroform.
- Busby, Reginald E.,Khan, Mohammad A.,Khan, Mohammad R.,Parrick, John,Shaw, C. J. Granville,Iqbal, Mohammad
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p. 1427 - 1430
(2007/10/02)
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