- Synthesis, antiepileptic effects, and structure-activity relationships of α-asarone derivatives: In vitro and in vivo neuroprotective effect of selected derivatives
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In the present study, we compared the antiepileptic effects of α-asarone derivatives to explore their structure-activity relationships using the PTZ-induced seizure model. Our research revealed that electron-donating methoxy groups in the 3,4,5-position on phenyl ring increased antiepileptic potency but the placement of other groups at different positions decreased activity. Besides, in allyl moiety, the optimal activity was reached with either an allyl or a 1-butenyl group in conjugation with the benzene ring. The compounds 5 and 19 exerted better neuroprotective effects against epilepsy in vitro (cell) and in vivo (mouse) models. This study provides valuable data for further exploration and application of these compounds as potential anti-seizure medicines.
- Zhang, Jian,Mu, Keman,Yang, Peng,Feng, Xinqian,Zhang, Di,Fan, Xiangyu,Wang, Qiantao,Mao, Shengjun
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- N,N+hu 1 +l SUBSTITUTED PIPERAZINES HAVING COMBINED ANTIAGGREGANT, ANTICOAGULANT AND VASODILATORY ACTIVITY, AND METHOD FOR PRODUCING SAME
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The invention relates to derivatives of N,N′-substituted piperazines of the general formula (I): where R1 and R2 denote linear or branched (C1-C4)alkyl, linear or branched (C1-C4)alkoxy, CH
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Paragraph 0133; 0134
(2013/10/22)
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- SUBSTITUTED ISOQUINOLINES AND THEIR USE AS TUBULIN POLYMERIZATION INHIBITORS
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The present invention relates generally to substituted isoquinolines and their use as tubulin polymerization inhibitors. In particular, the invention relates to substituted isoquinolines which possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds
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Page/Page column 78
(2011/12/14)
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- Separation, analyses and syntheses of trimethoprim impurities
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The analysis of several impurities of the chemotherapeutic agent trimethoprim with various methods, including thin layer chromatography, gas chromatography, capillary electrophoresis as well as nuclear magnetic resonance is described. These methods were used to identify new impurities in trimethoprim batches. The main impurities were separated by column chromatography. To ensure the identity of the impurities, de novo syntheses were successfully carried out. With the methods described, it was possible to detect, separate and identify new impurities in trimethoprim batches.
- Hess,Doelker,Haferburg,Kertscher,Matysik,Ortwein,Teubert,Zimmermann,Eger
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p. 306 - 310
(2007/10/03)
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- ESTER LINKAGES BETWEEN LIGNIN AND GLUCURONIC ACID IN LIGNIN-CARBOHYDRATE COMPLEXES FROM FAGUS CRENATA
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Conjugate acid oxidation of benzyl esters with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) and trifluoroacetic acid (TFA) was applied to the binding site analysis of ester linkages between lignin and glucuronoxylan in Fagus crenata wood.Based on the conjugate acid DDQ-oxidation of a watersoluble lignin-carbohydrate complex (LCC-WE) from the beech wood, the frequency of the ester bonds between the lignin and glucuronic acid residue of glucuronoxylan was determined to be 1.6 per molecule of LCC-WE. - Key words: Fagus crenata; Fagaceae; lignin-carbohydrate complex (LCC); 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ).
- Imamura, Takeshi,Watanabe, Takashi,Kuwahara, Masaaki,Koshijima, Tetsuo
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p. 1165 - 1174
(2007/10/02)
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- N-imidaxo[1,2-b]pyridazinyl carbamates
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Compounds of general formula (I) STR1 wherein R1 represents an optinally substituted carbocyclic or heterocyclic aryl group, or an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group; R2 represents an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl group or an optionally substituted carbocyclic or heterocyclic aryl or aralkyl group; R3 represents a hydrogen atom or an alkyl group; and either X represents an oxygen or sulphur atom, a group --CH2 -- or a group NR4 where R4 represents a hydrogen atom or a C1-4 alkyl group; and Y represents a group --CH2 -- or --CH2 CH2 -- X-Y together represent the group --CH=CH--; and salts and physiologically functional derivatives thereof are useful in the treatment of tumours. Processes for preparing the compounds, intermediates useful in their preparation, pharmaceutical compositions containing them and their use in the treatment of tumours are also described.
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