- 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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- Synthesis of C-alkylcalix[4]arenes, 6. - The interaction of resorcin[4]arenes with Fe(III) in chloroform
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Resorcinarene octamethyl ethers, bearing carboalkyloxy groups in the side chains, have been shown to interact with Fe(III) in organic media. 1H- NMR studies, carried out using Ga(III) instead of Fe(III), suggest that these systems have two active sites of interaction, the first located at the aromatic moiet and the other in the vicinity of the carbonyl groups. As a confirmation of this, resorcinarenes without carbonyl groups in the side chains have been found to exhibit only one active site. Notably, in the latter case the interaction results in configurational changes.
- Botta, Bruno,Delle Monache, Giuliano,Ricciardi, Paola,Zappia, Giovanni,Seri, Catia,Gacs-Baitz, Eszter,Csokasi, Pal,Misiti, Domenico
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p. 841 - 847
(2007/10/03)
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- Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides
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A series of substituted 6-methoxysalicylamides were synthesized from their corresponding 2,6-dimethoxybenzamides by demethylation of one methoxy group with boron tribromide. Substituted 6-methoxysalicylamides having a lipophilic aromatic substituent in the 3-position para with respect to the methoxy group, e.g. a bromo or an iodo atom or an ethyl or a propyl group, and having an (S)-N-(1-alkyl-2-pyrrolidinyl)methyl moiety as the side chain were found to be potent blockers of [3H]spiperone binding in vitro and potent inhibitors of the apomorphine syndrome in the rat. Similar to remoxipride but in contrast to haloperidol, some of the substituted salicylamides show a 10-20 fold separation between the dose that inhibits hyperactivity and that which inhibits stereotypy. It was concluded that, besides the requirement of a lipophilic substitutent in the position para to the methoxy group for antidopamine activity in vivo, the formation of a coplanar six-membered pseudoring involving the amide moiety and the methoxy group is a structural requirement for activity in vitro.
- de Paulis,Kumar,Johansson,Raemsby,Florvall,Hall,Angeby-Moeller,Ogren
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p. 1263 - 1269
(2007/10/02)
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- ISOMERISATION OF ο-ALKENYL SUBSTITUTED CYCLOHEXANE-1,3-DIONE ENOL DERIVATES USING RHODIUM CATALYSIS. A PRACTICAL SYNTHESIS OF SUBSTITUTED RESORCINOLS
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Treatment of the ο-alkenyl substituted cyclohexane-1,3-dione enol derivates (1), (11), and (13) with rhodium trichloride trihydrate leads to the corresponding resorcinol derivates (2), (12), and (15) respectively.By contrast, the RhCl3.3H2O catalysed isomerisations of the related enol ethers (5) and (9) instead produce the dienones (6) and (10) respectively.
- Blagbrough, Ian S.,Pattenden, Gerald,Raphael, Richard A.
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p. 4843 - 4846
(2007/10/02)
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