Enaminones 8: CoMFA and CoMSIA studies on some anticonvulsant enaminones
نویسندگان
چکیده
منابع مشابه
Evaluation of Anticonvulsant Actions of Dibromophenyl Enaminones Using In Vitro and In Vivo Seizure Models
Epilepsy and other seizure disorders are not adequately managed with currently available drugs. We recently synthesized a series of dibromophenyl enaminones and demonstrated that AK6 and E249 were equipotent to previous analogs but more efficacious in suppressing neuronal excitation. Here we examined the actions of these lead compounds on in vitro and in vivo seizure models. In vitro seizures w...
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Present work employs the QSAR formalism to predict the ED(50) anticonvulsant activity of ringed-enaminones, in order to apply these relationships for the prediction of unknown open-chain compounds containing the same types of functional groups in their molecular structure. Two different modeling approaches are applied with the purpose of comparing the consistency of our results: (a) the search ...
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Cinco enaminonas 4a-e, derivadas da reação do ânion da 2,4,4-trimetil-2-oxazolina com acetato de etila, benzoato de etila, ciclohexanoato de etila, hexanoato de etila e p-metil benzoato de etila, respectivamente, foram preparadas e caracterizadas por RMNH, RMNC, FTIR e EM. As enaminonas 4a e 4b também foram analisadas pela técnica de difração de raios-X. A enaminona 4a cristalizou-se no sistema...
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Selective S1P(1) receptor agonists have therapeutic potential to treat a variety of immune-mediated diseases. A series of 2-imino-thiazolidin-4-one derivatives displaying potent S1P(1) receptor agonistic activity were selected to establish 3D-QSAR models using CoMFA and CoMSIA methods. Internal and external cross-validation techniques were investigated as well as some measures including region ...
متن کاملThe Chemistry of Enaminones, Diazocarbonyls and Small Rings: Our Contribution
Depois de trinta e dois anos no Brasil e de aposentada da Universidade Estadual de Campinas, a autora gostaria de apresentar este resumo representando uma grande parte da pesquisa em metodologia sintética desenvolvida pelos grupos de pesquisa de Albert J. Kascheres e da autora no Instituto de Química da Universidade Estadual de Campinas. Contribuições foram feitas nas áreas de enaminonas, diazo...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry
سال: 2009
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2008.11.014