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Synthesis, anticonvulsant activity and molecular properties prediction of dialkyl 1-(di(ethoxycarbonyl)methyl)-2,6-dimethyl-4-substituted-1,4-dihydropyridine-3,5-dicarboxylates.

Abstract：

:The synthesis and anticonvulsant properties of new N-diethylmalonyl derivatives of nifedipine and other isosteric analogues (7a-7n) were described. Anticonvulsant screening was performed by subcutaneous pentylenetetrazole (scPTZ) and maximal electroshock (MES) induced seizures tests. Majority of the compounds were effective in scPTZ and MES screens. Compound 7k showed good activity displaying maximum protection, which may be due to the presence of styryl moiety at position 4 of 1,4-dihydropyridine nucleus and the methyl groups of diester functionality. Compounds 7a-7d, 7g, 7i and 7k obeyed the Lipinski's "rule of five" and have drug-likeness. Based on computational prediction of molecular and pharmacokinetic properties, it was found that the compounds have good oral absorption.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Prasanthi G,Prasad KV,Bharathi K

doi

10.1016/j.ejmech.2013.12.001

subject

Has Abstract

pub_date

2014-02-12 00:00:00

pages

97-104

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(13)00777-0

journal_volume

73

pub_type

杂志文章

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