Reaction of 2-amino-5-aryl-1,3,4-oxadiazoles with compounds with activated double bonds

Alekseeva, V. Ya.; Viktorovskii, I. V.; Yakovlev, S. I.; V'yunov, K. A.

doi:10.1007/bf00756427

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General Procedures For Preparation Of 5-{2-[(2-halobenzyl)thi1

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2008

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“…The resulting solution was neutralized with sodium bicarbonate solution. The solid thus separated out was filtered, washed with water, dried and recrystallized from ethanol [17]. -1,3,4-oxadiazol-2-amine (3a…”

Section: General Procedures For Preparation Of 5-{2-[(2-halobenzyl)thimentioning

confidence: 99%

Synthesis and Pharmacological Evaluation of New 2-Substituted-5-{2-[(2-halobenzyl)thio)phenyl}-1,3,4-oxadiazoles as Anticonvulsant Agents

Zarghi

2008

Sci Pharm

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A new series of 2-substituted-5-{2-[(2-halobenzyl)thio)phenyl}-1,3,4oxadiazoles was designed, synthesized and investigated for anticonvulsant activities. The designed compounds contain the main essential pharmacophore for binding to the benzodiazepine receptors. Conformational analysis and superimposition of energy minima conformers of designed molecules on estazolam, a known benzodiazepine receptor agonist, revealed that the main characteristics of the proposed benzodiazepine pharmacophore were well matched. Electroshock and pentylenetetrazole-induced lethal convulsion tests showed that some of the synthesized compounds had significant anticonvulsant activity. The structureactivity relationship study of these compounds indicated that the introduction of an amino group at position 2 of 1,3,4-oxadiazole ring and a fluoro substituent at the ortho position of the benzylthio moiety had the best anticonvulsant activity.

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Section: General Procedures For Preparation Of 5-{2-[(2-halobenzyl)thimentioning

confidence: 99%

Synthesis and Pharmacological Evaluation of New 2-Substituted-5-{2-[(2-halobenzyl)thio)phenyl}-1,3,4-oxadiazoles as Anticonvulsant Agents

Zarghi

2008

Sci Pharm

View full text Add to dashboard Cite

show abstract

Reaction of 2-amino-5-aryl-1,3,4-oxadiazoles with compounds with activated double bonds

Cited by 1 publication

References 2 publications

Synthesis and Pharmacological Evaluation of New 2-Substituted-5-{2-[(2-halobenzyl)thio)phenyl}-1,3,4-oxadiazoles as Anticonvulsant Agents

Synthesis and Pharmacological Evaluation of New 2-Substituted-5-{2-[(2-halobenzyl)thio)phenyl}-1,3,4-oxadiazoles as Anticonvulsant Agents

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