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SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL IODOPHTHALAZINEDIONE DERIVATIVES AS ANTICONVULSANT AGENTS

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Last updated: 03 Jan 2025

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Abstract

In view of their expected anticonvulsant activity, some new derivatives of phthalazine   (I, II, IIIa-f, IV, V, VIa-f and VIIa-h) were designed and synthesized by condensation of Iodophthalic anhydride with hydrazine hydrate to produce iodophthalazindione I which heating with Alc. KOH to give compound II. The compounds IIIa-f resulted from condensation of compound II with different alkylcholoroacetates. Compound IIb reacted with ammonia, hydrazinehydrate and different alkyl amines resulted compounds IV, V (hydrazide) and VI respectively. Compound V (hydrazide)  react with different aromatic aldehydes to produce compounds VIIa-h. the final compounds were structurally elucidated basis of IR , 1HNMR, Ms Carbon, hydrogen and nitrogen analysis. The final compounds were evaluated for anticonvulsant activity using pentylenetetrazole (ptz) to induce convulsion and phenobarbital as reference standard. The compounds I, II, IV, V, VIa, VIb, VIc, VId, VIf, VIIa, VIIb, VIIc and VIIgwere active than Phenobarbital as standard reference the remain compounds less active than Phenobarbital. To under stand the molecular significant of these results we compared the binding modes of these compounds. Acknalewlgement: Many thanks for Dr. Ahmed Mansour assist. Prof. of pharmacology and Dr. Farg Sherbiny lecturer of organic chemistry

DOI

10.21608/ajps.2012.7146

Keywords

phthalazine, phthalazinedione and anticonvulsant agent

Authors

First Name

Rezk

Last Name

Ayyad

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Affiliation

Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt

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Volume

45

Article Issue

1

Related Issue

1362

Issue Date

2012-03-01

Receive Date

2018-05-14

Publish Date

2012-03-01

Page Start

1

Page End

13

Print ISSN

1110-1644

Online ISSN

2535-1958

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https://ajps.journals.ekb.eg/article_7146.html

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https://ajps.journals.ekb.eg/service?article_code=7146

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Original Article

Type Code

518

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Journal

Publication Title

Al-Azhar Journal of Pharmaceutical Sciences

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https://ajps.journals.ekb.eg/

MainTitle

SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL IODOPHTHALAZINEDIONE DERIVATIVES AS ANTICONVULSANT AGENTS

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Article

Created At

22 Jan 2023