SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL IODOPHTHALAZINEDIONE DERIVATIVES AS ANTICONVULSANT AGENTS | ||
| Al-Azhar Journal of Pharmaceutical Sciences | ||
| Article 1, Volume 45, Issue 1 - Serial Number 45, March 2012, Pages 1-13 PDF (541.67 K) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/ajps.2012.7146 | ||
| Author | ||
| Rezk Ayyad | ||
| Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt | ||
| 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 | ||
| Keywords | ||
| phthalazine; phthalazinedione and anticonvulsant agent | ||
|
Statistics Article View: 444 PDF Download: 522 |
||
