Literature DB >> 16134091

Synthesis and reactions of some new substituted pyridine and pyrimidine derivatives as analgesic, anticonvulsant and antiparkinsonian agents.

Abd El-Galil E Amr1, Hayam H Sayed, Mohamed M Abdulla.   

Abstract

A series of substituted pyridine and pyrimidine derivatives were synthesized as analgesic, anti convulsant, and antiparkinsonian agents by using compounds 1, 2, and 9 as starting materials. Pyr idino-imide derivative 3 was prepared by condensation of 1 with tetrachlorophthalic anhydride and compounds 4 and 5 were also obtained by reaction of compound 1 with 1,2,4,5-benzene-tetra carboxylic dianhydride and 1,4,5,8-naphthalenetetracarboxylic dianhydride, respectively. Similarly, compound 2 was reacted with previous anhydrides to afford the corresponding imide 6 and bis-imide derivatives 7 and 8, respectively. Bis-arylmethylene derivatives 9 were treated with hydrogen peroxide to afford the corresponding bis-oxiranocycloalkanone derivatives 10, which condensed with thiourea to give the corresponding thioxopyrimidine derivatives 11. Treatment of compound 11 with chloroacetic acid in the presence of anhydrous sodium acetate afforded the corresponding thiazolopyrim idine derivative 12 which condensed with aromatic aldehydes in acetic acid/acetic anhydride to give arylmethylene derivative 13. Also, compounds 13 could be prepared by reaction of compounds 11 with chloroacetic acid, aromatic aldehydes, and sodium acetate in a mixture of acetic acid and acetic anhydride. The pharmacological screening showed that many of these obtained compounds have good analgesic, anticonvulsant, and antiparkinsonian activities comparable to Valdecoxib, Carbamazepine, and Benzatropine as reference drugs.

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Year:  2005        PMID: 16134091     DOI: 10.1002/ardp.200500982

Source DB:  PubMed          Journal:  Arch Pharm (Weinheim)        ISSN: 0365-6233            Impact factor:   3.751


  7 in total

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2.  Methyl 2-{6-[(1-meth-oxy-1-oxopropan-2-yl)amino-carbon-yl]pyridine-2-carboxamido}-propano-ate.

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3.  Synthesis and antibacterial activities of novel 2,5-diphenylindolo[2,3-e] pyrazolo[1',5':3",4"]pyrimido[2",1"-c] [1,2,4]triazines.

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4.  Synthesis of chiral macrocyclic or linear pyridine carboxamides from pyridine-2,6-dicarbonyl dichloride as antimicrobial agents.

Authors:  Rashad A Al-Salahi; Mohamed A Al-Omar; Abd El-Galil E Amr
Journal:  Molecules       Date:  2010-09-20       Impact factor: 4.411

5.  Synthesis and Cytotoxic Effect of Some Novel 1,2-Dihydropyridin-3-carbonitrile and Nicotinonitrile Derivatives.

Authors:  Eman M Flefel; Hebat-Allah S Abbas; Randa E Abdel Mageid; Wafaa A Zaghary
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6.  Synthesis, Molecular Docking and in Vitro Screening of Some Newly Synthesized Triazolopyridine, Pyridotriazine and Pyridine⁻Pyrazole Hybrid Derivatives.

Authors:  Eman M Flefel; Walaa I El-Sofany; Mahmoud El-Shahat; Arshi Naqvi; Eman Assirey
Journal:  Molecules       Date:  2018-10-06       Impact factor: 4.411

7.  Synthesis and antitumor activity against HepG-2, PC-3, and HCT-116 cells of some naphthyridine and pyranopyridinecarbonitrile derivatives.

Authors:  S F Mohamed; N A Abdel-Hafez; A E Amr; H M Awad
Journal:  Russ J Gen Chem       Date:  2017-08-02       Impact factor: 0.868

  7 in total

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