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Acta Pharmaceutica

The Journal of Croatian Pharmaceutical Society

4 Issues per year


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1846-9558
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Volume 59, Issue 4 (Dec 2009)

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Synthesis and preliminary screening of benzothiazol-2-yl thiadiazole derivatives for anticonvulsant activity

Nadeem Siddiqui
  • Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, New Delhi-110062, India
/ Arpana Rana
  • Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, New Delhi-110062, India
/ Suroor Khan
  • Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, New Delhi-110062, India
/ S. Haque
  • Department of Pharmacology, Faculty of Pharmacy, Hamdard University, New Delhi-110062, India
/ M. Arshad
  • Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, New Delhi-110062, India
/ Sharique Ahmed
  • Department of Biochemistry, Faculty of Medicine, 7th October University, Misurata, Libya
/ Waquar Ahsan
  • Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, New Delhi-110062, India
Published Online: 2009-11-16 | DOI: https://doi.org/10.2478/v10007-009-0031-x

Synthesis and preliminary screening of benzothiazol-2-yl thiadiazole derivatives for anticonvulsant activity

Various N-(5-chloro-6-substituted-benzothiazol-2-yl)-N'-(substituted phenyl)-[1,3,4]thiadiazole-2,5-diamines (5a-t) were designed and synthesized starting from substituted acetophenones. Structures of all the compounds were confirmed on the basis of spectral and elemental analyses. All the newly synthesized compounds were screened for their anticonvulsant activity and were compared with the standard drug phenytoin sodium. Interestingly, all the compounds showed protections against seizures in the range 50-100% indicative of the promising nature of the compounds against seizure spread. Compounds 5b and 5c showed complete protection against MES induced seizures.

Sinteza i preliminarna ispitivanja antikonvulzivnog djelovanja derivata benzotiazol-2-il tiadiazola

U radu je opisano dizajniranje i sinteza različitih N-(5-klor-6-supstituiranih benzotiazol-2-il)-N'-(supstituiranih fenil)-[1,3,4]tiadiazol-2,5-diamina (5a-t) polazeći od odgovarajućih acetofenona. Strukture spojeva određene su na temelju spektroskopskih podataka i elementarne analize. Ispitano je antikonvulzivno djelovanje svih novosintetiziranih spojeva i uspoređeno s djelovanjem natrijeve soli fenitoina. Spojevi 5b i 5c pružaju potpunu zaštitu od konvulzija uzrokovanih MES-om, a svi spojevi štite od konvulzija u rasponu od 50 do 100 %.

Keywords: benzothiazole; thiadiazole; anticonvulsant; neurotoxicity; hepatotoxicity

Keywords: benzotiazol; tiadiazol; antikonvulziv; neurotoksičnost; hepatotoksičnost

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About the article


Published Online: 2009-11-16

Published in Print: 2009-12-01



Citation Information: Acta Pharmaceutica, ISSN (Online) 1846-9558, ISSN (Print) 1330-0075, DOI: https://doi.org/10.2478/v10007-009-0031-x. Export Citation

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