ChemInform Abstract: Synthesis of Novel Pyrazole Derivatives and Evaluation of Their Antidepressant...
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ChemInform 2009, 40, issue 48 © 2009 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim www.cheminform.wiley-vch.de Pyrazole derivatives R 0180 Synthesis of Novel Pyrazole Derivatives and Evaluation of Their Antidepressant and Anticonvulsant Activities. — Carboxylic acid hydrazides (I) react with ethene- tetracarbonitrile (II) with formation of pyrazoletricarbonitriles (III) as major and di- acylhydrazines (IV) as minor products. Heating of equimolar amounts of (I) and dieth- yldicyanobutenedioate (V) yields the oxadiazole (VI) and pyrazolone derivatives (VII). Compounds (IVa) and (IVb) markedly induce antidepressant activity nearly equal twice the activity of imipramine. Further compounds including (IIIc), (IVc), and (VII) display good antidepressant activity. Moreover, (VIIa), (VIIb), and (VIId) display remarkable protective effects against clonic seizures. — (ABDEL-AZIZ*, M.; ABUO-RAHMA, G. E.-D. A.; HASSAN, A. A.; Eur. J. Med. Chem. 44 (2009) 9, 3480-3487; Dep. Med. Chem., Fac. Pharm., Minia Univ., Minia, Egypt; Eng.) — H. Hoennerscheid 48- 129
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Transcript of ChemInform Abstract: Synthesis of Novel Pyrazole Derivatives and Evaluation of Their Antidepressant...
www.cheminform.wiley-vch.de
Pyrazole derivativesR 0180 Synthesis of Novel Pyrazole Derivatives and Evaluation of Their Antidepressant
and Anticonvulsant Activities. — Carboxylic acid hydrazides (I) react with ethene-tetracarbonitrile (II) with formation of pyrazoletricarbonitriles (III) as major and di-acylhydrazines (IV) as minor products. Heating of equimolar amounts of (I) and dieth-yldicyanobutenedioate (V) yields the oxadiazole (VI) and pyrazolone derivatives (VII). Compounds (IVa) and (IVb) markedly induce antidepressant activity nearly equal twice the activity of imipramine. Further compounds including (IIIc), (IVc), and (VII) display good antidepressant activity. Moreover, (VIIa), (VIIb), and (VIId) display remarkable protective effects against clonic seizures. — (ABDEL-AZIZ*, M.; ABUO-RAHMA, G. E.-D. A.; HASSAN, A. A.; Eur. J. Med. Chem. 44 (2009) 9, 3480-3487; Dep. Med. Chem., Fac. Pharm., Minia Univ., Minia, Egypt; Eng.) — H. Hoennerscheid
48- 129
ChemInform 2009, 40, issue 48 © 2009 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
